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纳米乳剂作为二甲双胍高效递送的载体。

Nanomulsion as a carrier for efficient delivery of metformin.

作者信息

Akhtar Juber, Siddiqui Hefazat Hussain, Fareed Sheeba, Aqil Mohd

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi 110062, India.

出版信息

Curr Drug Deliv. 2014;11(2):243-52. doi: 10.2174/156720181102140411160817.

DOI:10.2174/156720181102140411160817
PMID:24410150
Abstract

Metformin (MTF) improves hyperglycemia primarily by suppressing glucose production by the liver. The objective of our investigation was to evaluate nanoemulsion as a promising carrier for MTF for sustained hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion, which finally improved biopharmaceutical properties achieved when compared with lipid based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% v/v of oil from the o/w nanoemulsion region of phase diagrams, and then thermodynamic stability and dispersibility tests were performed. The composition of optimized formulation was hydrogenated castor oil (5% v/v), 30% v/v of surfactant (tween 80), co-surfactant (transcutol) and distilled water (65% v/v) as an aqueous phase. The preparation showed maximum drug release (98.70%), optimal globule size (92.25 nm), lowest polydispersity value (0.172), lesser viscosity (22.124 cps) and infinite dilution capability. The antidiabetic activity of optimized MTF nanoemulsion formulation evaluated by blood glucose estimation showed significant hypoglycemic effect which was comparable to that observed with conventional marketed formulation in experimental diabetic rats. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated storage conditions.

摘要

二甲双胍(MTF)主要通过抑制肝脏葡萄糖生成来改善高血糖。我们研究的目的是评估纳米乳剂作为MTF的一种有前景的载体以实现持续降血糖效果。该药物被纳入纳米乳剂的油相中,与脂质基体系相比,最终改善了生物药剂学性质。采用水相滴定法绘制伪三元相图。从相图的o/w纳米乳剂区域中选取油含量相差5% v/v的制剂,然后进行热力学稳定性和分散性测试。优化制剂的组成是氢化蓖麻油(5% v/v)、30% v/v的表面活性剂(吐温80)、助表面活性剂(二乙二醇单乙醚)和作为水相的蒸馏水(65% v/v)。该制剂显示出最大药物释放率(98.70%)、最佳球粒尺寸(92.25 nm)、最低多分散性值(0.172)、较低粘度(22.124 cps)和无限稀释能力。通过血糖测定评估的优化MTF纳米乳剂制剂的抗糖尿病活性显示出显著的降血糖效果,这与在实验性糖尿病大鼠中观察到的传统市售制剂相当。对优化制剂在不同温度和相对湿度下进行稳定性研究,发现其稳定。在加速储存条件下3个月内,制剂未观察到显著变化。

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