Objective:The goal of the present investigation was to improve the solubility and bioavailability of atovaquone tablet, using in-house biosynthesized biosurfactant in the ternary system of solid dispersion containing hydrophilic polymers with varying concentrations of biosurfactant. Atovaquone is an anti-malarial agent and belongs to biopharmaceutical classification system class IV.
Methods:The solid dispersion of binary and ternary mixture was prepared using hydroxyl propyl methyl cellulose (HPMC) and biosurfactant respectively by a solvent evaporation method. All the atovaquone tablet formulations were prepared by incorporation of physical mixture, binary and ternary solid dispersed products with excipients by direct compression method. Pre-compression and post-compression parameters of atovaquone tablets were evaluated. In vivo bioavailability study was performed using female albino rabbits.
Results:In vitro dissolution profile of binary and ternary system of solid dispersion products showed 8.65% and 34.64% respectively. Precompression and post-compression values of all atovaquone tablets formulations were within the specified limits. In vitro dissolution efficiency of F2 and F5 were 1.44 fold and 6.62 fold respectively, in accordance to the F1. In vivo study revealed that bioavailability of optimized formulation F5 was increased by 2.5 times and time to reach peak concentration was reduced to 1.4 h, in accordance to pure atovaquone suspension.
Conclusion:Potential application of biosurfactant in the solid dosage form of atovaquone tablet was proved for enhanced dissolution rate and bioavailability of atovaquone for malaria treatment. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s
Objectives:The goal of the study was to develop, optimize and in vitro-ex vivo investigation of Brimonidine tartrate nanosuspension incorporated in situ gel formulation to differentiate with marketed (formulation) eye drops for the efficient treatment of glaucoma. Materials and Methods: Nanosuspensions were formulated by solvent evaporation method using probe sonication technique. The effect of the independent variables Tween 80 and Pluronic F68 concentration on Nanosuspension properties were investigated by performing 3 2 factorial design of experiment. Nanosuspensions were characterized by measuring particle diameter and zeta potential, surface morphology, drug entrapment efficiency and then nanosuspensions were incorporated in to in situ gel base for in vitro release and ex-vivo corneal permeability studies and were differentiated with marketed product. Results and Discussion: The most excellent nanosuspension formulation system selected via the Design Expert 12 software program was F7 which contains 0.5% of Tween 80 and 3 % of Pluronic F68. An optimized nanosuspension formulation F7 showed an average particle diameter of 157.4±0.95 nm with PDI of 0.379 and a zeta potential of -19.1 mV. It had an average entrapment efficiency of 85.95±1.40%. It also showed 98.36±0.58% of drug being released in vitro when incorporated in to in situ gel base over 24 hr. F7 showed significantly greater drug permeation in comparison to the marketed eye drop formulation in ex vivo transcorneal permeability studies and was able of retaining its stability for 90 days. Conclusion: The developed nanosuspension incorporated in situ gel base formulation could be utilized as potential delivery system for long time management of glaucoma with once daily dose.
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