Abstract

<p><strong>Objective</strong>:<strong> </strong>The objective of present study is to enhance solubility and bioavailability of poorly soluble <em>bacoside A</em> present in <em>Bacopa monnieri</em> extract using self nano emulsifying drug delivery system (SNEDDS) for the treatment of Alzheimer's disease.</p><p><strong>Methods: </strong>Solubility of the drug was assessed in various oils (edible as well as synthetic oil), surfactant and co-surfactant by saturation solubility study. Pseudo-ternary phase diagram was used to obtain appropriate concentration ranges of components include oil, surfactant and co-surfactant.</p><p><strong>Results: </strong>From the result of saturated solubility study and phase diagram, oleic acid, tween 20 and ethanol was selected as oil, surfactant and co-surfactant. The D-Optimal mixture design was used to optimize the formulation on the basis of solubility of drug and dilution potential. <em>In vitro</em> dissolution, study showed 89% of drug release from optimized SNEDDS formulation compared to untreated drug<em> </em>extract with 24% of drug release in 60 min. Ex vivo diffusion study showed more than 90% of drug diffused from optimized SNEDDS formulation compared to pure extract.</p><p><strong>Conclusion: </strong>In a nutshell, the developed SNEDDS formulation using the design of experimentation approach held great potential as a possible alternative to traditional oral formulations of poorly soluble <em>Bacoside A </em>to improve solubility and bioavailability.</p>

Highlights

  • Bacosides obtained from Brahmi (Bacopa monnierii) mainly used in brain disorder and memory-related disorder which is dose dependent Inhibitor of Acetylcholine esterase (AChe) [1]

  • The aim of the present study is to optimize the percentual composition, characterize and evaluate self nano emulsifying drug delivery system (SNEDDS) formulation of Bacopa monnieri extract employing the concept of design of experiment and enhancement in the solubility and bioavailability of bacoside A

  • Tween 20 was selected as the surfactant for SNEDDS formulation

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Summary

Introduction

Bacosides obtained from Brahmi (Bacopa monnierii) mainly used in brain disorder and memory-related disorder which is dose dependent Inhibitor of Acetylcholine esterase (AChe) [1]. The pharmacological effects of Bacopa monnieri are attributed to the presence of a number of biologically active compounds, including alkaloids, saponins and sterols. Self-micro/nano-emulsifying drug delivery system has gained more attention due to enhanced oral bioavailability enabling a reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug towards specific absorption window in GIT, and protection of drug from the hostile environment in gut. In which D-optimal mixture design technique provides an efficient means of optimizing the optimal formulation of a specific mixture of oil, surfactant, co-surfactant in self-micro emulsifying drug delivery system. The aim of the present study is to optimize the percentual composition, characterize and evaluate SNEDDS formulation of Bacopa monnieri extract employing the concept of design of experiment and enhancement in the solubility and bioavailability of bacoside A

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