Gundogdu Nuran, Cetin Meltem
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey.
Pak J Pharm Sci. 2014 Nov;27(6):1923-9.
In this study, the preparation and in vitro characterisation of metformin HCl-loaded CS-PLGA nanoparticles (NPs) were aimed. The prepared nanoparticles (blank nanoparticles (C-1), 50 mg of metformin HCl loaded nanoparticles (C-2) and 75 mg of metformin HCl loaded nanoparticles (C-3) ranged in size from 506.67±13.61 to 516.33±16.85 nm and had surface charges of 22.57±1.21 to 32.37±0.57 mV. Low encapsulation efficiency was observed for both nanoparticle formulations due to the leakage of metformin HCl to the external medium during preparation of nanoparticles. Nanoparticle formulations showed highly reproducible drug release profiles. ~20% of metformin HCl was released within 30 minutes and approximately 98% of the loaded metformin HCl was released at 144 hours in a phosphate buffer (PB; pH 6.8). No statistically significant difference was noted between the in vitro release profiles of the nanoparticles (C-2 and C-3) containing metformin HCl. Also, nanoparticles were characterised using FT-IR and DSC.
本研究旨在制备载盐酸二甲双胍的壳聚糖-聚乳酸-羟基乙酸共聚物纳米粒(NPs)并对其进行体外表征。制备的纳米粒(空白纳米粒(C-1)、50 mg载盐酸二甲双胍纳米粒(C-2)和75 mg载盐酸二甲双胍纳米粒(C-3))粒径范围为506.67±13.61至516.33±16.85 nm,表面电荷为22.57±1.21至32.37±0.57 mV。由于在纳米粒制备过程中盐酸二甲双胍泄漏到外部介质中,两种纳米粒制剂的包封率均较低。纳米粒制剂显示出高度可重复的药物释放曲线。在磷酸盐缓冲液(PB;pH 6.8)中,约20%的盐酸二甲双胍在30分钟内释放,约98%的载药盐酸二甲双胍在144小时时释放。含盐酸二甲双胍的纳米粒(C-2和C-3)的体外释放曲线之间未观察到统计学上的显著差异。此外,还使用傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)对纳米粒进行了表征。