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载姜黄素纳米结构脂质载体的部分水解人参皂苷修饰。

Curcumin-Loaded Nanostructured Lipid Carrier Modified with Partially Hydrolyzed Ginsenoside.

机构信息

College of Pharmacy, Gachon University, 191 Hambakmoero, Yeonsu-gu, Incheon, 21936, South Korea.

出版信息

AAPS PharmSciTech. 2019 Jul 12;20(6):252. doi: 10.1208/s12249-019-1467-z.

Abstract

The objective of the present study was to investigate the effect of partially hydrolyzed ginsenoside on the physicochemical properties and in vitro release of curcumin from phospholipid-based nanostructured lipid carrier (NLC). NLC formulas modified with partially hydrolyzed ginsenoside (NLC-PG) were prepared with different amounts of ginsenoside using the conventional hot-melt method. The average particle size of curcumin-loaded NLC-PG ranged from 150 to 200 nm, and polydispersity index was in the range of 0.101-0.177, indicating monodispersed particle size distribution. Optical microscopy showed no sedimentation or recrystallization of curcumin even at 10,000 μg/ml concentration as NLC-PG in distilled water, indicating significantly enhanced solubility. TEM image showed that the nanoparticles were monodispersed with a multilayered core/shell structure. X-ray diffraction and FTIR spectroscopy showed that curcumin was amorphous in the NLC-PG, and there was no interaction between curcumin and the excipients. In vitro release study using simulated gastric/intestinal fluid media revealed that the release rate (J) of curcumin from the NLC-PG increased as a function of the ginsenoside content in the lipid carrier. Moreover, the J of curcumin kept gradually increasing in the presence of lipase, whereas in the presence of viscozyme, it sharply increased until the ginsenoside content reached 9.09% and subsequently plateaued. Partially hydrolyzed ginsenoside increased the J of curcumin from curcumin-loaded NLC-PG and therefore may be useful for improving the bioavailability of curcumin.

摘要

本研究旨在探讨部分水解人参皂苷对姜黄素从基于磷脂的纳米结构化脂质载体(NLC)中理化性质和体外释放的影响。采用常规热熔法,用不同量的人参皂苷对 NLC 配方进行改性,制备部分水解人参皂苷(NLC-PG)。载有姜黄素的 NLC-PG 的平均粒径在 150 至 200nm 之间,多分散指数在 0.101 至 0.177 之间,表明粒径分布单分散。即使在 10000μg/ml 浓度下,NLC-PG 在蒸馏水中也没有显示出姜黄素的沉淀或重结晶,表明其溶解度显著提高。TEM 图像显示纳米颗粒呈单分散状态,具有多层核/壳结构。X 射线衍射和傅里叶变换红外光谱表明,姜黄素在 NLC-PG 中为无定形,姜黄素与赋形剂之间没有相互作用。使用模拟胃/肠液介质的体外释放研究表明,NLC-PG 中姜黄素的释放速率(J)随脂质载体中人参皂苷含量的增加而增加。此外,在存在脂肪酶的情况下,姜黄素的 J 逐渐增加,而在存在粘蛋白酶的情况下,J 急剧增加,直到人参皂苷含量达到 9.09%,随后趋于平稳。部分水解人参皂苷增加了载有姜黄素的 NLC-PG 中姜黄素的 J,因此可能有助于提高姜黄素的生物利用度。

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