Current Issue : October-December Volume : 2013 Issue Number : 4 Articles : 18 Articles
Transdermal patches are pharmaceutical dosage forms of varying sizes, containing, one or more active ingredient, intended to be applied to the unbroken skin in order to deliver in to systemic circulation through the skin barriers. Transdermal drug delivery system (TDDS) is a non-invasive route of drug administration and also it allows drug to release in sustain fashion as well as reduces the intensity of action and the side effects associated with its oral therapy. The patches had been proved effective because of its diverse advantages over other controlled drug delivery systems. This review article covers a brief outline on structure of skin, routes of penetration through the skin, various components required for formulation of transdermal patch, kinetics of drug release and permeation through skin, different approaches and advanced techniques for development of TDDS, various methods for development and evaluation of transdermal system....
From the past few years, there has been a considerable research in the area of drug delivery using particulate delivery systems as carriers for small and large molecules. Nanoparticles are one of the attractive research area for sustained release formulations because they are able to deliver drugs with the right dose at the appropriate time which increases patient compliance , reduces toxicity and have been used as a physical approach to alter and enhance the physicochemical properties of drugs. They have been used in vivo to protect the drug in the systemic circulation, with targeted delivery of drug and to deliver the drug at a controlled and sustained rate to the site of action. Various polymers are used for the formulation of nanoparticles to increase therapeutic benefit, with reduced side effects, the polymers are responsible for the sustained or controlled release of drug. Here, various aspects of nanoparticle preparation, characterization and their applications in delivery of drug molecules are reviewed....
Dendrimers are the polymers of 20th century having different and better functional properties than conventional linear polymers. Dendrimers are synthetic three dimensional strictly architectured polymers having some exclusive features like multiple surface functionality, highly branched structure, uniform size and molecular weight and having internal cavities for enclosing drug molecules. These distinguishing properties render them effective nano carrier for drug delivery in cancer tissues and for other targeted deliveries. In respective applications, dendrimers still need to be explored for their bio safety and toxicity study. Dendrimers are commercialized for diagnostic and gene transfecting agents. This review mainly focuses on basic structure, properties, types and potential applications of dendrimers in drug delivery....
The present study was aimed to develop a Chronotherapeutics based delayed total release tablet of Carvedilol with a lag time of 6 h. Full factorial 32 design (Minitab 16.0) used in this study provided valuable and efficient method to yield an optimized formulation. The independent variable used in this study includes concentration of SSG (% w/w) and percentage weight gain while drug release at 6 h was considered as response variable. A mathematical relationship, Y1= 73.77 + 1.56 X1 -7.5 X2 – 0.166 X1X1 + 3.83 X2X2 -2.1 X1X2 was obtained to explain the effect of all factors and their interactions on the dissolution of carvedilol at 6 h. From the in-vitro dissolution study it was observed that optimized batch displayed drug release of 88% in 6 h....
The objective of the present investigation was to formulate and evaluate a nail lacquer as Transungual drug delivery system for the treatment of onychomycosis. Nail lacquer is formulated with DMSO and thioglycolic acid as penetration enhancers. Nail lacquer was evaluated for its drying time and non volatile content. In vitro drug permeation studies were carried out across nitrocellulose membrane using Franz diffusion cells. The % of drug permeated at the end of 3h through the membrane was calculated....
Ondansetron HCl dihydrate is 5-HT3 receptor antagonist which is generally used for treatment of nausea and vomiting. This drug having low water solubility and low oral bioavailability (60%). Therefore, to provide this drug in a more accessible and patient compliant form and to overcome such problems, in the present study it was decided to formulation of rapid disintegrating tablet. On the basis of these considerations, in this study, effort has been made to formulate rapidly disintegrating tablet of Ondansetron hydrochloride using three superdisintegrants, Croscarmellose sodium, Crospovidone, SSG by using direct compression technology. Effect of different concentration of superdisintegrants on disintegration time of tablet and drug release was studied. The results concluded that poorly soluble drug Ondansetron hydrochloride dihydrate showing enhanced dissolution may lead to improved onset of action, bioavailability and patient compliance....
The purpose of this research was to formulate and systemically evaluate in-vitro performances of Floating Mucoadhesive Ramipril microspheres for its potential use in the treatment of hypertension, myocardial infarction. Ramipril Mucoadhesive microspheres were prepared by an emulsion-solvent evaporation technique containing HPMC K4M and chitosan as mucoadhesive polymer and ethyl cellulose and calcium carbonate as buoyancy increasing floating agent. Preformulation studies were carried out before formulation design. Total nine formulations were prepared. Microspheres were discrete, spherical, free-flowing and The prepared microspheres were subjected to evaluation for a good percentage of drug entrapment efficiency. particle size, in vitro buoyancy, in vitro mucoadhesion and in vitro drug release characteristics. An in-vitro wash off test showed that Ramipril mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could be retained in the gastrointestinal tract for an extended period of time. In-vitro dissolution test was carried out by using phosphate pH 2. All the formulations showed good dissolution profiles. Among all the formulation F5 showed good dissolution profile with 78.25% of drug release in 12 hours. In-vitro release kinetic data of Ramipril microspheres showed that the drug release mechanism was diffusion controlled as the plots of peppas model was linear. The results showed a sustained anti-hypertensive effect over a longer period of time in case of mucoadhesive microspheres, compared to the powder. In conclusion, the prolonged gastrointestinal residence time and slow release of Ramipril resulting from the Mucoadhesive microspheres could contribute to the provision of a sustained anti-hypertensive effect....
b-Cyclodextrin (b-CD) is widely used to increase the stability, solubility, and bioavailability of poorly soluble drugs because of the appropriate size of its cavity. Cefuroxime axetil is beta lactum antibiotic having poor water solubility. Here we report the complexation of cefuroxime axetil base with b-CD and the stability, dissolution, and pharmacokinetic properties of the cefuroxime axetil/CD complex. The formation of cefuroxime axetil/b-CD inclusion complexes is confirmed using differential scanning calorimetry, X-ray diffractometry. The thermal and photochemical stability of cefuroxime axetil is significantly improved by the complexation with b-CD, Our study suggests that cefuroxime axetil/b-CD complexation can be of great use to increase the stability and biological efficacy of cefuroxime axetil base....
The purpose of this research was to prepare a floating drug delivery system of cinnarizine in order to increase the gastric residence time for enhance solubility in gastric HCL because of cinnarizine have lower solubility in intestine. Cinnarizine floating tablet prepared by direct compression method using HPMC K4M as matrix formers, sodium bicarbonate as gas generating agent. The formulated tablets were evaluated for physical characteristics such as weight variation, hardness, friability, floating lag time and total floating time. The in vitro release of the tablets was evaluated in 0.1N HCl for 10hrs. The drug release kinetic was fitted in three different mathematical models like- Zero order, first order, Higuchi model. Amongst all the formulations, F2 and F3 were found to be better formulations and both contain same concentration of HPMC K4M (100 mg) with different concentrations of sodium bicarbonate (30 mg and 45 mg respectively). Formulation F2 and F3 showed 93.85% and 96.32% drug release at 10 hrs. Thus, it may be concluded that the cinnarizine floating tablet can be successfully formulated for improve absorption of cinnarizine with increase in the gastric residence time....
Floating drug delivery system is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastro intestinal tract (GIT) for local or systemic effects. This drug delivery system not only prolongs GI residence time but does so in an area of the GI tract that could maximize drug reaching its absorption site (intestine) in solution form and hence ready for absorption. Metformin hydrochloride, a BCS class III drug has absolute bioavailability of is 50–60% orally administered up to 2.5 g/day in three separate doses and the main site of its absorption is proximal small intestine and also has relatively short plasma elimination half life of 4 to 6.2. Gastric floating drug delivery matrix systems of metformin HCl are designed by direct compression using natural hydrophilic matrix forming polymer, almond gum and sodium bicarbonate as gas generating agent are employed. The powder blend in all the formulations showed good flow characteristics. Of various formulations F1 to F8 , formulation F8 containing 500 mg of Metformin HCl sustained drug release over a period of 10 hours with 96.62 % in 0.1 N HCl ( pH 1.2) and the results compared with the other hydrophilic matrix polymers which are existing polymers for sustained drug release formulations such as HPMC K 50 and Ethyl cellulose K4 included in sustained release formulations F6 and F7, studies conducted in phosphate buffer pH 6.8 and compared with drug release from formulation containing almond gum alone as a hydrophilic matrix polymer....
Acyclovir is a potent antiviral drug with low toxicity used in treatment of herpes simplex infection & varicella zoster infection. Acyclovir is used for its anti-viral effect for short term high dose therapy. It also requires frequent dose regimen. .It has maximum absorption in stomach and upper part of small intestine. Due to low gastric retention time, the bioavailability of drug is low as large portion of drug misses the absorption window. Acyclovir is a substrate for p-glycoprotein. Acyclovir has a high renal clearance value. It also contributes to eliminate the effect of Acyclovir rapidly. Oral route of drug administration is perhaps the most appealing route for the delivery of drugs. Of the various dosage forms administered orally, the table is most preferred dosage forms because of its ease of manufacturing, convenience in administration, accurate dosing, stability compared with oral liquids and because it is more tamperproof than capsule and suspension. It is great advantageous to both patient and clinician that medication to be formulated so that it may be administered in a minimum number of daily dosage form which can release the drug uniformly over desired period of time. The aim of the present study was to formulate and evaluate the novel tablet in tablet (Floating Delivery System) of Acyclovir using PEG 4000 as permeation enhancer by antagonizing effect on P-gp. In this the outer layer was of fast disintegrating PEG 4000 layer and Core tablet was of Sustained Release Floating Matrix Tablet of Acyclovir. After the formulation the tablets were evaluated for the Hardness, Friability, Thickness, Weight variation, Drug Release Profile, Stability and Compared with Marketed products and preclinical studies. Results and conclusions were noted down....
Oral administration is most popular route. About 40 to 50 % of novel chemical entities show poor bioavailability due to their low aqueous solubility. These drugs can be solublized to increase the bioavailability by using several methods as microemulsion, nanosuspension, liposome, solid lipid nanoparticles, self emulsifying drug delivery system (SEDDS), complexation with cyclodextrin etc. Self Micro-emulsifying Drug Delivery System (SMEDDS) is a novel approach to improve water solubility and ultimate bioavailability of drugs. SMEDDS is isotropic (one phase system) mixture of oil or modified oils, surfactants and co-surfactants, which are emulsified in aqueous media under conditions of gentle stirring and form the fine oil-in-water microemulsion, which presents the drug in solubilized form, and the small size of the formed droplet provides a large interfacial surface area for drug absorption. For lipophilic drugs, which display dissolution rate-limited absorption, SEDDS may be a promising strategy to improve the rate and extent of oral absorption....
There is considerable interest in the skin as a site of drug application both for local and systemic effect. Skin has always remained as the main part of drug delivery through last decades. There are many persons which you can see having patches attached to their body parts such as having it on the ear back for the vertigo like conditions, or alcohol dehydrogenase patch for alcohol de-addiction. This article deals with the how to enhance the delivery of drug through chemical and physical enhancers means how by they act, how they modify the structure of skin for transporting the drug through the skin and subsequently it will thus, it will help in the selection of suitable penetration enhancers for improving the permeation of poorly absorbed drugs via transdermal route....
The expenses for developing new drugs are exorbitant. Thus, in the present scenario, more emphasis is laid to develop newer drug delivery technologies, which would ensure better patient compliance, drug efficacy and extends the term of patents of the existing molecules. Colon specific drug delivery has gained a more importance for the delivery at colonic region by use of various drugs to treat the both local and systemic diseases. Local diseases include ulcerative colitis, crohn’s disease, irritable bowel syndrome, inflammatory bowel disease (IBD) and colorectal carcinomas. Other serious disorders which follow diurnal rhythm like nocturnal asthma, Hypertension, arthritis and angina can also be cured by this drug delivery system. A drug should be protected from the absorption and the upper GI environment to achieve the successful colonic drug delivery. This review mainly reveals on the various concepts and approaches include Prodrug, PH and time dependent systems and microbially triggered systems used in the development of colon specific drug delivery. This also focuses on the novel approaches namely Pressure controlled colonic delivery, osmotic controlled drug delivery and CODESTM. In-vitro and in-vivo evaluation parameters has been discussed here....
Nanoemulsions have pulled great aid in research, dosage form design and pharmacotherapy. This is as a result of a number of properties peculiar to nanoemulsions such as ease of preparation, optical clarity, thermodynamic stability and increasing surface area surface area. Another name of nanoemulsions is submicron emulsions which used in as vehicles for the delivery of active pharmaceutical ingredients. Conventional drug delivery systems comply with some of the disadvantages such as low bioavailability and noncompliance. So, to remove these disadvantages nanoemulsions are taken as novel drug delivery system. The main aim behind the development and design of nanocarrier emulsion systems are controlling and/or improving required bioavailability levels of therapeutic agents cannot be overemphasized. Reduction in the droplet sizes to the nanoscale results to some very interesting changes such as in physical properties, optical transparency and unusual elastic behaviour. This review mainly emphasis on the current status of nanoemulsions in the delivery of drugs. The morphology, formulation, characteristics and characterization of nanoemulsions were also addressed....
Large number of new chemical entities (NCE) present formulation and bioavailability problems because of the dose and poor solubility in solvent and co-solvent systems. There is an increasing interest to expand the range of targetable lipid based systems to solubilize a wide variety of drugs, to improve stability, ease of processing and manufacture in a sterile form. New class of parenteral lipid based drug delivery system includes tocol emulsions, solid lipid nanoparticles and nanosuspensions, sterically stabilized phospholipid micelles, lipid microbubbles and lipoprotein drug carriers. This review article covers the challenges faced by the formulation scientist at each stage of product development of lipid based drug delivery system....
The aim of this study was to formulate and evaluate sustained release pellets of highly soluble drug like Pregabalin by using matrix forming agent like Eudragit RS PO. The pellets were prepared by using Extrusion-Spheronization technique. Pregabalin is a BCS class 1 (highly soluble, highly permeable) drug, which makes it a good candidate, to be formulated in sustain release dosage form. The in-vitro dissolution study was carried out in 900 ml 0.1 N HCl pH-1.2 for 2 hrs and then in 900 ml phosphate buffer 6.8 pH for 24 hrs using USP apparatus type 1 (Basket Type). The release studies showed that the pellets prepared by using Eudragit RS PO were able to sustain the release of Pregabalin only for 5 hours. Thus pellets prepare with Eudragit RS PO was coated with different concentration of Eudragit RS 30D and Eudragit NM 30D and were able to sustain the release of drug for 24hrs. Among different combination concentration tried for coating, Eudragit RS 30D and Eudragit NM 30D (15%, 15%) showed desired release pattern and was able to sustain the release of Pregabalin for 24 hours. Selected formulation was subjected to kinetics studies and stability studies. The release kinetics studies shows that drug release follows Zero Order and Hixon Crowell Model while value of ‘n’ showed non-fickian diffusion mechanism. Stability studies indicate that the developed formulation were stable and retained pharmaceutical properties at room temperature and 40±2°C/75±5% RH for a period of 15 days....
Solid lipid nanoparticles were developed in early 1990s as an alternative to other traditional colloidal carriers like liposomes, polymeric nanoparticles and emulsions. Nanotechnology, as defined by the National Nanotechnology Initiative (NNI), is the study and use of structures roughly in the size range of 1 to 1000 nm. Solid lipid nanoparticles (SLN) are rapidly developing field of nanotechnology with several potential applications in drug delivery and research. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could use for drug targeting. Hence solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery. The overall goal of nanotechnology is the same as that of medicine: to diagnose as accurately and early as possible and to treat as effectively as possible without any side effects using controlled and targeted drug delivery approach. the bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood....
Loading....