齐墩果酸固体脂质纳米粒口服给药系统的制备与表征

doi:10.5246/jcps.2011.03.032

齐墩果酸固体脂质纳米粒口服给药系统的制备与表征

孙慧, 张现化, 王硕, 涂盈峰, 赵荣生^*, 谢英^*

1. 北京大学医学部药学院药剂学系, 北京 100191
2. 北京大学第三附属医院药剂科, 北京 100191
3. 瑞士巴塞尔大学药学院, 巴塞尔 CH-4056

收稿日期:2011-01-31 修回日期:2011-04-05 出版日期:2011-05-06 发布日期:2011-05-06
通讯作者: 赵荣生*, 谢英*

Preparation and characterization of oleanolic acid-loaded solid lipid
nanoparticles for oral administration

Hui Sun, Xian-Hua Zhang, Shuo Wang, Ying-Feng Tu, Rong-Sheng Zhao^*, Ying Xie^*

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
2. Departments of Pharmacy, Peking University Third Hospital, Beijing 100191, China
3. School of Pharmaceutics, Basel University, Basel CH-4056, Switzerland

Received:2011-01-31 Revised:2011-04-05 Online:2011-05-06 Published:2011-05-06
Contact: Rong-Sheng Zhao*, Ying Xie*

摘要/Abstract

摘要：

采用改良的乳化-溶剂挥发法制备齐墩果酸-固体脂质纳米粒(OA-SLNs) 并对其性质进行评价。其粒径, zeta电位, 包封率和载药率分别为(104.5±11.7) nm, (-25.5±1.8) mV, (94.2±3.9)%, 和(4.71±0.15)%。透射电子显微镜下, 可见球形实心纳米粒。X-粉末衍射和差示扫描量热 (DSC) 图谱证实药物分子均匀分散在脂质骨架中。体外释放实验表明, OA-SLNs以每小时4.88% 速率缓慢释放药物, 符合零级释放动力学模型。OA-SLNs在人工胃液和肠液中具有良好的稳定性。本文研究为OA-SLNs口服给药系统的应用进一步研究提供了可能。

关键词: 齐墩果酸, 固体脂质纳米粒, 制备, 表征

Abstract:

Oleanolic acid-loaded solid lipid nanoparticles (OA-SLNs) were prepared by using an improved emulsion-solvent evaporation method. The size, zeta potential, encapsulation efficiency, and loading efficiency of OA-SLNs were (104.5±11.7) nm, (-25.5±1.8) mV, (94.2±3.9)%, and (4.71±0.15)%, respectively. The morphology was illustrated by TEM as sphere stuffed particles. The XRD and DSC spectra confirmed that the OA molecules were dispersed uniformly into SLN matrixes. The results of in vitro release test suggested that OA was released slowly at a rate of 4.88% per hour from SLN preparation, which was consistent with the Zero-order Released Model. In addition, OA-SLNs were stable in artificial gastric juice and artificial intestinal juice. Together, our results provided new data for the potential application of OA-SLNs in oral administration.

Key words: Oleanolic acid, Solid lipid nanoparticles, Preparation, Characterization

中图分类号:

R943.4

Supporting:

Foundation items: National Basic Research Program of China (973 Program Grant No. 2009CB930300), National Integrity Innovational Technology Platform of New Drug and Research and Development (Grant No. 2009ZX09310-001).
^*Corresponding author. Tel.: 86-10-82801508 (Ying Xie); Tel.: 86-10-82266673 (Rong-Sheng Zhao)

孙慧, 张现化, 王硕, 涂盈峰, 赵荣生^*, 谢英^*. 齐墩果酸固体脂质纳米粒口服给药系统的制备与表征 [J]. , DOI: 10.5246/jcps.2011.03.032.

Hui Sun, Xian-Hua Zhang, Shuo Wang, Ying-Feng Tu, Rong-Sheng Zhao^*, Ying Xie^* . Preparation and characterization of oleanolic acid-loaded solid lipid
nanoparticles for oral administration [J]. , DOI: 10.5246/jcps.2011.03.032.

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