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The prime goal of drug delivery through drug carrier system to the specific target site at the suitable concentration for therapeutic action. Recently thin films are acquiring attention as drug carrier and various scientists are working on the formulation and development of thin films as a novel drug delivery system. Because of its capacity to safely load medications and release them in a regulated manner, thin films have attracted increasing interest in the field of drug delivery, which improves drug efficacy. They are more patient compliance and alternative to oral drug delivery employing self-application, prolonged action and easily terminate if drug toxicity is produced. Oral, buccal, sublingual, ocular, and transdermal routes have all been employed to deliver this delivery mechanism for both systemic and local effects. The development of thin films comprises of various methods with keeping in mind the anatomical and physiological constraints, physicochemical properties and types of drug substance and use of various polymers (matrix, hydrophilic and hydrophobic) as well as the characterisation methods with recent trends.

Background The overall objective was to prepare a highly accurate nanocarrier system of mesalamine for the treatment of ulcerative colitis with increased therapeutic efficacy and targeting. In the formulation of nanocarrier systems, optimization is a critical process for understanding nanoformulation variables and quality aspects. The goal of the present work was to determine the effect of independent variables, i.e., the concentrations of chitosan, carboxymethyl inulin (CMI), and the drug on the response variables, i.e., particle size and percent entrapment efficiency of the mesalamine-loaded nanoparticle using the Box Behnken design (BBD). The correlation between the independent and dependent variables was investigated using the Design Expert generated mathematical equations, contour, and response surface designs. Result An optimized batch was developed using the ionotropic gel method with selected independent variables (A: + 1 level, B: 0 level, C: − 1 level) and the developed nanoparticles had a particle size of 184.18 nm, zeta potential 26.54 mV, and entrapment efficiency 88.58%. The observed responses were remarkably similar to the predicted values. The morphological studies revealed that the formulated nanoparticles were spherical, and the results of the FTIR and DSC studies indicated the drug-polymer compatibility. The nanoparticle showed less than 5% release in the pH 1.2. In the colonic region (pH 7.4), more than 80 % of the medication was released after 24 h. The kinetics study showed that the Higuchi and Korsemeyer-Peppas models had R2 values of 0.9426 and 0.9784 respectively, for the developed formulation indicating linearity, as revealed by the plots. This result justified the sustained release behavior of the formulation. Conclusion The mesalamine-loaded chitosan-CMI nanoparticle has been successfully developed using the ionotropic gelation method. The nanoparticles developed in this study were proposed to deliver the drug to its desired site. The developed nanoparticles were likely to have a small particle size with positive zeta potential and high percent drug entrapment. It could be stated from the results that BBD can be an active way for optimizing the formulation and that nanoparticles can be a potential carrier for delivering therapeutics to the colon.

Background Present investigation for research was to develop matrix-type transdermal drug delivery system of flurbiprofen (FBP) with the various ratio of matrix polymers (hydrophilic and hydrophobic), the concentration of plasticizer and natural penetration enhancer by Box–Behnken statistical design to investigate the combined outcome of selected independent variables for effective management of rheumatoid arthritis. The influence of a binary mixture of polymers, plasticizer and penetration enhancer on physicochemical considerations including thickness, tensile strength, percent elongation, weight variation, percent moisture content, percent moisture uptake, water vapour transmission rate, folding endurance, drug content, in vitro drug dissolution study and then ex vivo drug permeation study was evaluated. Results The study demonstrated that the tensile strength of films improved by matrix polymer ratio and to a slighter gradation in the rise of plasticizer and natural penetration enhancer. Ex vivo drug permeation study was accompanied via excised porcine skin as a permeation barrier in Franz diffusion cell. Ex vivo drug permeation study indicated that matrix polymer ratio (HPMC K15M:ERL100) at 3:1 and natural penetration enhancer (d-limonene) at highest concentration 7.5% w/w containing formulation FBPT7 delivered maximum flux and supplementary improved the permeation of drug. The result of the skin irritation test revealed that the developed formulation is free from any type of skin irritation effects like erythema and oedema. Conclusion Based on the findings of this research, it can be established that a well-controlled release and very effective skin penetration of the drug was accomplished by the film FBPT7 in the existence of permeation enhancers for prolonged periods.

The present review is focused on the prebiotic impact of inulin on the management of the gastrointestinal disorder. Prebiotics can be described as "non-digestible food ingredient stimulating the growth of a certain number of bacteria in the colon, which can improve the host health". In 2004 this definition was modernized to include other areas that may benefit from selective targeting of particular microorganisms: "selectively fermented ingredients that alter the configuration and activity in the gastrointestinal microbiota that confer positive effect". The positive impact of prebiotics in experimental colitis and human inflammatory bowel disease (IBD) has already been established. Prebiotics shows a positive effect in the prevention of IBD by modulating the trophic functions of the flora. Inulin enhances the growth of indigenous lactobacilli and/or bifidobacteria by inducing colonic production of short chain fatty acids (SCFA's) and these properties are related to decreased mucosal lesion scores and diminished mucosal inflammation. Inulin shows a positive approach to retain microbial populations and to support epithelial barrier function by their prebiotic effect which helps in the host defense against invasion and pathogens translocation (endogenous and/or exogenous) and in the inhibition of gastrointestinal diseases and this impact should be verified in further clinical studies. In the present review, we discussed the positive effect of prebiotics in rat IBD models and in human subjects along with their potential protective mechanisms. Preclinical and clinical data revealed that the gut mucosal barrier would be improved by the use of prebiotics in IBD.

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release.

The delivery of a drug to the preferred site of action is referred to as drug targeting. The benefits of drug targeting are a reproducible and controlled release rate of the therapeutic compound, which forestalls overdose. Due to the potential to treat colonic diseases with minimum side effects, colon targeting has become of high interest over the last decades. Inulin was investigated for its potential as encapsulation material regarding its enzymatic degradability and its drug release behaviour. Inulin is a polysaccharide with a widespread range of therapeutic uses such as a carrier in a drug delivery vehicle, as a diagnostic/analytical tool or as a dietary fibre with additional health benefits. In the main, much research has focused on inulin as a drug delivery carrier for colon-specific drug delivery. The justification for this is its potential to survive in the stomach’s acidic environment. This unique stability and strength are utilized in many ways to deliver drugs safely to the colon, where they can be easily absorbed through the gut epithelium into the blood. There are also some proofs that inulin’s prebiotic features also lead to health benefits, mainly for patients with inflammatory bowel disease or in the prevention of colonic cancer. Inulin based hydrodynamic research will be useful to discover the potential of inulin.

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes.

The present study aimed to improve the aqueous solubility of the oral hypoglycemic agent, glibenclamide (GLI), so as to improve its oral absorption, and hence bioavailability after oral administration. This was accomplished by complex formation between GLI and ?-cyclodextrin (?-CD). The study involves the preparation of the inclusion complexes using different techniques. Differential Scanning Calorimetry (DSC) and XRay Diffractometry (XRD) results confirmed the complex formation between GLI and ?-CD. The solubility increase of GLI was due to 1:1 complex formation. The dissolution rate of GLI from the complex prepared by neutralization method was more rapid as compared to other methods used. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21855 Dhaka Univ. J. Pharm. Sci. 13(1): 15-21, 2014 (June)

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72%-82.27%, drug loading from 20.28%-33.26%. The size of the prepared microspheres ranged between 61.22-90.41µm which was found to increase with increase in polymer concentration. All values are statistically significant as p

Cosmetic acceptability and primary skin irritation are the two main parameters for assessing the suitability of any topical formulation meant for protection against the painful bites of mosquitoes. In the present study four newer analogs of N,N-diethyl-2-phenylacetamide (DEPA), were synthesized and formulated for topical application as insect repellent. They were assessed for their irritant behavior on rabbit’s skin for erythema and edema. The topical formulations of the analogs were also assessed for their protection time at varying concentrations against Aedes aegypti mosquitoes.

Solid lipid nanoparticles (SLN) have emerged as a next-generation drug delivery system with potential applications in pharmaceutical field, cosmetics, research, clinical medicine and other allied sciences. Recently, increasing attention has been focused on these SLN as colloidal drug carriers for incorporating hydrophilic or lipophilic drugs. Proteins and antigens intended for therapeutic purposes may be incorporated or adsorbed onto SLN, and further administered by parenteral routes or be alternative routes such as oral, nasal and pulmonary. The obstacles associated with conventional chemotherapy may be partially overcome by encapsulating them as SLN. The present review focuses on the utility of SLN in terms of their advantages, production methodology, characterization and applications. If properly investigated, SLNs may open new vistas in therapy of complex diseases.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12065 International Current Pharmaceutical Journal 2012, 1(11): 384-393

The ethanolic extracts of leaves of Morinda pubescens Linn . were explored for their phytochemical constituents and antimicrobial activity. The preliminary evaluation of ethanolic extract exhibited appreciable antimicrobial activity on the tested pathogenic bacterial isolates at a concentration of 100mg/g and displayed inhibitory potency (20-22mm) in diameter on the tested bacterial isolates. Phenol and alkaloids was found to be present in the plant parts while highest phenolic constituent was recorded in the leaves extract .

Purpose: To prepare and evaluate metformin microspheres for prolonged release. Methods: Metformin microspheres were prepared by non-aqueous solvent evaporation method using various polymers, including ethylcellulose (EC), hydroxypropyl methylcellulose (HPMC), carbopol 934P (CA) and chitosan (CH). The effect of process variables, viz, drug/polymer ratio, stirring rate and type of polymer on the mean particle size, drug entrapment efficiency, yield, drug content, micromeritic properties and drug release of the microspheres were studied. Results: It was observed that as the stirring speed increased from 600 to 1800 rpm, microsphere size decreased and hence drug release rate increased. Drug release rate at 1:2 drug: polymer for microspheres produced at a stirring rate of 1200 rpm was in the following order: carbopol 934P > HPMC > ethyl cellulose > chitosan. The formulations containing carbopol 934P (CA3) and HPMC (HPMC3) released drug faster than chitosan microspheres (CH3). Conclusion: Amongst the developed microspheres, CH3 formulation (with chitosan as the polymer) exhibited maximum prolonged drug release at gastrointestinal pH or at least 15 h. This oral sustained metformin formulation could potentially improve the bioavailability of the drug as well as patient compliance. Keywords: Metformin, Microspheres, Prolonged release, Solvent evaporation, Ethylcellulose, Hydroxypropyl methylcellulose, Chitosan

In the present study, an attempt was made to formulate mucoadhesive buccal patches of flurbiprofen (FBN) in order to enhance solubility. Solubity enhancement was attempted by making solid dispersion of drug with beta-CD (cyclodextrin). Initially preformulation were carried out using reported methods. Buccal patches were prepared by solvent casting technique using polymers like polyvinyl alcohol (PVA), sodium carboxymethyl cellulose (SCMC), and hydroxypropyl methylcellulose (HPMC). The prepared patches were evaluated for their weight variation, thickness, folding endurance, surface pH, swelling index, in vitro residence time, in vitro permeation studies, drug content uniformity and bioadhesion test.

Metronidazole microcapsules with a coat consisting of alginate and the natural cationic polymer, chitosan were formulated by using tripolyphosphate cross-linking method and were investigated with a view to develop mucoadhesive microcapsules. The microcapsules were evaluated for their surface morphology, microencapsulation efficiency, in-vitro wash-off test, swelling behavior and in-vitro drug release. The microcapsules formed had rough surface morphology in scanning electron microscopy. The drug entrapment efficiency was found to be in the range 75.2±1.31% and 82.1±0.75%. Chitosan microcapsules displayed a limited amount of swelling which is supposed to be related to the degree of cross-linking with tripolyphosphate. The microcapsules showed better mucoadhesive property at intestinal pH 7.4 than at gastric pH 1.2 in the in-vitro wash-off test. The drug release was found to be slow and extended over long duration of time. Key words: Metronidazole microcapsules; chitosan; mucoadhesion; tripolyphosphate DOI: http://dx.doi.org/10.3329/dujps.v9i2.7897 Dhaka Univ. J. Pharm. Sci. 9(2): 125-130, 2010 (December)