FORMULATION AND EVALUATION OF SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF GLICLAZIDE

Suwarna R Deshmukh,Gouri R Dixit,Kanchan P Upadhye,Suparna S Bakhle

doi:10.22159/ijpps.2016v8i11.14104

Abstract

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

Highlights

IntroductionWater-soluble drug candidates often emerge from contemporary drug discovery programs and present formulators with considerable technical challenges
The enhancement of oral bioavailability of poorly soluble drugs remains one of the most challenging aspects of drug development [1].Poorly water-soluble drug candidates often emerge from contemporary drug discovery programs and present formulators with considerable technical challenges
Solubility studies were performed to identify suitable excipients with maximum potential to solubilize the drug and having good miscibility with each other which helps in minimizing the final volume of Self-emulsifying drug delivery system (SEDDS) and potentiates optimal drug loading [18]

Summary

Introduction

Water-soluble drug candidates often emerge from contemporary drug discovery programs and present formulators with considerable technical challenges. The absorption of such compounds, when presented in the crystalline state to the gastrointestinal tract, is typically dissolution rate-limited, and the drugs are typically biopharmaceutical classification system (BCS) class II or class IV compounds [2]. To overcome these problems, various strategies are exploited including the use of surfactants, lipids, permeation enhancers, micronization, salt formation, cyclodextrins, nanoparticles and solid dispersions. The interests on lipid-based drug delivery systems (LBDDS) have increased over the past two decades as a function of identification of these pharmaceutically difficult candidates and increased even further after the successful launch of lipid-based oral pharmaceutical products, including in particular cyclosporine A, marketed as Sandimmune TM and Neoral TM [4]

Methods

Results

Conclusion