Abstract

Objective: The present study was aimed to alter the pharmacokinetic parameters of the drug pentoxifylline using a novel natural mucoadhesive polymer from two different plants, Manilkara zapotta Linn and Ocimum basilicum Linn.
 Methods: The polymer was isolated and six batches of mucoadhesive tablets of pentoxifylline was formulated with 3 different concentrations of each polymer. The best formulation from each of the polymer was selected and administered to rabbits and the plasma drug concentration was compared with the marketed formulation. The pharmacokinetic parameters such as such as Cmax, tmax, AUC, AUMC, λz, t1/2, and MRT were determined.
 Results: The plasma drug concentration vs time curve shows the extended-release of pentoxifylline when compared with the conventional marketed formulation. The results show that there is no change in the peak plasma concentration, but the significant difference was observed in t½, which showed approximately 2.5 fold increase from 2.44 to 6.87 h and the AUC showed five-fold increase from 22.40 to 117.19 μg*h/ml, and other pharmacokinetic parameters, when compared with the marketed formulation.
 Conclusion: The isolated polymer from the plants Manilkara zapotta Linn. and Ocimum basilicum Linn can be used as a carrier for developing mucoadhesive formulations and it alter the pharmacokinetic of pentoxifylline positively.

Highlights

  • Mucoadhesion is a converse of bioadhesion, which is aimed to localize the drugs in the mucosal area of the body

  • The water-soluble polymers were used for the formulation of mucoadhesive drug delivery systems because they become adhesive during hydration

  • The mucoadhesive drug delivery systems are aimed to target the drug with increased gastric residence time, bioavailability, minimized the first-pass effect, controlled release of the drug with reduced adverse effects [2, 3]

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Summary

Introduction

The water-soluble polymers were used for the formulation of mucoadhesive drug delivery systems because they become adhesive during hydration. In vitro experiments have previously reported that the mucoadhesive polymers of MZL [22] and OBL [23] were suitable agents for the preparation of a controlled release tablet formulation of PTX. In this present work, an attempt was made to investigate the effect of these two natural mucoadhesive polymers in the alteration of pharmacokinetic parameters of the PTX.

Results
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