氯诺昔康负载立方体体:制备和体外表征。

Rasha Saadi Younus Alkawak, Nawal A. Rajab
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引用次数: 4

摘要

立方体体是一种纳米级结构的自组装纳米结构材料,用于控制被包裹的药物分子的释放。氯诺昔康(LXM)是一种有效的镇痛非甾体抗炎(NSAID)药物,半衰期短(3-4小时)。本研究旨在制备形态清晰、粒径大小、PDI、包封效率高、药物缓释和zeta电位值高的lxm负载立方体体作为透皮给药系统。采用溶剂稀释法,以单油酸甘油酯(GMO)为极性脂质,不同稳定剂为Pluronic®F127或tween 80,不同类型的水相为乙醇或丙二醇,制备了12种负载lxm的立方体体分散体配方。对各配方进行粒径分析、PDI、E.E. %、体外释放度等评价,优选出一组最佳配方,并通过透射电子显微镜(TEM)和zeta电位分析仪对其进行表征,优选出最佳分散度。用红外光谱研究了该药物与辅料的配伍性。结果表明,由GMO、Pluronic®F127、乙醇、药物和磷酸盐缓冲液组成的F3,其pH分别为7.28%、1.82%、8%、2%和80.9% w/w,搅拌时间为20min,具有较高的e - e %(94.30±0.002%)、较小的粒径(16.3±0.19nm)、较低的PDI(0.06±0.02)、较高的zeta电位值(-65.9±0.05mV)和良好的立方结构。FTIR研究表明,LXM与其他配方成分无交互作用。本研究的结论表明,载lxm的立方体体分散体可以被认为是一种很有前途的经皮给药纳米载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Lornoxicam-Loaded Cubosomes: - Preparation and In vitro Characterization.
Cubosomes are nanosized structures self-assembled nanostructured materials used for controlling the release of the entrapped drug molecule. Lornoxicam (LXM) is a potent analgesic nonsteroidal anti-inflammatory (NSAID) drug with a short half-life (3-4) hours. The present study aims to prepare LXM-loaded cubosomes with well-defined morphology, particle size, PDI, high entrapment efficiency, sustained drug release, and high zeta potential value, as a transdermal drug delivery system.       Twelve formulas of LXM-loaded cubosomal dispersions were prepared by a solvent dilution method using Glyceryl monooleate ( GMO) as polar lipid with different stabilizers as Pluronic® F127 or tween 80 and different types of hydrotrope as ethanol or propylene glycol. These formulas were evaluated for their particle size analysis & PDI, E.E. %, and in-vitro drug release to select a group of the optimum formulas, that further characterized by transmission electron microscopy (TEM) and zeta potential analyzer to select the optimum dispersion. FTIR study was used to investigate the compatibility of the drug with excipients. The obtained results indicated that F3, composed of GMO, Pluronic® F127, ethanol, drug, and phosphate buffer solution pH 7.4 in the following per cents 7.28%, 1.82%, 8%, 2%, and 80.9% w/w, respectively, prepared in 20min agitation period, as the optimum formula for its high E.E. % (94.30±0.002%), small particle size (16.3±0.19nm), low PDI          (0.06±0.02), and high zeta potential value (-65.9±0.05mV), and well-defined cubic structure. FTIR study indicated no interaction between LXM and other formulas components. This study's conclusion illustrated that LXM-loaded cubosomal dispersion could be considered a promising nano-carrier for transdermal drug delivery.
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