Current Issue : October-December Volume : 2012 Issue Number : 4 Articles : 43 Articles
In order to enhance the delivery of poorly-soluble drugs, aquasomes will be the promising nanocarrier as the novel drug delivery system. These are nanoparticulate carrier systems with three layered self-assembling composition with ceramic carbon nanocrystalline particle core coated with polyhydroxy oligomers. Subsequently drug covalently bonded to outer coating. Three types of core materials are mainly used for producing aquasomes: tin oxide, nanocrystalline carbon ceramics (diamonds) and brushite (calcium phosphate dihydrate). Calcium phosphate is the core of interest, owing to its natural presence in the body. Aquasome deliver their content through specific targeting, molecular shielding and slow sustained release process. The polyhydroxy oligomer layer ensures that they have the dual advantage of protecting the native conformation of drugs and imparting water-like properties for enhanced dissolution. The nano-size dimensions ensure superior surface area for the enhanced dissolution of hydrophobic molecules....
Cancer is a diseases characterized by an uncontrolled proliferation of cells. There are over 200 different types of cancer, each of which gains its nomenclature according to the type of tissue the cell originates in. Many patients who succumb to cancer do not die as a result of the primary tumor, but because of the systemic effects of metastases on other regions away from the original site. One of the aims of cancer therapy is to prevent the metastatic process as early as possible. There are currently many therapies in clinical use, and recent advances in biotechnology and nanotechnology for fight against cancer. Nanomaterials such as carbon nanotubes (CNTs) have unique properties that can be exploited for drug delivery in cancer. CNTs are tubular materials with nanometer-sized diameters and axial symmetry, giving them unique properties that can be exploited in the diagnosis and treatment of cancer. In addition, CNTs have the potential to deliver drugs directly to targeted cells and tissues. Alongside the rapid advances in the development of nanotechnology-based materials, elucidating the toxicity of nanoparticles is also imperative. Hence, in this review, we seek to explore the biomedical applications of CNTs, with particular emphasis on their use as therapeutic platforms in oncology....
Targeted drug delivery systems have been used to deliver drugs in the disease sites of the body. This may reduce potential side effects of drugs and improve their therapeutic effects. The blood brain barrier, formed by brain capillary endothelial cells, represents the major obstacle for drug entry into the central nervous system. Development of brain targeting drug delivery system help in the treatment of disorders related to brain. The most challenging research topic in pharmaceutical sciences is brain targeting drug delivery system. Most of the drugs do not reach brain effectively because of presence of Blood-Brain Barrier (BBB). There are various strategic approaches that have been proposed for brain drug delivery system. By localizing drugs at their desired site of action one can reduce toxicity and increase treatment efficiency. In response to the insufficiency in conventional delivery mechanisms, aggressive research efforts have recently focused on the development of new strategies to more effectively deliver drug molecules to the CNS. This review intends to detail the recent advances in the field of brain-targeting, rational drug design approach and drug delivery to CNS. To illustrate the complexity of the problems that have to be overcome for successful brain targeting, a brief intercellular characterization of the blood–brain barrier (BBB) is also included....
An implant tablet of disulfiram (DSF) was developed in order to achieve its sustained supply and its release was evaluated in vitro and in vivo. In present work an attempt was made to formulate and evaluate a sustained release implant of Disulfiram and biodegradable polymer Chitosan. The effect of different proportion of polymer Chitosan (26.66, 33.33 and 40.00 % w/w) and Disulfiram on the drug release kinetics was also studied. The prepared implants were evaluated for hardness, thickness and diameter. Invitro drug release of Disulfiram was studied using three different methods, i.e. Vial, Paddle over Disk and Basket. In vivo release was studied by implanting the implants subcutaneously in mice of equal age and weight group. In vivo drug release from Disulfiram Chitosan implant was studied. The in vitro and in vivo release data was also subjected to Zero order, First order, Higuchi and Korsmayer Peppas kinetic treatment....
The basic structure of cubosomes includes honeycombed structures separating the two internal aqueous channels along with large interfacial area. Now a days the self assembled cubosomes applications as the drug delivery system is attracting great attention since its discovery. The cubosomes generally have different internal cubic structure along with variant composition related to the drug loading modalities. The cubosomes have huge potential in drug nano formulations for melanoma therapy due to their potential advantages consisting high drug payloads. The cubosomes having high internal surface area along with cubic crystalline structures and also exhibit several potential advantages like simple preparation method, biodegradability of lipids, the ability of encapsulating hydrophobic, hydrophilic, amphiphilic substances, targeting along with controlled release of bioactive agents. The preparation of cubosomes mostly involves simple emulsification of monoglycerides along with a polymer accompanied via sonication and homogenization. There are two different method are available for preparation of cubosomes includes top-down and bottom-up techniques....
The aim of the present investigation is to develop a pH-dependent system for colon specific drug delivery of Budesonide by using enteric coating of Eudragit S100. Budesonide insoluble in water and unstable in gastric environment was formulated into pH-dependent tablets coated with Eudragit S100. Budesonide tablets were prepared by weight granulation method and coated with Eudragit S100 by conventional pan coating machine. All the prepared granules were evaluated for the flow properties by studied the angle of repose, compressibility index and Hauser’s ratio. The physical properties of the tablets including weight variation, friability, hardness, content uniformity and release profile in simulated gastric fluid, simulated intestinal fluid and phosphate buffer 7.4 containing 4% rat caecal and colonic contents were studied. The result shows that the 10% coating over the tablets shows 0% drug release in the gastric and intestinal medium. The 100% drug release shows after 12hrs in the phosphate buffer 7.4 containing rat caecal content 4%. The results of the present study have demonstrated that the pH-dependent tablet system is a promising vehicle for preventing rapid degradation in gastric environment and improving oral bioavailability of Budesonide for the treatment of ulcerative colitis and crohn’s disease....
Recently self emulsifying drug delivery system has gained popularity among all other formulation strategies used for poorly water soluble drugs. The objective of the present study was to develop and characterize self-micro emulsifying drug delivery system (SMEDDS) of the poorly water-soluble drug, Glibenclamide (GBD). Solubility of GBD was determined in various oily vehicles. From the solubility study, better solubility was seen in Captex 200P (oil), Cremophor RH40 (surfactant), Capmul MCM C8 (co-surfactant). Phase diagrams were constructed to identify efficient self-emulsification region using oils, surfactants, and cosurfactants in aqueous environment. Formulations were prepared according to 32 full factorial design using two variables oil : Smix (X1) and S : Cos (X2) and their effects were evaluated for three responses like droplet size, self emulsification time and % drug release at 15 min. All the nine batches were assessed for dispersibility, emulsification time, % transmission, viscosity, zeta potential, particle size, electro conductivity, drug content, and dissolution studies. In vitro drug dissolution was carried out using USP type-II apparatus and compared with that of marketed GBD tablet (Daonil®) and dissolution was found to be increased in case of SMEDDS than marketed tablet formulation. Effects of various formulation variables on different responses were extracted out by using Design Expert® software. From that study it was found that X1 variable negatively affect self emulsification time while droplet size was negatively affected by X2 variable. From all desired responses batch G6 was considered as optimized batch. Optimized batch was found to be stable at ambient conditions for one month of storage....
Lisinopril is the drug of choice in hypertension. Bioavailability of the drug is 25% of orally administered dose. An attempt was made to provide safe medicine meeting pharmacokinetics requirement of plasma concentration by formulating a sublingual tablet of Lisinopril. The Objective of present study is to develop the sublingual tablet of Lisinopril and improve its bioavailability, in view to maximize therapeutic effect of the drug. The directly compressed tablet of Lisinopril was formulated using Mannitol, Micro Crystalline Cellulose and Kyron T-314 as super disintegrant. Formulation (F1-F7) was evaluated for disintegration time and in vitro release study. Further the optimized sublingual formulation (F6) and marketed formulation was subjected to in-vivo comparative bioavailability study using white New Zealand rabbits.It was observed that concentration of Micro Crystalline Cellulose, Kyron T-314 has significant effect on the disintegration time of Lisinopril sublingual tablet formulations. The super disintegrant concentration 5% w/w (Kyron T-314) was found optimum in all tablet formulations. AUC of optimized sublingual tablet and oral tablet are 925.35µg×h/mL and 641.97 µg×h/mL with Cmax of 60.80 µg/mL and 41.21 µg/mL and Tmax of 4 h and 4 h respectively. The bioavailability of optimized sublingual tablet of Lisinopril was improved by 1.44 times as compared to conventional oral marketed tablet of Lisinopril. The present approach of formulating sublingual tablet of Lisinopril would definitely improve bioavailability leading to reduced conventional dose of this drug. The administration of sublingual tablet becoming easy and it will improve patient compliance to therapy for hypertension for pediatrics, geriatric and bed ridden patient....
Nimesulide has been shown to have anti-inflammatory activity and is widely used in the long term therapy of rheumatoid arthritis, in alleviating pain and inflammation. However, its oral use is restricted due to its poor water solubility and some toxic effects. In order to alleviate the disadvantages associated with oral delivery, the transdermal delivery systems such as microemulsion gel with suitable organoleptic and rheological properties for topical administration have been developed. In addition, hydrogel containing carbopol 940 as a gelling agent were also prepared. The apparent viscosity values and the rheological behavior for different gel formulations were measured before and after storage at different temperature were taken as measures for stability of network structure. The formulations were characterized for particle size, pH, zeta potential, drug entrapment efficiency, spreadability, and viscosity. The results showed that the size of particles were greatly affected by the concentration of surfactant and from PCS measurements, the size and polydispersity index of microemulsion gel were found to be 1.8μm±0.29 and 0.2±0.022 respectively. The zeta potential study showed good stability of the formulation. The drug release showed zero-order profile. Rheogram of the developed formulation showed Newtonian type of flow behavior....
The scientist faced many challenges in Ocular drug delivery system due to unique anatomy and physiology of eye. At the site of eye, ocular drug delivery system faces two types of barriers static and dynamic barrier. Static barriers consist of different segment of eye such as cornea, sclera, retina and blood- retinal barriers. In other way dynamic barriers consists choroidal and conjunctival blood flow, lymphatic clearance, and tear dilution. These both barriers affect the bioavailability of drugs. In recent year some new concept of drug delivery such as iontophoresis, liposome bioadhesive gels, ocular insert, contact lenses etc has been developed to overcome problems associated by static and dynamic barriers These formulation based approaches have high capacity to carry maximum concentration of drug at targeted site of eye. In this article, we have summarized the different types of commonly used ophthalmic formulations and compared the conventional formulations with the advanced formulation in many respects like their applicability, acceptance, characteristics and utility...
The literature is abounding with attempts made repeatedly and sometimes successfully to carry agents into the body through the intact skin by using lipid suspension. The success of systemic drug delivery from liposomal formulation after topical application is low because of the inability of such vesicles to pass through the narrow (< 30 nm) intercellular passage in the outer skin layers. Ethosomes and elastic liposomes also known as Transfersomes. These are modified lipid carriers that enable drugs to reach into deeper skin layers and/or the systemic circulation. These are soft, malleable vesicles tailored for enhanced systemic delivery of drugs. This article reviews the work carried out in vitro, in vivo in both animal and humans with various ethosomal and transfersomal formulations with particular emphasis on ethosomes. Ethosomes represent a lipid vesicular carrier system embodying ethanol in relatively high concentration and are very efficient in delivering drugs into and across the skin. Unlike classic liposomes, that are known to mainly deliver drugs to outer layers of skin, ethosomes penetrate through the stratum corneum and deliver drugs to the deeper layers of skin....
The present study sought to examine the effects of minocycline (MH), its nanoparticles (MH NP) and ligand coated nanoparticles (coated MH NP) on anxiety in mice. The treatment protocol included injections of MH (100 mg/kg, i.p.), MH NP (equivalent to 100 mg/kg MH, i.p.) and coated MH NP (equivalent to 100 mg/kg MH, i.p.) at two different time intervals. The novel Elevated Plus Maze (EPM) test and Light/dark test were employed to assess anti-anxiety properties of the MH, MH NP and coated MH NP. The experimental outcome revealed that neither EPM nor Light/dark test exhibited any alteration in anxiety levels, although MH has been reported to exhibit significant antidepressant activity, comparable to that of amitriptyline. It may be concluded that although nanoparticles improved brain uptake of MH, but still they may not be a suitable candidate for therapeutic management of anxiety....
Lornoxicam is a non-steroidal anti-inflammatory drug with analgesic property which is used for the better treatment of pain and arthritics. Moreover the site of absorption of lornoxicam is in the intestine and the short half life of 3 to 4 hr. Due to the short half life the frequency of administration is more and it produced peptic ulceration, gastrointestinal disturbance and gastric bleeding. Therefore the present investigation was concerned with the development of the sustained release matrix tablets, which after oral administration were designed to prolong the duration of action. Lornoxicam Sustained release matrix tablet was prepared by wet granulation method using Acrypol 912G and Eudragit RSPO in formulation. 32 full factorial design applied for the optimization of satisfactory batch. Acrypol 912G(X1) and Eudragit RSPO(X2) selected as independent parameter % cumulative drug release at 2, 6 and 10 hr were selected as dependent parameter. The dissolution profile of all the batches was fitted to zero-order, first-order, Higuchi, Hixson Crowell and K-Peppas models to ascertain the kinetic modeling of drug release. From the result showed that Q2, Q6 and Q10 strongly depend on the independent parameter. In vitro drug release of factorial batches compared with theoretical release profile and indicate that batch F7 was most satisfactory batch. It was observed that the combination ratio of Acrypol 912G and Eudragit RSPO have distinct effect on in vitro drug release profile. Release rate of lornoxicam was decrease with increased the total polymer concentration. Mechanism of drug release was explained by K-Peppas equation and found that diffusion-erosion occurs by anomalous transport (non-Fickian) release is predominant....
In the recent years, scientific and technological advancements have been made in the research and development of novel drug delivery systems by overcoming physiological troubles such as short gastric residence times and unpredictable gastric emptying times. Several approaches are currently utilized in the prolongation of the gastric residence times, including floating drug delivery systems, swelling and expanding systems, polymeric bioadhesive systems, modified-shape systems, high-density systems and other delayed gastric emptying devices. Developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. This review also summarizes the in vitro techniques, in vivo studies to evaluate the performance and application of floating systems, and applications of these systems. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form....
The aim of present work was to formulate and evaluate novel capsule containing two drugs to treat the prime cause of Gastro Esophageal Reflux Disease (GERD). The system consist of two dosage forms ie-Pantoprazole enteric coated microspheres and Itopride HCl sustained release floating tablet. Pantoprazole microspheres were prepared by spray drying technique while itopride HCl sustained release floating tablet was prepared by direct compression method.Both of the dosage forms were prepared by using 22 full factorial design For microspheres, Independent variables chosen were Drug: Polymer ratio and Feed flow rate whereas independent variables for sustained release floating tablet were concentration of retardant and concentration of gas generating agent. The formulated Microspheres were characterised for Encapsulation Efficiency, Particle size analysis, XRD, SEM studies and In-vitro drug release while sustained release floating tablet was characterised for floating lag time and floating time, micromeritic properties of powder blend, % water uptake, friability test, hardness test, in-vitro drug release study etc....
The purpose of present study outlines a systematic approach for designing and development of Tolterodine Tartarate floating tablets to enhance the bioavailability and therapeutic efficacy of the drug. Floating tablets of Tolterodine Tartarate have shown sustained release thereby proper duration of action at a particular site and are designed to prolong the gastric residence time after oral administration. Different formulations were formulated by direct compression technique using HPMC K15M and Xanthan gum (floating agent) as polymers along with sodium bicarbonate and citric acid as gas generating agent. The formulations were evaluated for their physicochemical properties, buoyancy lag time, total floating time, swelling index and invitro drug release. It was found that the hardness of the tablets affects the Buoyancy characteristic of the dosage form. All nine formulations possessed good floating properties with total floating time between 9 – 12 hrs. The invitro cumulative % drug release of the formulations F1A, F1B, F2A, F2B, F3A and F3B were 102.85%, 101.32%, 100.2%, 99.98%, 99.28% and 97.25%.The F2B formulation showed the best release....
Paracetamol is an anti‐inflammatory analgesic agent indicated for acute and chronic treatment of rheumatoid arthritis. Paracetamol is poorly water soluble and may show dissolution limited absorption. Here,solid dispersion(SDs) of paracetamol with diff. Carrier (PEG 4000, PEG 6000, β-cyclodextrine) by the physical mixing method, kneading method and solvent evaporation method were prepared using 1:2, 1:4 and 1:6 ratio. The SDs was characterized in physical appearance, solubility, Drug content, IR, and in vitro dissolution studies. Solubility of paracetamol from SDs increased in distilled water. The drug content was found to be high and uniformly distributed in the all formulations. The prepared dispersion showed a marked increase in the dissolution rate of paracetamol than that of pure drugs. The dispersion with β-cyclodextrine (1:6) by kneading method (F24) showed faster dissolution rate (100.98%) as compared to other dispersions. The dissolution of the Paracetamol could be improved by solid dispersion technique may be due to increase wettability and hydrophilic nature of carriers....
In the present study, the sustained release hydrophilic matrix tablets of diclofenac sodium have been formulated using the direct compression technique with almond gum as the natural hydrophilic matrix former. The formulated tablets were evaluated and before the formulation, the almond gum was even evaluated to check out its purity through the parameters like Ash value, flow properties, water absorption test and swelling index. As the method of preparation is direct compression the initial powder blend was evaluated for flow properties. Finally after performing the evaluation of the sustained release hydrophilic matrix tablets of the diclofenac sodium which is having a very less half-life of around 1-2hrs, it was found that the formulation F3 having 45mg of the almond gum had shown optimum drug release after a time period of 24hrs indicating that the required sustained release can be achieved with that concentration of gum in the formulation. In the present scenario the use of the natural gums would help in reducing the severe side effects caused by the synthetic products and the almond gum had proved to be an efficient hydrophilic matrix forming polymer....
Floating Sustained release delivery systems for oral dosing are effective in achieving optimal therapy with drugs that have a narrow therapeutic range of blood concentration which eliminate rapidly. The present work involves use of gastric floating drug delivery system (GFDDS) for Stavudine which is primarily absorbed in the stomach and upper intestine segments. The main objective of the present work was to formulate and evaluate the regiospecific floating tablet of Stavudine. Stavudine gifted sample, Polymers such as HPMC K15M, HPMC K100M and Xanthan gum are selected for the formulation development. Pre formulation studies includes Drug excipient interaction studies were studied using Fourier Transform Infrared and Differential Scanning Calorimetery, developed formulation subjected for all the In-vitro evaluation studies for tablets, floating behavior was studied by In- vitro buoyancy studies, drug release behavior was studied by Kinetic modeling and the best formulation was loaded for stability studies under 40 ºC and 70% RH. From the above studies it was concluded that the formulation F5 showed the sustained drug release profile with good matrix integrity, less floating lag time with good total floating time and higher swelling index as compared with the selected batches. It may be concluded that the floating effervescent tablets of stavudine was feasible and may be manufactured with reproducible characteristics with the aid of HPMC K100M as a hydrophilic polymer....
The Aim of present work was to formulate Mucoadhesive buccal patches of Venlafexine Hydrochloride .The buccal region of the oral cavity is an attractive target for administration of the drug of Choice for increase bioavailability and prevent first pass metabolism of drug. Venlafexine Hydrochloride patches were prepared using HPMC K15, HPMC K100, PVP K30 Carbopol 934. Formulations were prepared using 23 Factorial Design by YATE’s method. FTIR and DSC data revealed that there is no interaction between Venlafexine Hydrochloride and polymers. The patches were evaluated for their thickness, Uniformity content, folding endurance, weight uniformity, Swelling index, tensile strength and surface pH. In-vitro studies of Venlafexine Hydrochloride -loaded patches in phosphate buffer (pH 6.8) exhibited drug release in the range of 84 to 99% in 8 hrs. Data of In-vitro release from patches were fit in to different mathematical models to explain kinetics. The models used were zero and first-order equations, Higuchi and Korsmeyer-peppas models. The Ex-vivo release study showed that patches could deliver drug to the oral mucosa. The results indicate that the mucoadhesive buccal patches of Venlafexine Hydrochloride may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability of Venlafexine Hydrochloride through buccal mucosa....
Matrix type transdermal films of Metoprlol Succinate, an antihypertensive drug were prepared using different polymers such as Ethyl Cellulose, HydroxyPropyl Methyl Cellulose (E15, E50) and Polyvinyl pyrrolidone in varied ratios. The present study aims to formulate and evaluate transdermal film for Metoprlol Succinate,The purpose of this research work was to develop and evaluate matrix-type transdermal therapeutic system of Metoprlol Succinate containing different ratios of hydrophilic and hydrophobic polymeric combinations. The formulations were prepared by using solvent casting technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. All formulations carried dimethyl sulfoxide (5%) as penetration enhancer and propylene glycol (30%) as plasticizer in chloroform and ethanol as solvent system. The diffusion studies were performed by using Franz diffusion cells. The formulation J with combination of polymers (HPMC E50+EC) emerged to be ideal formulation. The developed transdermal film increases the efficacy for the therapy of hypertension. Physicochemical parameters were characterized. The permeability studies indicate that the drug is suitable for transdermal drug delivery. The film were evaluated for various parameters like Thickness, Water-Vapour Permeability, Tensile Strength, moisture loss, moisture uptake, folding endurance, Drug Content, flatness, surface pH, swellability, % elongation, skin irritation study and Diffusion studies. The Optimized formulation containing HPMC E50+EC (3:2), with enhancer DMSO showed 70% drug release after 12 hours....
From the last two decades the main focus of formulation scientists is the modification of release pattern of active moiety from the dosage form and tailoring the same by modification of drug delivery system, also by changing the site of drug release. Taking the advantage of physiological studies and parameters affecting the drug release at the same time studies on newer excipients gave birth to the site specific and release modified novel drug delivery systems. In the present review the formulation and physiological aspects for developing the efficient Gastrortentive Floating Drug Delivery Systems (GRFDDS) are considered. Gastric retention time can be increased by different ways but when the drug has absorption window in the upper region of GI and/or shows erratic bioavailability. Such drugs can be well formulated by using low density inactives thus making it to float on the gastric content and get retained in stomach providing drug release near absorption window over a long time. In the present article various aspects like basic gastrointestinal tract physiology, rational for developing and types of GRFDDS, physiological and formulation factors affecting buoyancy and drug release to be considered while developing floating drug delivery systems, recent advances, potential applications for GRFDDS are considered....
The purpose of this research was to prepare a floating drug delivery system of acyclovir. Floating matrix tablets of acyclovir were developed to prolong gastric residence time and increase its bioavailability. The tablets were prepared by direct compression technique, using polymers such as HPMC K15M, HPMC K100M, Xanthan gum and effervescent agent sodium bicarbonate. Batches were carried out using HPMC K15 M,HPMC K-100 M, Xanthan gum in 1:0.25, 1:0.5, 1:0.75 and 1:1 ratio (drug: polymer) and evaluated. By fitting the data into zero-order, first-order, and Higuchi models, Peppas model we concluded that the release followed Higuchi diffusion kinetics and Peppas model. Storage of the prepared formulations at 40°C/75% relative humidity for 3 months showed no significant change in drug release profiles and buoyancy of the floating tablets. From evaluations we can conclude that natural gum i.e. Xanthan gum containing batches are most promising than HPMC K15 and K100 M. These floating tablets seem to be a promising gastroretentive drug delivery system....
Gold nanorods have potential applications in the area of drug delivery and photothermal therapy. These promises arises due to their unique optical and photothermal properties, the existence of some synthetic protocols that can tune the size and shape of the particles and modification regarding surface and conjugate drugs or molecules to the nanorods with relative biocompatibility of gold nanorods. The current utilization of gold nanorods as drug delivery vehicles along with their issues regarding dosage, toxicity and biological interactions are focused in this review....
Hot-melt granulation is an established process that has been used since the early 1930s, predominately in the plastics manufacturing industry, but also in the food processing industry. Currently, it is an emerging field in Novel drug delivery system. Hot Melt Granulation is becoming an important technology within the Pharmaceutical Industry as a means for formulating poorly water-soluble active pharmaceutical ingredients (API’s) and sustained release formulation. In this article containing marketed sustained release tablet compare with this formulation. First of all done authentication test for drug sample and got same result as per data, Differential scanning colorimetry and infra red spectroscopy for compatibility and ensure that whatever wax and polymer used in this formulation is compactable with drug, flow properties for flow of granules, compressibility. List of suitable three wax containing carnauba wax give good result, same way different grade of Hypromallose among them HPMCK100M give good result for sustained release formulation. Carnauba wax, Hypromallose and drug were observed better dissolution release profile for sustained release tablet formulation. There were got good result for this formulation. And last done the stability study of this product....
Most of the drugs that are emerging from contemporary drug discovery programs are poorly water-soluble often present formulators with considerable technical challenges. The absorption of such compounds when presented in the crystalline state to the gastrointestinal tract is typically dissolution rate-limited, and the drugs are typically BCS class II or class IV compounds. The rate and extent of absorption of class II compounds is highly dependent on the performance of the formulated product. These drugs can be successfully formulated for oral administration, but care needs to be taken with formulation design to ensure consistent bioavailability. Essentially the options available involve either reduction of particle size (of crystalline drug) or formulation of the drug in solution, as an amorphous system or lipid formulations. The performance of amorphous or lipid formulations is dependent on their interaction with the contents of the gastrointestinal tract, therefore, a formulation exercise should involve the use of techniques which can predict the influence of gut physiology. A major consideration is the fate of metastable supersaturated solutions of drug, which are formed typically after dispersion of the formulation and its exposure to gastrointestinal digestion. A better understanding of the factors which affect drug crystallization is required, and the introduction of standardized predictive in vitro tests would be valuable. The use of a lipid formulation classification system combined with appropriate in vitro tests will help to establish a database for in vitro–in vivo correlation studies. For lipophilic drugs, which display dissolution rate-limited absorption, SEDDS may be a promising strategy to improve the rate and extent of oral absorption. Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro- or nanoemulsions containing the solubilized drug. Owing to its miniscule globule size, the micro/nanoemulsified drug can easily be absorbed through lymphatic pathways, by passing the hepatic first-pass effect....
Nanomedicines an emerging field utilized for development of targeted therapies like in cancer and found most to date. The several side effects and low selectivity of conventional techniques in treatment of cancer is counter by application of drug loaded nanocarriers like liposomes. But, they lack capacity to encapsulate lipophilic drugs, found as leaky, unstable in biological fluids and in aqueous solutions for being commerlized and due to this the lipid nanocapsules technology emerged. They have potential applications to encapsulate lipophilic drugs efficiently and able to administered via intravenous route. The structure of lipid nanocapsules is hybrids between the polymeric nanocapsules and liposomes having lipoprotein like structure with size around 100 nm. The lipid nanocapsules (LNCs) have been used to encapsulate the different anticancer drugs like paclitaxel, docetaxel, etoposide etc....
Arteether is one of the artemisnin derivatives, which has proved to be efficient against acute severe falciparum malaria and can clear the parasite even in multiple drug resistant falciparum. However water insoluble nature of arteether limits the delivery of drug only by oral and i.m. parenteral route. This review highlights the properties of nanoparticles used in targeted drug delivery of arteether. Nanoparticles exploit biological pathways to achieve payload delivery to various cellular and intracellular targets. Different nanodispersion systems such as micelles, nanoemulsions and nanosuspensions along with advantages and disadvantages are discussed here. Various nano formulations represent promising means for delivering many bioactive agents, including peptide and protein drugs. The importance of these methods grew with the advancement in the understanding pharmacology of hydrophobic drugs as well as the ability to mass-produce these compounds....
Nanotechnology is a broad field which involves variety of applications including drug delivery, medical diagnostics etc. Among the nanoparticular drug delivery systems, nanosuspensions are colloidal systems stabilized by surfactants. These are dispersed systems in which the drug acts as dispersed phase in the nanosuspension. This review article throw light on the various features, additives used, manufacturing methods of nanosuspensions and reported nanosuspension for various drugs. This article focuses the application of nanosuspensions for delivery of drugs by oral route....
Solubility is an essential factor for drug effectiveness, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Nanosuspension technology can be used to improve the stability as well as the bioavailability of poorly soluble drugs. Nanosuspension are biphasic systems consisting of pure drug particles dispersed in an aqueous vehicle, stabilized by surfactants. These are simple to prepare and are more advantageous than other approaches. Techniques such as wet milling, high-pressure homogenization, emulsification-solvent evaporation and super critical fluid have been used in the preparation of nanosuspensions. It has the advantage of delivery by various routes, including oral, parenteral, pulmonary and ocular routes. The present article reviews the current methods used to prepare nanosuspensions and their application in drug delivery....
The nanocarrier systems involves different toxicity consist of physiological, physicochemical and molecular considerations. Normally nanocarriers show exposure through the skin, the respiratory tract, the gastrointestinal tract and the lymphatic systems. The property of nanocarrier systems to alter the properties of xenobiotics producing pharmaceutical changes in stability, solubility along with pharmacokinetic disposition and may induce cytotoxicity or genotoxicity. The enviourmental, health and safety issues are important factors to be studied while using the nanocarrier systems....
Oral dosage form has the short transit time of approximately 12 hrs through GIT. In intravenous drug delivery, the duration of drug action is short. In topical drug delivery, percutaneous absorption of most drugs is limited due to highly impermeable stratum -corneum. Implantable drug delivery devices are devoid of limitations associated with oral, intravenous, topical drug administration. Implantable delivery have advantages like Potential for controlled release, intermittent release, bio-responsive release Improved drug delivery. Osmotic pump, implant Ceramic composite system, Intraocular implant, Intrauterine implant, Transurethral implant are some of the examples of implantable delivery. Newer technologies include DURIN biodegradable implant technology which uses the biodegradable polyester excipients and have features like Superior delivery kinetics, Superior drug loading & stability, Fully biodegradable, History of safe use and Cost effective. ATRIGEL drug delivery technology consists of biodegradable polymers in biocompatible carrier. Atrigel system is somewhat viscous polymer solution, so currently marketed products available in pre-filled plastic syringes. Other technology is ALZAMER DEPOT TECHNOLOGY offers sustained delivery of therapeutic agents, including proteins, peptides, and other bio-molecules for up to a month with minimal initial drug burst & bio-erosion of the dosage form. SABER DEPOT TECHNOLOGY uses a high viscosity carrier such as sucrose acetate isobutyrate (SAIB), solvent. REGEL depot technology, IMPLANTABLE PUMP, PERISTALTIC PUMP, MEMS based IDD TECHNOLOGY, MICROCHIP DRUG DELIVERY DEVICE are some of the example of the newer technologies of implantable drug delivery....
The eye presents unique opportunities and challenges when it comes to the delivery of pharmaceutical dosage forms. The existing ocular drug delivery is fairly primitive and inefficient; however the design of ocular system is undergoing gradual transition from empirical to rational basis.To improve ocular drug bioavailability, there are significantefforts directed towards newer drug delivery systems for ophthalmic administration.Newer research in ophthalmic drug delivery systems is directed towards prolonging the contact time of the vehicle at the ocular surface, but which at the same time slow down the elimination of the drug. The conventional forms offer lot of drawbacks hence the novel drug delivery like ocular inserts was prepared which proved to be a boon to the developing drug ophthalmic drug delivery....
Ocular drug delivery is very challenging for the pharmaceutical scientist, as compared to other drug delivering systems. The major problem faced by the conventional dosage forms is the rapid precorneal drug loss. Hence, the main objective for the development of ocular insert is to increase the ocular bioavailability, contact time, residence time of the drug. Ocular inserts thus maintains the drug concentration in the desired range and increases the patient compliance and also it reduces the frequency of drug administration. The present article summarizes the characteristics, advantages, disadvantages, release mechanism of drug from ocular inserts, pharmacokinetic parameters and the compilation of the research work so far done in the field of development of ocular inserts....
The purpose of this study is to develop an optimized nanostructured lipid carriers (NLC) formulation for Ritonavir, and to estimate the potential of NLC as oral delivery system for poorly watersoluble drugs. Nanostructured lipid carrier (NLC) systems were developed using response surface methodology to optimize the concentrations surfactant and oil based on the size of the resulting NLC. From preliminary experiments, a formulation composed of Myristic acid, Capmul MCM EP, and Poloxamer 188 formed a stable NLC dispersion. Concentrations of the surfactant and Capmul MCM EP were optimized by a central composite design and response surface methodology. All the batches were prepared by emulsification-probe sonication method. The prepared NLCs were examined by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Scanning electron microscopy (SEM) and found to have an imperfect crystalline lattice and a spherical morphology. The Ritonavir-loaded NLCs had high release rates and Entrapment efficiency of the drug compared to plain drug....
Novel drug delivery systems (NDDS) constitute the mainstay of pharmaceutical research and development. A significant milestone in oral NDDS is the development of the osmotic drug delivery system, an innovative and highly versatile drug delivery system. Osmotic drug delivery systems utilize the principle of osmotic pressure, as an energy source, for the delivery of drugs. Oral osmotic drug delivery systems with their versatility and their highly predictable drug release rates offer various biomedical advantages. Osmosis is an aristocratic phenomenon that seizes the attention for its exploitation in zero-order drug delivery systems. The drug delivered from these systems is independent of pH and the physiological conditions. Optimizing semi permeable membrane and the osmotic agents can modulate drug release from the system. In this article, a detailed description of various oral osmotically driven systems along with their formulation aspects, therapeutic applications and evaluation techniques are described....
Liquid crystals are phase of matter having properties between those of a liquid and a solid. They are mainly divided into thermotropic, lyotropic and metallotropic liquid crystal. In this review, characterization technique, their properties and its various applications in pharmaceutics as Sustained release, transdermal patch, dermatological preparation like ointment, gel, optical lenses, dental care, microcapsule, polymer science, and gene therapy is discussed....
Different types of lipid based vesicular systems have been developed now a days for several applications inside the controlled and targeted drug delivery. Pharmacosomes bearing unique advantages over liposomes along with niosomes have been emerged as potential alternative to conventional vesicles. These are the amphiphilic phospholipid complexes of drugs which having active hydrogen that bind to phospholipids. They provide an efficient method for delivery of drug directly to the site of infection as well as reduction of drug toxicity with no adverse effects along with low cost of therapy. They help for better biopharmaceutical properties to the drug, resulting in improved bioavailability, especially in case of poorly soluble drugs. Pharmacosomes have been produced for several applications like non-steroidal anti-inflammatory drugs, proteins, cardiovascular and antineoplastic drugs....
Phonophoresis or sonophoresis is consists of use of ultrasonic energy for enhancement of drugs through the transdermal or topical route. Some 40 years ago, the combination of ultrasound and steroids or analgesics has been utilized by physiotherapist to treat a several range of muscular and arthritic conditions. But this method involves several subjective and non-quantitative basis including the common deficiencies of proper control along with incomplete accounts of dosimetry and regarding the protocols too. The non-calibrated ultrasound source is also vital deficiency of this method but fortunately several researches has also been done for improvement regarding these deficiencies. Hence, it shows some potential application in the field of drug delivery beneficial than the conventional techniques....
The nanoparticles have several potential biomedical application like they facilitate laboratory diagnostics or in the medical drug targeting along with as a contrast agent for magnetic resonance imaging (MRI) for tumor therapy or in the case of cardiovascular disease. The emerging advance in the nanoparticles for such application is the superparamagnetic nanoparticles consist of a core of iron oxides (SPION) which get targeted via external magnets. These nanopartilces usually coated with some of biocompatible materials and functionalized with drugs, proteins or plasmids....
Liquisolid tablets of furosemide were prepared by using new mathematical model design using cremophor RH 40, synperonic PE/L 81 and PEG 400 as liquid vehicle and avicel, aerosil as carrier and coating material, respectively. Furosemide liquisolid systems were evaluated for its identification of amorphous state within liquisolid system. Depending on flow property, 11 batches were selected for compression out of 45 liquisolid systems. Further for in-vitro dissolution profile directly compressed tablet was compared with that from liquisolid tablets. These studies showed that DR value decreases with increase in drug concentration in cremophor or synperonic upto a minimum plateau dissolution rate and there is a linear relationship between fraction of molecularly dispersed drug in liquid vehicle and DR. Furosemide had better dissolution profile in cremophor than synperonic and PEG 400. Batch LS 34 having the highest dissolution rate of furosemide....
The present study was aimed for solubility enhancement of candesartan (CND) by dendrimers. The aqueous solubility of CND was measured in the presence of dendrimers in distilled water. The effect of variables (pH condition, concentration of dendrimer, temperature) has been studied via implementation of Box-Behken design of experiment. The order in which the dendrimers increased the solubility at a constant pH condition was G3 > G0. Results revealed that the solubility of CND in the dendrimer solutions was proportional to dendrimer concentration. The influence of dendrimer solution pH on the solubility enhancement of CND suggests that it involves an electrostatic interaction between the carboxyl group of the CND molecule and the amine groups of the dendrimer molecule. The solubility of CND was inversely proportional to the temperature under which the experiment was performed. Polyamidoamine (PAMAM) dendrimers have the potential to significantly enhance the solubility of poor water soluble drugs, CND....
The purpose of writing this review on Stomach specific dosage forms for technological attempts have been made in the research and development of rate-controlled oral drug delivery systems to overcome physiological adversities, including the physiological and formulation variables affecting gastric retention and unpredictable gastric emptying times (GET). It is known that differences in gastric physiology, such as, gastric pH, and motility exhibit both intra-as well as inter-subject variability demonstrating significant impact on gastric retention time and drug delivery behaviour. We have reviewed various gastroretentive approaches designed and developed until now, i.e. high density, floating, bio-or mucoadhesive, expandable, unfoldable, super porous hydrogel and magnetic systems, classification and formulation aspects are covered in detail....
Loading....