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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. 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*

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

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