Objective: The study aims at the formulation and optimization of gemfibrozil (Gem) nanosuspension (NS) for improving its solubility and dissolution rate.Method: Gem NS was prepared by precipitation-ultrasonication method using ethanol as solvent, water as anti-solvent, and polyvinyl alcohol (PVA) as a stabilizer. A Box–Behnken design was employed to study the effect of the independent variables, Gem concentration in the organic phase (X1), PVA concentration (X2) and sonication time (X3) on the dependent variable, drug release after 90 min (Y). The resulting data were statistically analyzed and subjected to 3D response surface methodology to study the influence of variables on the response. NS was evaluated for particle size, zeta potential, solubility and in vitro drug release and characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD).Results: On the basis of the evaluation, NS4 formulation (with 80 mg/ml Gem, 0.5% PVA concentration, and 20 min of sonication time) demonstrated highest drug content with a particle size of 191.0 nm and zeta potential of −12.0 mV. Dissolution profiles of NS indicated 2.5-fold increase in drug release than pure drug. NS demonstrated 5- and 9-fold increase in solubility, in water, and phosphate buffer (pH 7.5), respectively, pure drug. DSC and XRD studies indicated changes in the crystallinity of Gem during NS formulation. No chemical change was evident in NS as indicated by FTIR.Conclusion: Gem NS formulation could serve as a promising approach for improving its solubility and dissolution rate.

Objective: The purpose of this study was to developed microemulsion based gel formulation for topical delivery of dapsone with an objective to increase the solubility and skin permeability of the drug for treatment of acne. Methodology: The solubility of dapsone in oils, surfactants and cosurfactants was evaluated by saturation solubility to screen the components of the microemulsion. The pseudoternary phase diagrams were constructed using capryol 90 and N-methyl-2 pyrrolidone as the oil phase, Kolliphor EL as surfactant and PEG 400 as the co-surfactant. The system were assessed for drug-loading efficiency and characterized for pH, conductance, viscosity, particle size, drug content, globule size, zeta potential and drug release. Optimized formulation systems were formulated into gel form by using poloxamer-407 and evaluated for viscosity, spreadability, drug content, stability, in-vitro skin permeation, steady state flux, permeability coefficient, enhancement ration and skin irritation study. Result and Discussion: Globule size of optimized microemulsion (F2) was found to be 27.53 nm, zeta potential was found to be-14.6 mV, permeability of drug from microemulsion within 8h was observed 82%, In-vitro diffusion study showed increase in flux of microemulsion based gel (392.43 µg cm-2 h-1) to that of simple dapsone gel (274.4 ± 0.78 µg cm-2h-1). Draize test revealed absence of irritation and inflammation on rat skin. Conclusion: Microemulsion based gel of dapsone formulation provided better application property and stability in comparison to simple gel. This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

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Vaginitis is a very common gynecological problem in women of all age groups. Metronidazole is a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class and used against protozoa such as Trichomonas vaginalis, amebiasis, and giardiasis. The present study was aimed with the application of chitosan in combination with anionic polymers for the design and development of mucoadhesive tablets for vaginal delivery of Metronidazole. Matrix tablets of metronidazole were prepared in combination with polyelectrolyte complex by wet granulation method and further characterized for various formulation parameters, in-vitro muco adhesion and antimicrobial activity. The developed formulation showed significant mucoadhesion due to presence of chitosan or carrageenan and ionisation of amino groups of chitosan at pH 5.2. The developed formulation showed desirable characteristics in terms of FTIR, DSC, SEM, in vitro drug release, swelling behaviour as well for mucoadhesion and antimicrobial potential compared with the marketed formulation. In overall developed dosage form imparts desirable characteristics in formulation for vaginal delivery of metronidazole with enhanced therapeutic effects. Thus, this dosage form can be further investigated for therapeutic applications of metronidazole in vaginal drug delivery.

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