The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release-Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability.

The objective of the present work was to prepare cocrystals of poorly soluble drug Atorvastatin Calcium (AVA) with the aim of increasing its solubility and dissolution properties. Screening of 8 cocrystal formers (CCFs) was performed by Hansen solubility parameter (HSPs) using 4 methods-neat grinding, solvent drop grinding, solvent evaporation and sonocrystallization in equimolar ratio. Solubility of AVA cocrystal (1.9 fold increase) in comparison to plain AVA drug has been demonstrated with solubility experiments. FTIR spectra of AVA cocrystal showed disappearance of O-H group indicating the formation of hydrogen bond synthon between the drug and CCFs. DSC thermogram showed drastic reduction in melting point from 164.6°C to 71.9 °C indicating the reduction in cohesive energy and increase in solubility. XRD pattern showed new crystalline peaks at 2θ values of 9.858°, 15.201°, 22.907°, 25.407°, 29.496°. SEM analysis showed changes in the morphological characteristics as compared to drug and CCFs, indicating different crystalline nature. Experimental design was applied to optimize AVA cocrystal IR tablet for concentration of aerosil (X1) and MMC 102 (X2) and were evaluated for drug release (Y1) and friability (Y2). It was found that as the concentration of aerosil and MMC 102 increased friability decreased and %drug release increased. A drug release of 98.54±1.163% and friability of 0.515±0.090 % was obtained for optimized batch. Ex vivo diffusion study was carried out by isolating rat stomach tissue, exhibiting higher drug release (95.71±0.98 %) than plain AVA and marketed tablet. Thus formulating AVA cocrystal and its subsequent formulation in optimized IR tablet gives a promising opportunity for manufacturing a drug with increased bioavailability.

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Objective: To investigate the in vitro antibacterial activity of a naturally occurring polyphenol chlorogenic acid (CGA) and compares it with formulated chlorogenic acid phytovesicles against 4 different bacterial strains; two gram positive [Staphylococcous aureus and Bacillus subtilis] and two gram negative strains [Klebsiella pneumonia and Escherichia coli]. Methods: CGA phytovesicles were developed and optimized using central composite design to improvise CGA’s physicochemical properties. Bactericidal activity was evaluated using agar diffusion, minimum inhibitory concentration (MIC) and time kill assay. The effect of pH and temperature on the antimicrobial activity was determined. Results: The optimized CGA phytovesicles showed entrapment of 96.89% with 30 times better lipophilic solubility than the plain drug. The inhibition zone sizes for CGA phytovesicle ranged from 17-25 mm as compared to 15-20 mm of plain CGA while the MIC values ranged 200-250 µg/ml as compared to 500-550 µg/ml of plain CGA. CGA phytovesicles exhibited a strong bactericidal effect at MIC with a log reduction in the range of 0.90-2.04 in Colony forming units (CFUs) at 24h for different strains as compared to 1.38-2.17 of plain CGA. Furthermore, the antibacterial effect was found to augment with increasing temperature but decreased with alkaline pH. Conclusion: Results strongly supports the hypothesis of potential use of CGA phytovesicles as a mode of drug delivery for its antibacterial use against different resistant bacteria.