PREPARATION, EVALUATION AND STABILITY OF LAMIVUDINE LOADED ALGINATE-TAMARIND MUCILAGE MICROSPHERES

Santosh Gada,C Mallikarjuna Setty,Anandkumar Y

doi:10.22159/ijap.2019v11i4.33808

Abstract

Objective: The objective of the present study was to investigate the possibility of obtaining a controlled, relatively constant effective level of lamivudine microspheres. Methods: Lamivudine loaded sodium alginate (SA) and tamarind mucilage(TM) mucoadhesive microspheres were prepared by ionic gelation technique with three different proportions of SA and TM with different concentrations of CaCl2. The prepared microspheres were evaluated for drug loading, particle size distribution, surface morphology, FTIR, in vitro wash off, in vitro release and stability studies. Results: The microspheres were found to be free flowing having diameter ranging from 769.22 to 978.56 µm, drug encapsulation efficiency (DEE) was found to be 65.28 to 92.33%. Percent drug release after 12 h were ranging from 85±1.51 to 97±1.44. In vitro release profile of all formulations shows slow controlled release up to 12 h. In vitro wash off studies shown fairly good mucoadhesivity with 20% microspheres adhered after 6h. Stability studies showed that no significant change in particle size and maximum DEE in comparison to the formulation stored at room temperature. Results: The lamivudine loaded SA-TM mucoadhesive microspheres can be conveniently prepared which showed better result and it may be used full for controlling the drug release and improve the bioavailability.

Highlights

Oral drug delivery systems continue to be the most accepted and popular one among all the drug delivery systems as it offers several advantages over the conventional drug delivery systems like improving patient’s compliance and convenience due to the reduction of frequency of administration [1]
Rigid and discrete lamivudine loaded sodium alginate (SA)-tamarind mucilage (TM) mucoadhesive microspheres were obtained when dispersion mixture of SA, TM and core material lamivudine added in a solution containing calcium ions
The drug encapsulation efficiency (DEE) in lamivudine loaded SA-TM mucoadhesive microspheres were within the range between 65.28±3.14 and 92.33±3.93 % w/w

Summary

Introduction

Oral drug delivery systems continue to be the most accepted and popular one among all the drug delivery systems as it offers several advantages over the conventional drug delivery systems like improving patient’s compliance and convenience due to the reduction of frequency of administration [1]. The formulation of controlled drug delivery systems is important to achieve better clinical efficacy and patient compliance [2], Such systems are highly desirable for drugs that have a short half-life to avoid unnecessary side effects, burst effect or overdose [3, 4]. Microspheres possess important features among the controlled drug delivery systems by virtue of their small size and efficient carrier characteristics [9], but the success of dosage form is limited due to its residence time. Mucoadhesive microsphere drug delivery systems are used to extend the residence time at the site of application, maintain therapeutically effective plasma drug concentration levels for a longer duration, reducing the dosing frequency and minimize fluctuations in the plasma drug concentration at the steady state in the controlled and reproducible manner [10,11,12].

Methods

Results

Conclusion