Β-榄香烯纳米聚合物胶束包封率、载药量及释药性测定

CJI (Traditional Chinese Medicine) - - Chinese Journal Of Information On Traditional Chin -

王静,李学涛,袁子民

辽宁中医药大学,辽宁 大连 116600

摘要:目的 建立 β-榄香烯纳米聚合物胶束包封率和载药量的RP-HPLC测定方法,并对其释药性进行考察。方法 以二硬脂酰磷脂酰乙醇胺-聚乙二醇 2000(DSPE-PEG2000)为载体材料制备载药胶束,采用石油醚萃取法测定包封率和载药量,采用透析法对其释药性进行研究。结果 所制备的 β-榄香烯纳米聚合物胶束平均包封率为 89.47%,平均载药量为 8.33%,体外释药缓慢。结论 包封率和载药量的测定简便、准确,所制得的胶束具有缓释作用。

关键词: β-榄香烯纳米聚合物胶束;包封率;载药量;释药性

DOI: 10.3969/j.issn.1005-5304.2017.02.023

中图分类号: R284.1 文献标识码: A 文章编号: 1005-5304(2017)02-0091-03

Determination of Encapsulation Efficiency and Medicine Loading and Release of β-elemene in β-elemene-loaded Nano Polymeric Micelles

WANG Jing, LI Xue-tao, YUAN Zi-min (Liaoning University of TCM, Dalian 116600, China)

Abstract: Objective To establish a RP-HPLC method for the determination of encapsulation efficiency (EE) and medicine loading (ML) in β-elemene-loaded Nano Polymeric Micelles; To study its release characteristic in vitro. Methods DSPE-PEG2000 was used as carrier to prepare medicine-loaded micelles. EE and ML were determined by petroleum ether extraction method, and its release characteristic in vitro was studied by dialysis method. Results The average EE and ML of β-elemene-loaded Nano Polymeric Micelles were 89.47% and 8.33%, respectively. Its release characteristic was slow. Conclusion The method for EE and ML determination is simple and accurate, and the prepared micelles have the property of sustained release.

Key words: β-elemene-loaded Nano Polymeric Micelles; encapsulation efficiency; medicine loading; release characteristic

榄香烯是临床常用的中药广谱抗肿瘤药物,该药及其脂质体注射液和口服乳制剂通过抗增殖和诱导凋亡作用,在体外及临床用于脑胶质瘤治疗方面取得

[1-3]了较好治疗效果,但也存在一定不良反应 。β-榄香烯是由榄香烯经精馏后去除 γ、δ-榄香烯异构体,得

[4]

到的抗癌单体有效成分 。为增加 β-榄香烯对血脑屏障的透过性及其载药制剂在肿瘤组织的通透和滞留增强效应,本课题组以二硬脂酰磷脂酰乙醇胺-聚乙二醇( DSPE-PEG2000)为载体材料,将其制成抗脑胶质瘤的新型脑靶向制剂,本研究对其包封率、载药量进行测定,并考察其体外释药性,为进一步控制本品质量、优化制备工艺及其应用提供依据。

1 仪器与试药

Agilent 1100 高效液相色谱仪(美国安捷伦公 基金项目:辽宁省科学技术计划(2015020703)通讯作者:袁子民,E-mail:yuanzmin@163.com

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