Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, 25240, Erzurum, Turkey.
Pharm Dev Technol. 2013 May-Jun;18(3):570-6. doi: 10.3109/10837450.2011.604783. Epub 2011 Aug 24.
The aim of the present study was to develop and characterize metformin HCl-loaded nanoparticle formulations. Nanoparticles were prepared by the nanoprecipitation method using both a single polymer (Eudragit(®)RSPO) and a polymer mixture (Eudragit/PLGA). The mean particle size ranged from 268.8 to 288 nm and the nanoparticle surface was positively charged (9.72 to 10.1 mV). The highest encapsulation efficiency was observed when Eudragit®RSPO was used. All formulations showed highly reproducible drug release profiles and the in vitro drug release in phosphate buffer (pH = 6.8) ranged from 92 to 100% in 12 h. These results suggest that Eudragit(®)RSPO or Eudragit/PLGA nanoparticles might represent a promising sustained-release oral formulation for metformin HCl, reducing the necessity of repeated administrations of high doses to maintain effective plasma concentrations, and thus, increasing patient compliance and reducing the incidence of side-effects.
本研究旨在开发和表征盐酸二甲双胍载药纳米粒制剂。纳米粒通过纳米沉淀法制备,使用单一聚合物(Eudragit(®)RSPO)和聚合物混合物(Eudragit/PLGA)。平均粒径范围为 268.8 至 288nm,纳米粒表面带正电荷(9.72 至 10.1 mV)。当使用 Eudragit®RSPO 时,观察到最高的包封效率。所有制剂均表现出高度重现的药物释放曲线,在 12 小时内,在磷酸盐缓冲液(pH = 6.8)中的体外药物释放范围为 92%至 100%。这些结果表明,Eudragit(®)RSPO 或 Eudragit/PLGA 纳米粒可能代表一种有前途的盐酸二甲双胍缓释口服制剂,减少了维持有效血浆浓度所需的高剂量重复给药的必要性,从而提高了患者的依从性并降低了副作用的发生率。