Current Issue : April-June Volume : 2013 Issue Number : 2 Articles : 22 Articles
Multiparticulate dosage forms are receiving a great deal of attention as alternative system for oral drug delivery. The present review outlines the theory behind the pellet formation, its growth mechanism, its purposes and advantages. The techniques namely extrusion-spheronization, the most widely used pelletization technique in the pharmaceutical industry as it is a robust, simple, fast processing and reproducible pellet production process, have been described along with parameters affecting pelletization. Extrusion spheronization is widely utilized in formulation of immediate release, sustained release and controlled release delivery systems. Evaluation of the pellets is discussed with reference to the size distribution, shape, surface morphology, specific surface area, friability, tensile strength, density, porosity, disintegration time and in vitro dissolution studies of pellets. This review focuses on the extrusion-spheronization techniques of pelletization with its merits, process mechanisms, process variables and pellets characterization, as a tool in the multiparticulate drug delivery system....
A design for controlled release drug delivery system can be used for solving problems of targeting of drug to a specific organ or tissue and controlling the rate of drug delivery to the target site. This technique used for prevention of protein degradation by the encapsulation method and it provide the protection, taste masking, alteration in absorption site and prolong the drug release. Many different active materials like drugs, flavor, enzyme, vitamins, pesticides and catalyst have been successfully encapsulated inside microcapsules made from variety of polymeric and non-polymeric materials. The aim of this article is to present a concise review on the applications of microencapsulation in the pharmaceutical field, general over view and method of preparation of microencapsulation....
Floating matrix tablets are designed to prolong the gastric residence time after oral administration, at a particular site and controlling the release of drug especially useful for achieving controlled plasma level as well as improving bioavailability. With this objective, floating dosage form containing glipizide as drug was designed for the management of type-II diabetes. Tablets were prepared by using release rate controlling and gel forming polymers such as hydroxypropyl methyl cellulose (HPMC K4M, HPMC K15M, HPMC K100M) in single by direct compression method. The study shows that tablet composition and mechanical strength have great influence on the floating properties and drug release. Incorporation of gas-generating agent like sodium bicarbonate together with polymer improved drug release, besides optimal floating (floating lag time <35 s; total floating time up to 12 h). Tablets were evaluated for their physical characteristics, viz., hardness, friability, and mass variation, drug content, swelling index and floating properties. Further, tablets were studied for in vitro drug release characteristics for 12 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Based on evaluating parameters, Formulation prepared by using 40% HPMC K4M and 20% sodium bicarbonate was selected as optimized formulation. Finally, Kinetic modeling correlation with zero order, first order and Higuchi equations was confirmed as the drug release mechanism from optimized formulation, indicating that water diffusion and polymer rearrangement played an essential role in drug release. Stability studies were carried out at 30OC/65% RH and 40OC/75% RH for optimized formulation for 2 months. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, floating properties, and drug content of the tablets....
Cyclodextrin nanosponges are novel highly cross-linked cyclodextrin nanoporous polymer. These are prepared by reacting cyclodextrin (CD) with several cross linking agents such as carbamate (Isocyanates), carbonate (carbonyl diimidazole, Diphenyl carbonate), ester (Maleic anhydride, Pyromellitic dianhydride) and polyamidoamine compounds. They are spherical, crystalline or paracrystalline, porous, nontoxic, nonhemolytic and stable solid nanoparticles. They can be used as carriers for lipophilic and hydrophilic drugs. They can also decrease side effects and protect drugs from degradation....
The aim and objective of the present investigation describes the development and evaluation of chitosan based Interpenetrating polymeric network of hydrogel beads for modified release of simvastatin. A Box benhken design was employed to design Interpenetrating polymeric network of hydrogel beads of simvastatin by precipitation technique. Simvastatin has less solubility in water hence effort is to increase the solubility by forming an inclusion complex (1:1) with beta-cyclodextrin and then incorporate in to polymer bland. This effort also protects the drug from solvent and crosslinker effect during preparation. The effect of critical formulation variables namely amount of polymers, concentration of glutaraldehyde, and time of crosslinking on % drug entrapment, beads diameter, swelling and in vitro % drug release was investigated using response surface methodology. The response parameters were statistically analyzed. The parameters were evaluated using the F test and mathematical models were generated for each response parameter using multiple linear regression analysis (MLRA) and analysis of variance (ANOVA). The three main factors studied had a significant effect (P < 0.05) on response variables. The optimized formulation showed 91.12 cumulative percentage releases in duration of 12 h following zero order kinetics. The % drug entrapment, area increased after swelling study and beads diameter were found to be 78.51%, 35.0 mm2and 1.22 mm2 respectively. The mechanism of drug release was characterized by Higuchi diffusion model. The experimental values of the response parameters were in agreement with those predicted by the mathematical models confirming the prognostic ability of MLRA and ANOVA. Optimized formulation further process for various instrumental study such as scanning electron microscopy (SEM) and trinocular optical microscopy to study surface morphology of beads. Fourier transform infrared spectroscopy (FTIR) study and differential scanning calorimeter (DSC) are used to confirms the crosslinking, stability of drug in the formulation, to confirm the formation of inclusion complex, characterization of drug and polymers as well as drug- excipients compatibility. Stability study on optimized formulation also performed as per ICH guideline for 6 week.It is concluded from results data that the prepared formulation fulfil the aim of the work....
Diclofenac sodium (DFN), a non steroidal anti-inflammatory drug (NSAIDS) was formulated as microspheres using Sodium Alginate (SA) as a polymer by employing ionotropic gelation technique. The prepared microspheres were made subjected for various evaluation parameters and in vitro characterization at 0.1 M HCL (pH 1.2) which is followed in 6.8 pH phosphate buffer. The particle size of microspheres was measured by using optical microscope. The prepared DFN-microsphere proves a better spherical geometry. The formulation D4 shows a better release profile in increased Sodium Alginate concentration and may also proves a better choice for site specific delivery of drug....
The present work is focus to develop and characterize an oral sustained release matrix tablet of Nicardipine Hydrochloride by employing hydrophilic and hydrophilic polymers. Due to poor water solubility of the drug its bioavailability is dissolution rate limited. The purpose of the study was to increase the solubility of Nicardipine Hydrochloride by solvent evaporation technique. Complexes of different molar ratio were prepared. Matrix tablets were prepared by direct compression technique using different concentration of polymers and selected complex. The blended powders and tablets were evaluated for various physico-chemical parameters as per official protocol. The In Vitro dissolution study was carried out in acidic medium (pH 1.2) for 2 h, followed by phosphate buffer dissolution medium (pH 6.8) for next 10 h. The blended powders showed satisfactory flow properties and compressibility. The In Vitro release pattern indicated that formulation F7 releases the drug for period of 12 h and was best fitted to Higuchi release profile. The present study has demonstrated that combination of hydrophobic and hydrophilic polymers effectively sustained the drug release for prolonged period of time12 h....
5-Fluorouracil (5-FU) has been the most widely used drug for the chemotherapy of gastrointestinal cancer for many decades. The present investigation concerns the development and evaluation of single unit floating tablets of 5-FU which, after oral administration, are designed to prolong the gastric residence time, increase drug bioavailability and target the stomach cancer. A floating drug delivery system (FDDS) was developed using gas-forming agents, like sodium bicarbonate, citric acid and hydrocolloids, like hydroxypropyl methylcellulose (HPMC) and Carbopol 934P. The prepared tablets were evaluated in terms of their physical characteristics, in vitro release, buoyancy, buoyancy lag-time and swelling index. The formulations were optimized for the type of filler, like lactose, microcrystalline cellulose (MCC) and dicalcium phosphate (DCP) as well; different viscosity grades of HPMC and concentrations. The results of the in vitro release studies showed that the optimized formulation could sustain drug release for 24 h and remain buoyant for 16 h. When these dissolution profiles were subjected to various kinetic release investigations and it was found that the mechanism of drug release was predominantly diffusion with a minor contribution from polymeric relaxation....
The aim of the present study was to formulate an Ibuprofen loaded microemulsion based gel (MBG) for the topical delivery. The oil phase selected for the preparation of stable microemulsion was IsoPropyl Myristate (IPM). Tween-80 and PEG 400 were selected as surfactant and co-surfactant respectively. For the ease of application microemulsion was gelled by using carbopol 940. The optimized MBG was evaluated for pH measurements, spreadability, swelling index study, drug content and in-vitro permeation study. The in-vitro skin permeation was carried out in pH 7.4 phosphate buffer on excised mice skin using franz-diffusion cell for 4 h and was compared with a conventional gel formulation. The results showed that release of drug from MBG was found to be 97.78% as compared to 79% from conventional gel formulation. The study also showed flux value 0.453µg/cm2/min for MBG as compared to 0.353 µg/cm2/min which was found in the case of conventional gel. Hence MBG is the promosing alternative for the topical delivery of the drug....
Metoprolol tartrate is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially for hypertension. Transdermal patches of Metaprolol tartarate were prepared by using different polymers such as Eudragit L100, Eudragit RL100, polyethylene glycol with different ratios. Solvent casting method was employed for the preparation of transdermal patches. The prepared patches were evaluated for flexibility, thickness, weight variation, moisture content, hardness and for tensile strength. The drug release studies were carried out using Franz diffusion cell with dialysis membrane as the diffusion medium. The prepared trandermal patches were further characterized by Fourier transform infrared spectroscopy, Differential scanning colourimetry and Scanning electron microscopic analysis. The drug release from the formulations with 1% eutragit L100, 1% eutragit RL100 was extended up to 24 hrs. The results of stability studies indicated that all patches were stable after storing that accelerated conditions. Compatibility studies indicated that there are no interactions between drug and excipient used....
Valsartan was formulated as oral-controlled release matrix tablets using hydrophilic polymer such as hydroxypropyl methyl cellulose K15M (HPMC K15M) along with natural gum such as Copal gum. In this work a new attempt was made for in situ interactions between drug and polymers were devised to control the release of poorly water soluble drugs from oral hydrophilic monolithic systems. Polymers such as HPMC K15M and natural gum such as Copal gum were used at different concentrations in various formulations, while drug was maintained constantly in all the formulations. These polymers were used to monitor matrix swelling and gel properties. These findings indicated that the swelling and gel formation in the presence of ionizable species within the hydrophilic matrices provide an attractive alternative for controlled drug delivery from a simple monolithic system....
The Goal of the present investigation was to design and evaluate gels for topical delivery of water insoluble antifungal agent, Bifonazole with an aim to increase its penetration through skin. Bifonazole is a broad spectrum imidazole derivative useful in the treatment of superficial fungal infections. Purpose was to improve the solubility, inviter characteristics and dissolution properties of Bifonazole by the preparation of its solid dispersion with beta cyclodextrin using kneading method by using different drug carrier ratios. Prepared solid dispersion was evaluated for percent practical yield, drug content uniformity, in-vitro dissolution rate, DSC and IR studies. Faster dissolution was exhibited by solid dispersion containing l: l ratio of drug: β-cyclodextrin by kneading method. Gels have gained more importance because the gel-bases formulations are better percutaneously absorbed than creams and ointment bases. The gels were formulated by using Carbopol 940, HPMC, and Methyl cellulose and evaluated for pH, drug content, spreadability, extrudability, viscosity determination and diffusion study. In-vitro drug release of bifonazole solid dispersion incorporated gels was showed that Carbopol gels was showed higher drug release as compared to HPMC, methyl cellulose gels. Optimized gel was then undergone skin irritation test, stability studies, and inviter antifungal test. In conclusion, the optimized gel showed good physicochemical properties, better drug release, and reasonable stability....
In the present study, an attempt was made to formulate sustained release matrix tablets of Lornoxicam using Okra gum as release modifier. Five batches of sustained release matrix tablets of Lornoxicam were prepared by using different drug: polymer ratios. The tablets were analyzed for their hardness, friability, weight variation, and In-vitro release was performed in phosphate buffer saline (PBS) pH 7.4 for nine hours. Swelling study was also carried out to study dispensability of okra gum at different concentrations. The physical characters of the fabricated tablet were within acceptable limits. A better sustained drug release (98.7%) was obtained with the matrix tablet of the Okra gum. Results showed that the drug release from matrix tablets prepared by using natural polymers can be sustained for more than 9 hrs and the drug release vary with concentration of polymer in matrix tablets....
After oral administration, the drugs which are better absorbed from stomach suffer from mainly two difficulties: the short gastric retention time and unpredictable short gastric emptying time, which can reduce the bioavailability of administered drug. This drawback has led to the development of oral gastro-retentive dosage forms (GDFs). The gastroretentive dosage form is a type of sustained release dosage form from which the drug is released on continuous basis for a longer period of time as the formulation has enhanced gastric retention period and better bioavailability. Antidiabetic agents of different classes have been proven to be good candidates for the formulation of gastroretentive drug delivery system. The purpose of this paper is to review the literature of the work done on the GDFs of Antidiabetic drugs....
Moxifloxacin is a novel fourth generation fluoroquinolone antibacterial drug effective in the treatment of bacterial conjunctivitis. Ocuserts containing different combination of HPMC (E-50), EC and PVP (K-30). The ocuserts were prepared by solvent casting technique and characteristic like thickness, weight variation, drug content, moisture loss, moisture absorption, ocular irritation study, in vitro release sterility test and microbiological studies. All the ocuserts were found to be sterile, non irritant and stable. The drug content of the ocusert was found to be varied between 96.00 - 97.90 %. All the formulations followed zero order release pattern. Ocusert (MHF 4) containing EC (600 mg) and HPMC (400 mg) has shown good in vitro controlled release i.e. 77.13% was found to be better than the other formulations over an extended period of 8 hours and showed excellent microbiological activity for 3 days and remained stable and intact at ambient conditions....
Cancer is an uncontrolled growth of body cells. Skin cancer, the most common human malignancy, is classified into non-melanoma and melanoma skin cancers. In recent years, incidence of skin cancer is increasing throughout the world. The top most layer of the skin is epidermis that presents a principle barrier to topically applied medicines for the treatment of skin cancer. To overcome the limitations like poor penetration, low solubility and side effects associated with the use of cytotoxic agents, nanocarrier based approaches are gaining popularity in the pharmaceutical field. Liposomes and nanoparticles are representatives of their own classes of nanocarriers. Encapsulation of cytotoxic drugs within nanocarriers enhances the therapeutic index of the drug and improves the concentration to be delivered to the tumor site. Targeting principles can be applied on these nanocarriers by surface modification. In this comprehensive review, the recent advancements made in the development of nanocarrier-based chemotherapeutics for use in skin cancer therapy are discussed....
Now a days Nanotechnology is applied to diverse medical fields such as oncology, cardiovascular medicine and in treatment of other chronic diseases. It is multidisciplinary field deals with the development of the various formulation in the nanometer scale range. Nano refers to particles size range of 1-1000nm.Because of the Nanometer scale the physicochemical Properties of the various Nanoparticles are changed and it is important in the formulation of the Nanopharmaceuticals. In the present scenario Interest towards the Nanopharmaceuticals is increased due to the various Advantages. The present Overview on the Nanopharmaceuticals Represent Various Nanopharmaceuticals like Nanoemulsion, nanosuspension, nanogel,liposome,dendrimers etc.in which their method of preparation, evaluation test,Applications are described....
Herbal medicines are widely used all over the world due to their miraculous therapeutic effects and less side effects as compared to the modern medicines. Drug delivery systems based on lipid are an accepted, proven, commercially strategy to formulate pharmaceuticals, for topical, oral, pulmonary or parenteral delivery. The phospholipid molecular structure includes a water-soluble head and two fat-soluble tails, because of this dual solubility, the phospholipid acts as an effective emulsifier, which is also one of the chief components of the membranes in our cells. “Phytosome” is formed by complexing the polyphenolic phytoconstituents in molar ratio with phosphatidylcholine. Phytosomes are advanced forms of herbal products that are better absorbed, utilized, and as a result produce better drug delivery than conventional herbal extracts. This article reviews the recent advances and applications of various standardized herbal extract phytosomes as a tool of drug delivery....
Polysaccharidase producing microflora in the large intestine could facilitate the use of polysaccharides as the carriers for the drug delivery to the colon site to cure the local diseases of the colon. Bacterial enzyme degradable polysaccharides are now extensively used for the development of oral solid dosage forms for delivery of drug molecules to the colon as they having outstanding merits such as low toxicity and biodegradability, yet a high stability. Polysaccharides have been applied to the area as controlled release systems with external coatings, matrices formation, macromolecular and biodegradable carriers. Colon, the distal part of the intestine is hosted by a large variety of anaerobic gram negative microflora which secrete many enzymes e.g. amylase, pectinase, β-D-glucosidase, β-D-galactosidase, xylanase, dextranase etc. These enzymes play a vital role in the drug release mechanism of polysaccharide based systems. Polysaccharides can avoid degradation in the small intestine, but are a substrate of the colonic microbiota, e.g. amylose, chitosan, guar gum, xanthan gum, pectin, chondroitin sulphate, cyclodextrin, dextrans, inulin, locust bean gum, furcelleran, glucomannan, gellan gum, hyaluronic acid, karaya gum, scleroglucan, pullulan and xylan. The present review highlights the recent advancements made in the usage of polysaccharides in colon-specific drug delivery are discussed....
Now-a-days different newer approaches are introduced in the field of colon specific drug delivery system. This approaches having advantages for the treatment of colonic diseases like Ulcerative colitis, Crohn’s diseases, Inflammatory bowel diseases ,and also colon is selected as successful for site for oral administration of peptide and protein and can be protected from enzymatic degradation. Covalent linkage of drug with carrier is the newer approaches introduced now-a-days in which microbially triggered system is a novel approach of colon deals with specific enzyme activity of micro flora present in colon, like reducing and hydrolytic enzyme, and prodrug approaches deals with transformation of inactive derivative to the active drug at target site. So this article deals with different approaches used as microbially triggered system and its advantages and disadvantages....
The solid lipid nanoparticles (SLN) are sub-micron colloidal carriers ranging from 50 to 1000 nm, made up of physiological lipid dispersed in water or aqueous surfactant solution. Solid lipid nanoparticle is very important, excellent, novel drug delivery. In 1990 Scientist introduced solid lipid nanoparticles. The first patents have been granted in 1993 for method of producing solid lipid nanoaprticles.this paper review on various patents on solid lipid nanoparticles which show current research scale related to solid lipid nanoparticles....
In the past few decades, considerable attention has been made on the discovery and development of novel drug delivery system (NDDS). Different types of pharmaceutical carriers such as particulate, polymeric, macromolecular and cellular vesicles are discovered. Out of them, vesicles are ideal means of drug delivery that can enhance bioavailability of encapsulated drug by various mechanisms viz. controlled, sustained and targeted drug release, penetration enhancement so provide better therapeutic activity. Designing of the drug in the vesicular system has brought a new life to the old pre-existing drugs and thus has improved their therapeutic efficacies by controlling and sustaining the actions. This review mainly focuses on the various aspects related to the vesicular systems including their method of preparations, stability issues associated with them, their applications and drawbacks. A number of vesicular drug delivery systems like Liposomes, Niosomes, Transfersomes and Ethosomes have been developed. Every new system shows one or more advantages over the older vesicular systems. However they are still suffered with various stability issues aggregation, fusion, leaking, sedimentation of vesicles, difficulty in sterilization etc. This review also covers all aspects of provesicular carriers including their properties, applications and advantages over vesicular drug carrier systems. This review would be helpful for researchers working in the area of vesicular drug delivery and provesicular drug delivery systems....
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