PROCESS AND PARAMETERS AFFECTING DRUG RELEASE PERFORMANCE OF PREPARED CROSS-LINKED ALGINATE HYDROGEL BEADS FOR EZETIMIBE

K V Ramana Reddy,M V Nagabhushanam

doi:10.22159/ijpps.2017v9i2.16235

Abstract

Objective: The objective of this study was to formulate an oral sustained release delivery system of ezetimibe mucoadhesive beads by ionic gelation technique based on sodium alginate used as a hydrophilic carrier in combination with carbopol 934P which acts as a rate modifier.Methods: Microbeads of ezetimibe were prepared using an easy method of ionotropic gelation by little modification while in addition of drug. The prepared beads were characterised for mean particle size, entrapment efficiency, swelling capacity, and in vitro release. They were also subjected to various studies such as Fourier Transform Infrared Spectrophotometer (FTIR) Spectroscopy for drug polymer reaction, Scanning Electron Microscopy for surface morphology, and Differential Scanning Calorimetric Analysis to determine the physical state of the drug in the beads.Results: The microspheres of ezetimibe were formulated successfully. The addition of drug concentration gives higher drug loading and higher conc. of Alcl+3 yields small diameter beads and lower drug entrapment. Analysis of the release profiles showed that the data corresponds to zero order release and the diffusion-controlled mechanism as suggested by Higuchi concept.Conclusion: It can be concluded that beads produced by the sequential method had higher drug entrapment. Beads produced by simultaneous yields larger beads in diameter. The concept was cleared that drug release was dependent upon the quantity of polymer and increase in conc. of. aluminium chloride retarded the drug release in the sequential method. Prepared beads enhance the dissolution of ezetimibe and the oral bioavailability and also reduce the fluctuations in the oral bioavailability.

Highlights

Controlled release systems have been extensively developed and advised to superior due to their extensive therapeutic advantages over conventional forms [1]
In Simulated gastric fluids, alginate beads prepared by the sequential method, ezetimibe releases about less than 21% drug in the first 2 h
Ezetimibe was entrapped in aluminium alginate beads prepared with hydrophilic polymer sodium alginate and retarding material carbopol 934P by the using ionotropic gelation method

Summary

Introduction

Controlled release systems have been extensively developed and advised to superior due to their extensive therapeutic advantages over conventional forms [1]. The versatility of polymeric materials allows ease fabrication of the drug delivery devices with a desirable degree of swelling and of the release of the drug. This microparticulate material as in the form of microbeads may be dispensed as filled in hard gelatin capsules or they can be compressed into a suitable dosage form like tablets or hard gelatin capsule [2]. The numbers of the apparent cross-linking sites within the formed aluminium alginate gel beads increased with increasing sodium alginate concentration in the formulation This increase in the apparent crosslinking density delayed the alginate gel disintegration in phosphate buffer due to the retardation of Al+3 exchange with Na+and eventually increasing lag time. Increased alginate gel density per unit volume was thought to affect the decreased pore size within the gels, and ezetimibe release becomes slow

Methods

Results

Conclusion