Introduction: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water. Materials and Methods: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats. Results: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets. Conclusions: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.

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Background : Glibenclamide is an oral hypoglycemic drug completely metabolized in the liver, the principal metabolite being very weakly active, buccal delivery may be useful for the treatment of diabetes more effectively. The aim of the present study was to design formulations and systematically evaluate in vitro and ex vivo performances of buccal films of glibenclamide so that the required therapeutic plasma concentrations can possibly be achieved more rapidly using the different grades of hydroxypropyl methyl cellulose (HPMC) as the base matrix. Materials and Methods: Mucoadhesive buccal films of glibenclamide were prepared by solvent casting technique using different grades of HPMC with different ratios. Prepared films were evaluated for weight, thickness, surface pH, swelling index (SI), folding endurance, drug content uniformity, in vitro release, and ex vivo permeation studies. Results: The film thickness and weight were in the range of 0.213-0.4892mm and 22.25-39.83 mg, respectively. The films exhibited controlled release over more than 6 h. HPMC, HPMCK100, and HPMC3000 films exhibited satisfactory swelling. Surface pH of buccal films was found to be 6.4-6.8. SI observed to be highest for GF12 (275.3 ± 12.17) and lowest for GF1 (173.5 ± 5.65). The films exhibited controlled release over more than 6 h. HPMC exhibited satisfactory swelling, an optimum residence time, and promising drug release. The Higuchi plots were found to be linear with correlation coefficient values of 0.8933, 0.9138, and 0.9947 for GF4, GF8, and GF9, respectively. Conclusions: Among all the formulations, GF9 shows good controlled release results correlated with ex vivo permeation studies.

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Background: Efavirenz is the preferred nonnucleotide reverse transcriptase inhibitor for first-line antiretroviral treatment in many countries. It is orally active and is specific for human immunodeficiency virus type 1. Its effectiveness can be attributed to its long half-life, which is 52-76 h after multiple doses. The drug is having poor water solubility. The formulation of poorly soluble drug for oral delivery will be one of the biggest challenges for formulation scientists in the research field. Among the available approaches, the solid dispersion technique has often proved to be the most commonly used method in improving dissolution and bioavailability of the drugs because of its simplicity and economy in preparation and evaluation. Materials and Methods: Solid dispersions were prepared by solvent evaporation and physical mixture methods by using polyethylene glycol as the hydrophilic carrier and PEGylated product was also prepared. The prepared products were evaluated for various parameters, such as polymer interaction, saturation solubility study, and drug release studies. The drug release data were analyzed by fitting it into various kinetic models. Results: There is an improvement in the dissolution from 16% to 70% with solid dispersion technology. Higuchi model was found to be the best fit model. Conclusion: Solid dispersion is the simple, efficient, and economic method to improve the dissolution of the poorly water-soluble drugs.

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Background: The main aim of this study was to develop a gastroretentive, multiple-unit floating drug delivery system for a drug which is poorly absorbed from the lower gastrointestinal tract. Such a dosage form may provide an extended retention of drug in the upper gastrointestinal tract resulting in enhanced absorption and improved bioavailability. Materials and Methods: Microspheres were prepared by the emulsion solvent diffusion method. Four different ratios (1:1, 1:2, 1:3, and 1:4) from each polymer, i.e., Eudragit RL 100 (E1-E4) and cellulose acetate (C1-C4) were prepared. Results: Hollow microspheres were characterized by particle size using optical microscopy. The in vitro release data obtained for the formulations E1-E4 and C1-C4 showed good entrapment efficiency, good percentage buoyancy, and prolonged drug release. The in vitro drug release showed the highest regression coefficient values for Higuchi's model, indicating diffusion to be the predominant mechanism of drug release. The surface and cross-sectional morphology of the formulations E1-A and C1-A were determined using scanning electron microscopy. Conclusions: Thus, prepared floating hollow microspheres of famotidine may prove to be potential candidates for the multiple-unit drug delivery device adaptable for any intragastric condition.

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Background: This project aims to formulate and characterize a drug-eluting contact lens to provide controlled release of drug for a longer period of time, using liposomes as drug delivery system. Materials and Methods: Drug delivering contact lenses were created by coating disposable soft contact lenses with ciprofloxacin entrapped in the liposomes. Reverse phase evaporation and lipid film hydration methods were used for the preparation of ciprofloxacin trapping reverse phase evaporation vesicles, that is, unilamellar vesicles (REVs) and multilamellar vesicles (MLVs), respectively. Soya lecithin and cholesterol (CH) were used in the molar ratios of 7:4 and 7:2. The spherical structure of the liposomes, the mean diameter, and their purity were determined by photomicroscopic, transmission electron microscope, and chromatographic analysis, respectively. The prepared liposomes were evaluated for their entrapment efficiency, in vitro drug release, stability, and toxicity. Results: MLVs were larger than REVs with their mean diameter 338.32 nm and also entrapped greater amount of ciprofloxacin. Drug loading and its release from the liposomal vesicles was dependent on CH content. Ciprofloxacin released from the liposomes coated on the contact lenses not only inhibited both Staphylococcus aureus and Pseudomonas aeruginosa on an agar plate but also showed an enhanced antibacterial effect as determined by minimal inhibitory concentrations. Approximately 40% of ciprofloxacin was retained up to a period of 3 months at 4΀C. Furthermore, the formulation was found to be nontoxic and also a reduction in toxicity of ciprofloxacin was observed after entrapment when assessed by lymphocyte toxicity assay and chick embryo inoculation. Conclusions: An innovative drug delivery system consisting of drug-loaded liposomes coated onto the surface of contact lenses has been developed. This system is highly specific in terms of localized and sustained application of the drug.

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Introduction: For the real-time clinical utilization of curcumin (an ayurvedic natural product) to treat breast cancer, its dissolution, rate limited solubility, poor tissue absorption, and extensive in vivo metabolism that leads to its poor systemic bioavailability should be overcome. A polymer-based nanoparticle formulation using bovine serum albumin can increase its aqueous solubility and can achieve protected, sustained, and targeted therapy in breast cancer. Materials and Methods: Desolvation technique was optimized for the preparation of albumin nanoparticles. Particle size, drug release, encapsulation efficiency, drug polymer interaction were the in vitro properties that were determined. Cell culture studies, in vivo pharmacokinetics in rats were used for biological characterization of the formulation. Results: The formulations were successfully prepared using 1:1, 1:2, 1:3, 1:4 drug: polymer ratios and the percent entrapment was found to be 74.76%, 91.01%, 85.36%, 86.42%, respectively, and particle size determined by zetasizer was found to be 225.1, 223.5, 226.3, 228.7 nm, respectively, and in vitro release was sustained for at least one month with drug release of 75.74%, 65.97%, 64.42%, 54%, respectively. The dissolution rate and aqueous solubility of curcumin was enhanced with this formulation. Fourier transform infrared spectroscopy (FTIR) studies demonstrated that the drug was not changed in the formulation during the fabrication process. The proliferation assays in MDA-MB-231 tumor cell lines indicated more effectiveness of the formulation compared to its solution form. In rats, albumin nanoparticles sustained drug release, demonstrated more bioavailability, improved pharmacokinetic properties, and enhanced tissue targetability of the drug. Conclusions: An effective curcumin-albumin nanoparticle formulation was successfully developed using a desolvation technique.

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Background and Aim: Telmisartan (TEL) is an angiotensin II receptor blocker (ARB) antihypertensive agent. The aim of the present investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance the oral bioavailability of poorly water soluble TEL. Materials and Methods: The solubility of TEL in various oils was determined to identify the oil phase of a SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify the selected oil. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. A SNEDDS was further evaluated for its percentage transmittance, emulsification time, drug content, phase separation, dilution, droplet size, zeta potential, pH, refractive index, and viscosity. Results: The developed SNEDDS formulation contained TEL (20 mg), Tween^; 20 (43.33%w/w), Carbitol^; (21.67%w/w), and Acrysol^; EL 135 (32%w/w). The optimized formulation of the TEL-loaded SNEDDS exhibited a complete in vitro drug release in 15 min as compared with the plain drug, which had a limited dissolution rate. It was also compared with the pure drug suspension by oral administration in male Wister rats. The in vivo study exhibited a 7.5-fold increase in the oral bioavailability of TEL from the SNEDDS compared with the pure drug suspension. Conclusions: These results suggest the potential use of the SNEDDS to improve the dissolution and oral bioavailability of poorly water soluble TEL.

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Background: Tramadol hydrochloride (HCl) and ketorolac tromethamine are analgesic drugs, which are commonly used in combination in postoperative pain management. According to some studies, metoclopramide and magnesium sulfate (MgSO ₄ ) as adjuvant agents can improve analgesia and decrease the need for other pain drugs. Materials and Methods: The chemical stability of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl has been studied using a stability-indicating high-performance liquid chromatographic assay method. Calibration curves were produced using linear regression of the peak area against concentration of each drug, with an r ² value ≥ 0.96. Our aim was to investigate the stability of admixture solution of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl for 48 h (25ºC) and 5 days (5ºC), with MgSO ₄ , which has never been assessed. Results: Data obtained for admixtures prepared and stored at temperatures of 25ºC and 5ºC, show that all drugs have reached at least 98% of the initial concentration. Conclusions: For the purpose of pre-preparing drug admixtures to use with confidence, tramadol HCl infusions may be prepared in advance and then thawed before use in clinical units. On the basis of our results, the intravenous mixture of tramadol (7.69 mg/mL), metoclopramide (0.19 mg/mL), ketorolac (1.15 mg/mL), and magnesium sulfate (77 mg/mL) may be considered for a possible commercial formulation.

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Vaccines are the preparations given to patients to evoke immune responses leading to the production of antibodies (humoral) or cell-mediated responses that will combat infectious agents or noninfectious conditions such as malignancies. Alarming safety profile of live vaccines, weak immunogenicity of sub-unit vaccines and immunization, failure due to poor patient compliance to booster doses which should potentiate prime doses are few strong reasons, which necessitated the development of new generation of prophylactic and therapeutic vaccines to promote effective immunization. Attempts are being made to deliver vaccines through carriers as they control the spatial and temporal presentation of antigens to immune system thus leading to their sustained release and targeting. Hence, lower doses of weak immunogens can be effectively directed to stimulate immune responses and eliminate the need for the administration of prime and booster doses as a part of conventional vaccination regimen. This paper reviews carrier systems such as liposomes, microspheres, nanoparticles, dendrimers, micellar systems, ISCOMs, plant-derived viruses which are now being investigated and developed as vaccine delivery systems. This paper also describes various aspects of "needle-free technologies" used to administer the vaccine delivery systems through different routes into the human body.

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Chewing gum is an excellent drug delivery system for self medication as it is convenient, can be administered discreetly without water and offers the removal of 'needle fear' for the patients. As it releases insulin orally, it helps in tackling of the deprivation of insulin by digestive enzyme without adding digestive enzyme inhibitor. This can be done by binding of vitamin B12 and insulin. The vitamin B12 is protected with haptocorrin which is a salivary protein. Another chemical pathway takes over to help vitamin B12 pass into the bloodstream as haptocorrin reaches the intestines. The binding of vitamin B12 and insulin molecules makes the insulin to be protected on this supply chain. The insulin could ride all the way into the bloodstream, where it is released to do its work. By stimulating the brain, chewing gum also increases the releases of insulin. Finding simpler ways to deliver insulin into the blood stream is one important avenue for tackling the diabetes epidemic that is sweeping the developed world. The conditions in gastrointestinal tract may damage the body's protecting and absorbing mechanisms for the valuable molecules. Chewing gum would be a better delivery method in humans.

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Of late, micro and nanoparticluate drug delivery systems have been gaining immense importance primarily attributed to their improved drug release controlling and targeting efficiencies. Also, the small particle size and desirable surface charge associated with these delivery systems render them suitable for specific applications like lymphatic uptake, pulmonary uptake, tumor targeting, brain targeting, etc. For decades, micro and nanoparticulate systems have been prepared by the conventional "trial and error" approach of changing One Variable at a Time (OVAT). Using this methodology, the solution of a specific problematic formulation characteristic can certainly be achieved, but attainment of the true optimal composition is never guaranteed. Thus, the present manuscript provides an updated account of the systematic approach "Design of Experiments (DoE)" as applicable to formulation development of microparticles and nanostructured systems. Besides providing a bird's eye view of the various experimental designs and optimization techniques employed for DoE optimization of such systems, the present manuscript also presents a copilation of the major micro/nano-structuctred systems optimized through DoE till date. In a nutshell, the article will act both as a ready reckoner of DoE optimization of micro/nano drug delivery systems and a catalyst in providing an impetus to young pharmaceutical "nano & micro" researchers to venture into the rewarding field of systematic DoE optimization.

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Background: Azithromycin (AZT) is a macrolide antibiotic derived from and similar in structure to erythromycin. Oral administration of AZT is effective for the treatment of trachoma; however, topical formulations are difficult to develop because of the drug's hydrophobicity. The aim of this study is to formulate a novel topical ophthalmic delivery system of AZT. Materials and Methods: In the present study, ocular inserts of AZT are prepared using alginate, carbopol, and hydroxypropyl methylcellulose (HPMC) to solve the said formulation problem of drug and to facilitate ocular bioavailability. Ocular inserts were prepared by film casting method and the prepared films were subjected to investigations for their physical and mechanical properties, swelling behaviors, ex vivo bioadhesion, and in vitro drug release. Ocular irritation of the developed formulation was also checked by hen's egg chorioallantoic membrane test for ocular irritation potential. Results: The physicochemical, bioadhesive, and swelling properties of films were found to vary significantly depending on the type of polymers used and their combinations. The alginate films exhibited greater bioadhesion and showed higher tensile strength and elasticity than the carbopol films. HPMC addition to the films significantly affected the properties of ocular inserts. Carbopol:HPMC (30:70)-based ocular inserts sustained drug release for longest span of 6 h. The release profile of AZT showed that drug release was by both diffusion and swelling. The formulation was found to be practically nonirritant in ocular irritation studies. Conclusion: AZT can therefore be developed as an ocular insert delivery system for the treatment of ocular surface infections.

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Background: A novel aspiration in treatment of migraine, to provide greater therapeutic effect, overcome the side effects by complex therapeutic regimen and to improve patient compliance upon administering bucco-adhesive tablet formulations of sumatriptan succinate which have not been tested literally. Materials and Methods: This study was designed to develop a bucco-adhesive tablet containing sumatriptan succinate using blends of different bio-adhesive polymeric combinations such as hydroxy propyl methyl cellulose K4M, sodium carboxy methyl cellulose, and Carbopol 934P with a backing layer of ethyl cellulose by a direct compression technique. Tablets were subjected to physico-chemical parameters, swelling index, surface pH, ex vivo bioadhesive force, in vitro drug release, ex vivo drug permeation, and stability in saliva. Results: Good results were obtained in all the evaluated parameters. The drug release of all formulation follows zero-order kinetics by a diffusion mechanism type. Stability studies in human saliva, ex vivo buccal permeation studies by using sheep and porcine buccal mucosa were carried out for the optimized formulation (S4 CP:HPMC 3:1). Conclusion: The developed buccal drug delivery system containing sumatriptan succinate might be the alternative routes available to bypass the first pass metabolism and might be a milestone in the therapy of migraine and among all formulations S4 shows good controlled release results correlated with ex vivo permeation studies.

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Aim : Orodispersible tablets also known as fast dissolving tablets disintegrate instantaneously within the mouth and thus can be consumed without water. The present study was aimed to formulate orodispersible tablets of nimesulide by using Lallemantia reylenne seeds as natural superdisintegrant. Materials and Methods: Powdered lallemantia seeds were characterized for powder flow properties (bulk density, tapped density, carr's consolidation index, hausner ratio, angle of repose), swelling index, viscosity, pH, and loss on drying. The prepared tablets were evaluated for different tablet parametric tests, wetting time, water absorption ratio, effective pore radius, porosity, packing fraction, in vitro and in vivo disintegration time, in vitro dissolution and stability studies. Results and Discussion: Increase in Lallementia reylenne concentration had an appreciable effect on tablet hardness and friability which clearly indicated binding potential of the seeds. Water absorption ratio increased with increase in Lallemantia reylenne concentration from batch A1 to A4. Water uptake coupled natural polymer swelling could be the most probable mechanism for concentration dependent reduction in disintegration time by the Lallemantia reylenne seeds. Porosity of the formulated tablets was found to increase from batch A1-A4. The in vitro disintegration results were in line with in vivo disintegration results. Conclusion: It could be concluded that Lallemantia reylenne seeds could be used as natural superdisintegrant in the formulation of orodispersible tablets.

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The overall objective of the present work was to develop an oral sustained-release (SR) metformin tablet prepared by the direct compression method, using hydrophilic hydroxylpropylmethylcellulose (HPMC) and Guar gum polymer alone and in combination at different concentrations. Metformin hydrochloride (HCl), a biguanide, has a relatively short plasma half-life and low absolute bioavailability. All the batches were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. Mean dissolution time is used to characterize the drug release rate from a dosage form, and indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h whereas when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating SR matrix tablets. Fitting the data to the Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release. Similarity factor ƒ2 values suggest that the test and reference profiles are identical.

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Background: Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by narrow absorption window. The aim of current study was to design sustained release bioadhesive gastroretentive dosage form of ofloxacin. Materials and Methods: A 3 ² full factorial design was employed to systematically study the drug release profile and bioadhesive strength. Carbopol 934P and HPMC K100M were selected as the independent variables. Compatibility between drug and polymer was tested by fourier transform infrared (FTIR) and X-ray diffraction (XRD) techniques. Tablets were prepared by direct compression and were evaluated for tablet characteristics, swelling study, adhesion strength, percent drug released, radiographic imaging study and stability study. The optimized formulation was then compared with marketed formulation (Oflin OD®). Results: Tablets prepared showed good tablet characteristics, optimum swelling property, and good adhesion strength with high detachment force. Most of the formulations including the optimized formulation followed Higuchi kinetics and the drug release mechanism was found to be anomalous. Radiographic image proved that tablet remains intact in its structural integrity and shape in stomach up to 24 h. The short-term accelerated stability testing was carried out for the optimized formulation, and results revealed that drug content, in-vitro dissolution and all other parameters were within acceptable limits. Conclusion: Thus, the prepared bioadhesive gastroretentive ofloxacin tablet may prove to be a potential candidate which increases the bioavailability of ofloxacin for any intragastric condition.

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Aim: Synthesis of superporous hydrogel with different concentrations of crosslinker was carried out using solution polymerization to study its effect on characteristics of superporous hydrogel. Methylene-bis-acrylamide was used as a crosslinker. Materials and Methods: The characterization studies were performed by measurement of apparent density, porosity, swelling studies, mechanical strength studies, and scanning electron microscopy analysis. Results and Discussion: As the concentration of crosslinker increased from 7.37% to 14.36 % the porosities decreased. In double distilled water, superporous hydrogels showed good increase in equilibrium swelling capacity compared to that in simulated gastric fluid. Scanning electron microscopic images clearly indicated the formation of interconnected pore and capillary channels. Characterization studies revealed that the increase in crosslinker concentration is beneficial from the mechanical stability point of view, but at the same time the decrease in porosity may lead to decrease in drug release rate by diffusion through these capillary channels. Batches B1 and B2 with low concentrations of crosslinker provide good porous structure, swelling characteristics, and mechanical strength appropriate for further applications of superporous hydrogel-based drug delivery systems. Conclusion: The concentration of crosslinker affects the porous structure, swelling characteristics and mechanical strength. By setting appropriate degree of crosslinking it is possible to prepare superporous hydrogel having desired characteristics, which will provide a platform to design the drug delivery systems based on it.

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Introduction: Betamethasone dipropionate (BD) has anti-inflammatory, immunomodulatory, and antiproliferative activity. The aim of the current work was to test the hypothesis that the addition of corticosteroid such as BD and a keratolytic agent such as salicylic acid in nanocarrier based microemulsions formulation would result in enhancement and sustaining of corticosteroid delivery rate leading to better anti-psoriatic activity. Clinical use of BD is restricted to some extent due to its poor permeability across the skin. So to increase its permeation across the skin, microemulsion-based gel formulations were prepared and characterised. Materials and Methods: Microemulsions were prepared by aqueous phase titration method, using oleic acid:sefsol (1.5:1), Tween 20, isopropyl alcohol, and distilled water as the oil phase, surfactant, cosurfactant and aqueous phase, respectively. Selected formulations were subjected to physical stability studies and consequently in vitro skin permeation studies. Surface studies of optimized formulation were done by transmission electron microscopy. In vivo anti-inflammatory activity was done by carageenan-induced raw paw edema method. Results: The droplet size of microemulsions ranged from 60 to 190 nm. The optimized formulation exhibited viscosity 28.55 ± 2.03 mP, refractive index 1.409, pH 6.4, and conductivity 10 ^-4 scm ^-1 . The optimized microemulsion was converted into hydrogel using carbopol 934, and salicylic acid was incorporated into it. Drug deposition in skin was found to be 29.73 μg/mg. Assessment of skin permeation was done by histopathology studies which indicated changes in the structure of epidermal membrane of skin. In vivo anti-inflammatory activity indicated 72.11% and 43.96% inhibition of inflammation in case of developed microemulsion gel and marketed gel, respectively. Conclusions: The developed microemulsion gel containing BD and salicylic acid provided sustained and good anti-inflammatory activity for the treatment of psoriasis.

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This paper describes the synthesis of thermosensitive surfactants by polymerizing N-isopropylacrylamide (NIPAAm) into the Pluronic F68 surfactant and their application for a controlled drug release. Poly(NIPAAm)-Pluronic surfactants with different lengths of the NIPAAm block were synthesized by activating two hydroxyl groups of poly(ethylene oxide) (PEO) at the end of Pluronic F68 using cerium ammonium nitrate (CAN, redox initiator), followed by adding the NIPAAm monomer into a reactor. The resultant poly(NIPAAm)-Pluronic surfactants were characterized by FT-IR and gel filtration chromatography (GPC). It was observed that their critical micellar concentrations increased with an increase in the length of the poly(NIPAAm) block. In addition, poly(d,l-lactide-co-glycolide) (PLGA) microparticles was prepared by an oil-in-water emulsion and solvent evaporation method using the poly(NIPAAm)-Pluronic surfactants in an aqueous continuous phase. At 37°C, nile red (model dye) was released from the PLGA microparticles in a more sustained manner when the length of poly(NIPAAm) was longer due to a thicker layer of shrunken poly(NIPAAm) at the surface of the microparticles.

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Introduction: A modified pulsincap dosage form of 5-fluorouracil was developed to target drug to colorectal carcinoma according to daily oscillations of rate-limiting metabolizing enzyme dihydropyrimidine dehydrogenase. Materials and Methods: The capsule body was made water insoluble by exposing the body to formaldehyde vapor. A mixture of granules containing drug, superdisintegrant, and osmogen was filled in the capsule body. A hydrogel plug was fitted to the mouth of the treated body, and the untreated cap was fitted to the body which was coated with Eudragit S100. Developed formulations were evaluated for in vitro drug release in 1.2 pH (2 h), 6.8 pH (3 h), and 7.4 pH (up to 12 h) buffer solutions. A 2 ³ full factorial design was used for optimization in which the type of hydrogel plug (X1), the type of osmogen (X ₂ ), and the type of superdisintegrant (X ₃ ) were selected as independent variables while, cap opening time, percentage drug released in 5(Q ₅ ), 6(Q ₆ ), and 12(Q ₁₂₎ h were taken as dependent variables. Results: Dissolution data were fitted to various models to ascertain the kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. The results of the F-statistics were used to select the most appropriate model. Conclusion: Formulation F ₁ containing sodium starch glycolate, potassium chloride, and hydroxypropyl methylcellulose K4M plug was considered optimum since it showed more similarity to the theoretical predicted dissolution profile (f ₂ = 77.33). The studies indicate that the formulation was effective in providing in vitro colon targeted release and controlled release after predetermined lag time.

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Aim: The aim of the project was to develop cross-linked b-cyclodextrin (CL β-CD) microparticles for controlled delivery of a highly water-soluble drug. Materials and Methods: CL β-CD microparticles were prepared by emulsification phase separation technique using epichlorohydrin as a cross-linking reagent. The developed microparticles were compared with β-CD for their pharmacotechnical properties. A highly water-soluble model drug, pravastatin sodium (PS) was loaded within these hydrophobic microparticles by active drug loading method using nonionic surfactant Tween 80 as the loading facilitator. Results: Maximal drug fixation (216.8 mg/g beads) was observed in pH 4 at 20ºC. In vitro release studies of PS-loaded CL β-CD microparticles in simulated gastric fluid and simulated intestinal fluid resulted in modified dissolution profiles. Modeling of release profiles confirmed controlled release (r² = 0.9910) of PS from the cross-linked system. Conclusion: Controlled release CL β-CD microparticles PS that have the potential to enhance its therapeutic properties by offering the advantage of less frequent dosing and decreased fluctuations in the blood levels during the dosing interval were successfully developed.

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In the present study we investigated the effect of polyamidoamine (PAMAM) dendrimers on the aqueous solubility of aceclofenac. The aqueous solubility of aceclofenac was measured in the presence of dendrimers in distilled water. The effect of variables, such as pH condition, concentration, temperature and generation (molecule size) of dendrimer, has been investigated. Results showed that the solubility of aceclofenac in the dendrimer solutions was proportional to dendrimer concentration. The order in which the dendrimers increased the solubility at a constant pH condition was G3 > G0. The influence of dendrimer solution pH on the solubility enhancement of aceclofenac suggests that it involves an electrostatic interaction between the carboxyl group of the aceclofenac molecule and the amine groups of the dendrimer molecule. The solubility of aceclofenac was inversely proportional to the temperature of dendrimer solution.Different generation (G0 and G3) PAMAM dendrimers have the potential to significantly enhance the solubility of poor water-soluble drugs.

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Buccal films of ondanstron hydrochloride were fabricated from mucoadhesive polymer, chitosan, and polyvinyl pyrrolidone (PVP K30) for the purpose of prolonging drug release and improving its bioavailability. All fabricated film formulations prepared were smooth and translucent, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 98 - 99%, indicating favorable drug loading and uniformity. The inclusion of PVP K30, a hydrophilic polymer, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of the films, although the degree of swelling increased. In vitro drug release studies in simulated saliva showed a prolonged release of over five to six hours for all formulations, except C4, with 99.98% release in 1.5 hours. Kinetic analysis of the release data indicated that the best fit model with the highest correlation coefficient for all formulations was the Peppas model. In vivo studies, on selected films in rabbits, were conducted, to determine the pharmacokinetic parameters such as C _max , T _max , and AUC _0-∞ , using model-independent methods with nonlinear least-squares regression analysis. The AUC and values of C _max of ondansetron hydrochloride were found to be significantly greater (P < 0.005) than the selected films C2 and C3, as compared to those from the oral solution, thereby confirming improved bioavailability via the buccal route. The T _max values were also significantly greater (P < 0.005), indicating the slower release of the drug from buccal films, thereby, providing prolonged effects. Good in vitro-in vivo correlation was observed with R ² values exceeding 0.98, when the percentage of drug released was correlated with the percentage of drug absorbed.

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