粉防已碱纳米醇质体的制备、表征和抗关节炎疗效

doi:10.5246/jcps.2012.04.042

粉防已碱纳米醇质体的制备、表征和抗关节炎疗效

范超, 李馨儒, 周艳霞, 赵勇, 李文静, 马淑金, 刘艳^*, 李桂玲, 李眉

1. 北京大学医学部药学院药剂学系, 北京 100191
2. 中国医学科学院北京协和医学院医药生物技术研究所制剂室, 北京 100050

收稿日期:2012-03-23 修回日期:2012-05-20 出版日期:2012-06-25 发布日期:2012-06-25
通讯作者: 刘艳*

Preparation and characterization of nanosized ethosomes loaded with tetrandrine and their in vivo efficacy in arthritis treatment

Chao Fan, Xin-Ru Li, Yan-Xia Zhou, Yong Zhao, Wen-Jing Li, Shu-Jin Ma, Yan Liu^*, Gui-Ling Li, Mei Li

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
2. Institute of Medicinal Biotechnology, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China

Received:2012-03-23 Revised:2012-05-20 Online:2012-06-25 Published:2012-06-25
Contact: Yan Liu*

摘要/Abstract

摘要： 本研究旨在探索醇质体用于改善粉防己碱局部给药治疗关节炎的可行性。用pH梯度法制备醇质体, 并对其粒径、形态和包封率进行表征。所制备的粉防己碱醇质体为球形, 平均粒径约为78 nm, 包封率为 (52.87±3.81)%。而粉防己碱脂质体具有较大的粒径 (99 nm) 和较高的包封率 (98.80±0.01)%。此外, 与粉防己碱脂质体相比, 粉防己碱醇质体显示出显著的体外透皮性能和抗大鼠关节炎疗效, 并与市售地塞米松软膏的疗效无显著性差异。结果表明, 醇质体有望成为粉防己碱皮肤局部给药的纳米载体。

关键词: 粉防己碱, 醇质体, 脂质体, 抗关节炎疗效

Abstract:

The purpose of this work was to explore the feasibility of ethosomes for improving the anti-arthritic efficacy of topically administered tetrandrine, a bisbenzylisoquinoline alkaloid. Ethosomes were prepared by using the transmembrane pH-gradient loading method and characterized by mean diameter, morphology and entrapment efficiency. The prepared tetrandrine-loaded ethosomes exhibited spherical shape with about 78 nm of average diameter and entrapment efficiency of (52.87±3.81)%, whereas the liposomes had bigger size (99 nm) and higher entrapment efficiency (98.80±0.01)%. In addition, ethosomes exhibited favorable and enhanced penetration behavior as compared with liposomes. More importantly, tetrandrine-loaded ethosomes had a significantly better anti-adjuvant arthritis efficacy in rats compared to liposomes formulation, but no significant difference in the anti-arthritic efficacy between tetrandrine-loaded ethosomes and commercial dexamethasone ointment was observed. These results suggest that ethosomes would be a promising nanocarrier for topical delivery of tetrandrine across skin.

Key words: Tetrandrine, Ethosomes, Liposomes, Anti-arthritic efficacy

中图分类号:

R943

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 81172990), National Development of Significant New Drugs of China (New Preparation and New Technology, Grant No. 2009zx09310-001), National Key Science Research Program of China (973 Program, Grant No. 2009CB930300) and Innovation Team of Ministry of Education (Grant No. BMU20110263).
^*Corresponding author. Tel.: 86-10-82801508

范超, 李馨儒, 周艳霞, 赵勇, 李文静, 马淑金, 刘艳^*, 李桂玲, 李眉. 粉防已碱纳米醇质体的制备、表征和抗关节炎疗效[J]. , DOI: 10.5246/jcps.2012.04.042.

Chao Fan, Xin-Ru Li, Yan-Xia Zhou, Yong Zhao, Wen-Jing Li, Shu-Jin Ma, Yan Liu^*, Gui-Ling Li, Mei Li. Preparation and characterization of nanosized ethosomes loaded with tetrandrine and their in vivo efficacy in arthritis treatment[J]. , DOI: 10.5246/jcps.2012.04.042.

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