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用于体外药物释放研究的载有特比萘芬的脂质体纳米颗粒的制备。

Preparation of liposomal nanoparticles incorporating terbinafine in vitro drug release studies.

作者信息

Koutsoulas Charalampos, Pippa Natassa, Demetzos Costas, Zabka Marian

出版信息

J Nanosci Nanotechnol. 2014 Jun;14(6):4529-33. doi: 10.1166/jnn.2014.9026.

Abstract

Terbinafine hydrochloride (TBH) (E)-N-(6,6-dimethyl-2-hepten-4-inyl)-N-methyl-1-naphthaline-methanamine(-hydrochloride) is an effective antifungal agent already existing on the market in the form of topical formulations. The present study deals with the preparation and physicochemical characterization (size, polydispersity, zeta-potential) of 1,2-Diacyl-sn-glycero-3-phosphocholine (EggPC) incorporating TBH in two different dispersion media (tris-buffered saline (TBS) of pH 7.4 or in phosphate buffer solution (PS) of pH 5.5) in order to investigate how pH of dispersion media affects the incorporation efficiency of TBH into liposomes. There were further prepared three Carbopol 934 hydrogels of different concentrations (0.5, 1 and 2%) and their viscosity was measured and evaluated. Moreover, the in vitro drug release from three liposomal gels was studied, in order to investigate the ability of liposomes to act as carriers for TBH in a gel. All formulations were found to retain their original physicochemical properties at least for three weeks. These early studies on the release kinetics from liposomal gel show that Korsmeyer-Peppas model could be the best fitted model concerning the TBH release profile and could be supported biophysically from extended Derjaguin-Landau-Verwey-Overbeek (DLVO) theory.

摘要

盐酸特比萘芬(TBH)(E)-N-(6,6-二甲基-2-庚烯-4-炔基)-N-甲基-1-萘甲胺(盐酸盐)是一种有效的抗真菌剂,已以局部制剂的形式投放市场。本研究涉及在两种不同的分散介质(pH 7.4的三羟甲基氨基甲烷缓冲盐水(TBS)或pH 5.5的磷酸盐缓冲溶液(PS))中制备并对包载TBH的1,2-二酰基-sn-甘油-3-磷酸胆碱(EggPC)进行物理化学表征(粒径、多分散性、ζ电位),以研究分散介质的pH值如何影响TBH掺入脂质体的效率。还制备了三种不同浓度(0.5%、1%和2%)的卡波姆934水凝胶,并对其粘度进行了测量和评估。此外,还研究了三种脂质体凝胶的体外药物释放情况,以研究脂质体在凝胶中作为TBH载体的能力。所有制剂至少在三周内保持其原始物理化学性质。这些关于脂质体凝胶释放动力学的早期研究表明,Korsmeyer-Peppas模型可能是最适合TBH释放曲线的模型,并且可以从扩展的Derjaguin-Landau-Verwey-Overbeek(DLVO)理论得到生物物理学支持。

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