PREPARATION, CHARACTERIZATION AND EVALUATION OF POLY (LACTIDE –CO –GLYCOLIDE) MICROSPHERES FOR THE CONTROLLED RELEASE OF ZIDOVUDINE

Seema Kohli,Suchit Jain,Abhisek Pal

doi:10.22159/ijpps.2017v9i12.18377

Abstract

Objective: The purpose of this research work was to develop and evaluate microspheres appropriate for controlled release of zidovudine (AZT).Methods: The AZT loaded polylactide-co-glycolide (PLGA) microspheres were prepared by W/O/O double emulsion solvent diffusion method. Compatibility of drug and polymer was studied by Fourier-transform infrared spectroscopy (FTIR). The influence of formulation factors (drug: polymer ratio, stirring speed, the concentration of surfactant) on particle size encapsulation efficiency and in vitro release characteristics of the microspheres was investigated. Release kinetics was studied and stability study was performed as per ICH guidelines.Results: Scanning electron microscopy (SEM) images show good reproducibility of microspheres from different batches. The average particle size was in the range of 216-306 μm. The drug-loaded microspheres showed 74.42±5.08% entrapment efficiency. The cumulative percentage released in phosphate Buffer solution (PBS) buffer was found to be 55.32±5.89 to 74.42±5.08 %. The highest regressions (0.981) were obtained for zero order kinetics followed by Higuchi (0.968) and first order (0.803).Conclusion: Microsphere prepared by double emulsion solvent diffusion method was investigated and the results revealed that 216-306 μm microsphere was successfully encapsulated in a polymer. FT-IR analysis, entrapment efficiency and SEM Studies revealed the good reproducibility from batch to batch. The microspheres were of an appropriate size and suitable for oral administration. Thus the current investigation show promising results of PLGA microspheres as a matrix for drug delivery and merit for In vivo studies for scale up the technology.

Highlights

Human Immunodeficiency Virus infection and Acquired Immune Deficiency Syndrome commonly referred to as HIV/AIDS has emerged as being the most serious and challenging public health problems in the world
Once the genetic material of HIV has been changed into DNA, this viral DNA enters the host cell nucleus where it can be integrated into the genetic material of the cell
Microsphere coating or encapsulation with polymer using the double emulsion solvent diffusion method was investigated in this research

Summary

Introduction

Human Immunodeficiency Virus infection and Acquired Immune Deficiency Syndrome commonly referred to as HIV/AIDS has emerged as being the most serious and challenging public health problems in the world. Following fusion of the virus with the host cell, HIV enters the cell. The virus RNA is released and undergoes reverse transcription into DNA by an enzyme in HIV called reverse transcriptase. Once the genetic material of HIV has been changed into DNA, this viral DNA enters the host cell nucleus where it can be integrated into the genetic material of the cell. Once the viral DNA is integrated into the genetic material of the host, it is possible that HIV may persist in a latent state for many years [2,3,4,5]. Activation of the host cells results in the transcription of viral DNA into messenger RNA (mRNA), which is translated into viral proteins. Following assembly at the cell surface, the virus buds forth from the cell and is released to infect another cell [6]

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