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The aim of this study was to formulate nanoparticles (NPs) containing glibenclamide (GB) prepared with Eudragit L100 to achieve a better release profile suitable for per oral administration with enhanced efficacy. The NPs were prepared by solvent displacement method. The influence of various formulation factors (drug: polymer ratio and concentration of surfactants) on particle size, size distribution, zeta potential, drug loading and encapsulation efficiency were investigated. Drug: polymer ratio was observed to be important parameter influencing mean particle size, beside others. Encapsulation efficiency and drug loading capacity were found to be increased as drug concentration increases with respect to polymer. Addition of surfactants showed a promising result in decreasing particle size of NPs. Dissolution study revealed increased release of GB from NPs. Transmission electron microscopy (TEM) study revealed spherical morphology of the developed NPs. Differential scanning calorimetry (DSC) studies confirmed phase transition behavior of NPs. They also showed very significant change in saturation solubility in comparison with pure drug. Developed NPs revealed a decreased tmin and enhanced bioavailability and hence superior activity as compared to plain GB in alloxaninduced diabetic rabbit model. The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance.