The purpose of the present study was to develop and optimize the emulgel system for MTZ (Metronidazole), a poorly water soluble drug. The pseudoternary phase diagrams were developed for various microemulsion formulations composed of Capmul 908 P, Acconon MC8-2, and propylene glycol. The emulgel was optimized using a three-factor, two-level factorial design, the independent variables selected were Capmul 908 P, and surfactant mixture (Acconon MC8-2 and gelling agent), and the dependent variables (responses) were a cumulative amount of drug permeated across the dialysis membrane in 24 h (Y 1) and spreadability (Y 2). Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equations were generated for responses Y 1 and Y 2. The statistical validity of the polynomials was established, and optimized formulation factors were selected. Validation of the optimization study with 3 confirmatory runs indicated a high degree of prognostic ability of response surface methodology. Emulgel system of MTZ was developed and optimized using 23 factorial design and could provide an effective treatment against topical infections.

Oral therapy of NSAIDs for treatment of rheumatoid arthritis causes gastric irritation and ulceration. In the present study transdermal patch of ketoprofen was developed using hydroxyl propyl methyl cellulose E5 and Eudragit S100. Patches were prepared by solvent evaporation method. Optimization was carried out by 32 factorial design with polymer concentration (HPMC E5) and plasticizer concentration (propylene glycol) as independent variables. Patches were evaluated for folding endurance, surface pH, drug content, percent moisture content, water uptake and swelling studies. Ex vivo permeation studies of optimized patch was performed using Franz diffusion cell while bioadhesion force and tensile strength were measured by using texture analyzer. Hydrophilic nature, swelling ability and wettability of polymer and plasticizer were responsible for increase in flux and bioadhesion with increase in their concentrations in the factorial batches. Swelling index of all formulations was in the range of 17.3 ±1.2 to 65.29 ±4.78 up to 3h. Flux obtained from all batches was in the range of 3.37±0.23 to 5.43±0.13µg/h/cm2. Anti-inflammatory studies using carrageenan-induced rat paw edema showed greater paw swelling reduction in case of ketoprofen patch. Cumulative percent drug permeation of optimized patch through nylon 66, Wistar rat skin and cadaver skin was found to be 92.3% >86.28 %>63.42% in 8h, while flux order was 6.073> 5.442 > 2.219 µg/h/cm2 respectively. The study concludes that transdermal patch of ketoprofen will be more efficacious with absence of gastric irritation observed in oral formulations. Keywords: Ketoprofen, Bioadhesion, HPMC E5, Flux, Backing membrane

Objective: In the present study, thiol-functionalization of psyllium seed polysaccharide (PSY) was cross-linked with thioglycolic acid by esterification in an attempt to reveal the mucoadhesive properties of thiolated psyllium seed polysaccharide (TPSY). Methods:The crosslinking was carried out by the microwave-assisted method. A simplex centroid design was employed to systematically study the mucoadhesive strength, mucoadhesive retention time and drug release profile. Comparative evaluation of carbopol-based ciprofloxacin hydrochloride (HCl) tablets containing PSY and TPSY was carried out. Acute oral toxicity studies and repeated oral toxicity for TPSY were also conducted.Results: Thiol-functionalization was confirmed by-SH stretch in Fourier Transform infra-red spectra at 2353 cm -1 . Thiolation was observed in thiolated PSY (TPSY) by a change in the surface morphology of psyllium from fibrous to granular and resulted in 82 %swelling in deionized water. TPSY was found to contain 102.35 mmol of thiol groups/g as determined by the Ellman's method. The percent increase in mucoadhesive strength of TPSY was found to be 50.31 % as compared to PSY and 128.30 % as compared to carbopol. The percent increase in mucoadhesive retention time of TPSY was found to be 110 % as compared to PSY and 50 % as compared to carbopol. Conclusion:Mucoadhesion strength and mucoadhesive retention time were greater of tablets containing a higher amount of TPSY. Further, the acute oral toxicity studies and repeated oral toxicity for TPSY proved it as non-toxic and hence safe for human use.

Efavirenz, a non-nucleotide reverse transcriptase inhibitor is an important drug for treating patients with Human Immunodeficiency Virus infections. It belongs to BCS class II have low solubility and poor intrinsic dissolution rate. It is highly basic (pKa 10.2) which makes it suitable candidate for floating dosage form for continuous delivery in stomach.The study was aimed to improve the solubility by solid dispersion technique.Saturation solubility study and drug content were evaluated for solid dispersion preparation. Saturation solubility shows 8 fold increases in 0.1 N HCL compared to plain drug and drug content was found to be between 95%-102%. Further effervescent floating gastroretentive drug delivery system was prepared by 32 full factorial design with independent variables i.e., concentration of HPMC K100 as matrix forming agent and citric acid as gas generating agent. Lag time, floating time, percent drug release were studied as responses. The optimized batch exhibited floating lag time of 40 sec and the in vitro release studies showed 89.5% drug release in 9 h and tablet remained floating for greater than 8 h. The study thus demonstrated that solubility is increased by solid dispersion technique and floating delivery systems may increase solubility and bioavailability of Efavirenz.

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