Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2486351 | Journal of Pharmaceutical Sciences | 2011 | 8 Pages |
Abstract
Entrapping inclusion complexes in liposomes has been proposed to increase the entrapment efficiency (EE) and stability of liposomes compared with conventional liposomes. In the present study, a stable honokiolâinâhydroxypropylâβâcyclodextrinâinâliposome (honokiolâinâHPâβâCDâinâliposome) was developed as honokiol delivery system by a novel method. The final molar ratio of honokiol/HPâβâCD/lipid was selected as 1:2:2. The mean particle size was 123.5 nm, the zeta potential was â25.6 mV, and the EE was 91.09 ± 2.76%. The release profile in vitro demonstrated that honokiol is released from honokiolâinâHPâβâCDâinâliposome with a sustained and slow speed. Crystallographic study indicated that honokiol was first bound within HPâβâCD and then the inclusion complex was encapsulated within liposomes. HonokiolâinâHPâβâCDâinâliposome without freeze dry kept stable for at least 6 months at 4°C. Pharmacokinetic study revealed that honokiolâinâHPâβâCDâinâliposome significantly retarded the elimination and prolonged the residence time in circulating system. The data of bioactivity showed that honokiolâinâHPâβâCDâinâliposome remained similar antiproliferative activity in A549 and HepG2 tumor cells compared to free honokiol. These results suggested that we had successfully prepared honokiolâinâHPâβâCDâinâliposome. The novel honokiol formulation was easy to push industrialization forward and might be a potential carrier for honokiol delivery in tumor chemotherapy. © 2011 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 100:3357-3364, 2011
Keywords
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Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
Xianhuo Wang, Linyu Deng, Lulu Cai, Xiaoyan Zhang, Hao Zheng, Chongyang Deng, Xingmei Duan, Xia Zhao, Yuquan Wei, Lijuan Chen,