Dora Chander Parkash, Singh Shailendra Kumar, Kumar Sanjeev, Datusalia Ashok Kumar, Deep Aakash
Division of Drug Delivery and Research, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001, India.
Acta Pol Pharm. 2010 May-Jun;67(3):283-90.
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 t(min) and enhanced bioavailability and hence superior activity as compared to plain GB in alloxan-induced diabetic rabbit model. The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance.
本研究的目的是制备含有格列本脲（GB）的纳米颗粒（NPs），该纳米颗粒由Eudragit L100制备，以实现更适合口服给药的释放曲线，并提高疗效。通过溶剂置换法制备纳米颗粒。研究了各种制剂因素（药物:聚合物比例和表面活性剂浓度）对粒径、粒径分布、zeta电位、载药量和包封率的影响。除其他因素外，药物:聚合物比例被认为是影响平均粒径的重要参数。随着药物浓度相对于聚合物的增加，包封率和载药量增加。表面活性剂的添加在降低纳米颗粒粒径方面显示出有希望的结果。溶出度研究表明纳米颗粒中格列本脲的释放增加。透射电子显微镜（TEM）研究显示所制备的纳米颗粒呈球形形态。差示扫描量热法（DSC）研究证实了纳米颗粒的相变行为。与纯药物相比，它们在饱和溶解度方面也显示出非常显著的变化。在四氧嘧啶诱导的糖尿病兔模型中，所制备的纳米颗粒显示出t(min)降低、生物利用度提高，因此与普通格列本脲相比具有更高的活性。所制备的纳米颗粒可以减少给药频率，降低副作用，并提高患者的依从性。
