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负载α-硫辛酸的纳米结构脂质载体:体外对HaCaT细胞的缓释及生物相容性

Alpha-lipoic acid-loaded nanostructured lipid carrier: sustained release and biocompatibility to HaCaT cells in vitro.

作者信息

Wang Jianmin, Xia Qiang

机构信息

School of Biological Science and Medical Engineering, State Key Laboratory of Bioelectronics, Southeast University , Nanjing , China and.

出版信息

Drug Deliv. 2014 Aug;21(5):328-41. doi: 10.3109/10717544.2013.846435. Epub 2013 Oct 21.

Abstract

ALA-loaded nanostructured lipid carrier (ALA-NLC) was designed to improve physicochemical stability and water solubility, and promote sustained release of ALA as well as determine the biocompatibility of ALA-NLC. The ALA-NLC manufactured using hot high-pressure homogenization technique was investigated in terms of size, zeta potential, FTIR analysis and release behavior. In vitro cytotoxicity and biocompatibility were determined by incubating with HaCaT cells using the MTT assay, HE staining and Hoechst 33342 staining. Cell behavior and cellular division of HaCaT cells untreated and treated by ALA-NLC were investigated in real-time images gathered using time-lapse imaging system. The release investigation illustrated that only 6.9% of ALA released in 30 min from ALA-NLC formation, whereas it was 30.3% in free ALA system. ALA-NLC possessed a satisfactory release behavior of sustained release up to 72 h. It showed that ALA-NLC did not exert hazardous effect on HaCaT cells up to 81.9 mg/L without morphological alterations, revealing a satisfactory biocompatibility. Evidence was provided from time-lapse imaging system that cell behavior and cellular division of ALA-NLC treated HaCaT cells were in accordance with the control. These results of this investigation demonstrated that NLC encapsulated ALA formation (ALA-NLC) can improve stability, solubility and release of ALA; ALA-NLC was biocompatible to HaCaT cells.

摘要

负载α-亚麻酸(ALA)的纳米结构脂质载体(ALA-NLC)旨在提高其物理化学稳定性和水溶性,促进ALA的持续释放,并确定ALA-NLC的生物相容性。对采用热高压均质技术制备的ALA-NLC进行了粒径、zeta电位、傅里叶变换红外光谱(FTIR)分析及释放行为研究。通过MTT法、苏木精-伊红(HE)染色和Hoechst 33342染色,与HaCaT细胞共孵育来测定体外细胞毒性和生物相容性。利用延时成像系统采集的实时图像,研究了未处理及经ALA-NLC处理的HaCaT细胞的细胞行为和细胞分裂情况。释放研究表明,ALA-NLC形成后30分钟内只有6.9%的ALA释放,而游离ALA体系中这一比例为30.3%。ALA-NLC具有长达72小时的令人满意的持续释放行为。结果表明,在高达81.9 mg/L时,ALA-NLC对HaCaT细胞未产生有害影响,且无形态改变,显示出良好的生物相容性。延时成像系统提供的证据表明,经ALA-NLC处理的HaCaT细胞的细胞行为和细胞分裂与对照组一致。本研究的这些结果表明,NLC包裹的ALA制剂(ALA-NLC)可提高ALA的稳定性、溶解性和释放率;ALA-NLC对HaCaT细胞具有生物相容性。

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