Abstract
Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage.
 Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design.
 Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism.
 Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.
Highlights
The main goal of drug delivery systems is to achieve a desired concentration of the drug in blood or tissue, which is therapeutically effective and non-toxic for a prolonged period
Lamivudine obtained as gift sample from Hetero Drugs Private Ltd, Sodium alginate and calcium chloride were procured from yarrow chemicals and SD fine chemicals Mumbai respectively
Mucilage was isolated from drumstick (Moringa oleifera) pod and the average yield of mucilage was found 5.86% w/w
Summary
The main goal of drug delivery systems is to achieve a desired concentration of the drug in blood or tissue, which is therapeutically effective and non-toxic for a prolonged period. The mucoadhesive polymer containing oral drug delivery systems has the capacity to prolong the residence time of drugs at the absorption site and facilitate intimate contact with an underlying absorptive surface to enhance bioavailability [2]. Alginates have been widely used in the development of drug delivery applications [4,5,6,7]. The blending of different mucoadhesive polymers is one of the most popular approaches to formulate ionotropically cross-linked alginate-based mucoadhesive spheres [10, 12, 13]. Blending with suitable polymers, may improve the drug encapsulation, which is found comparatively lower in alginate-based microspheres prepared by ionotropic-gelation method [7]
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