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学科主题: 药学
题名:
Increase of the pharmacological and pharmacokinetic efficacy of negatively charged polypeptide recombinant hirudin in rats via parenteral route by association with cationic liposomes
作者: Meng, Meng; Liu, Yu; Wang, Yi-Bo; Wang, Jian-Cheng; Zhang, Hua; Wang, Xue-Qing; Zhang, Xuan; Lu, Wan-Liang; Zhang, Qiang
关键词: recombinant hirudin ; cationic liposomes ; sustained release ; entrapment ; in vivo studies
刊名: JOURNAL OF CONTROLLED RELEASE
发表日期: 2008-06-04
DOI: 10.1016/j.jconrel.2008.03.001
卷: 128, 期:2, 页:113-119
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Chemistry ; Pharmacology & Pharmacy
关键词[WOS]: GENE-TRANSFER ; IN-VITRO ; PHASE-I ; DELIVERY ; PROTEIN ; CELLS ; COMPLEXES ; CARCINOMA ; INSULIN ; PHARMACODYNAMICS
英文摘要:

Two biodegradable cationic lipids, stearylamine and DC-Chol, were chosen to investigate the effect of cationic lipids on the in vitro and in vivo characteristics of hydrophilic proteins or peptides of low isoelectric point. Thrombin inhibitor recombinant hirudin variant-2 (rHV2) was selected as the model drug. The cationic lipids were found to achieve higher entrapment efficiency of rHV2 in liposomes than zwitterionic lipids. The positively charged liposomes became less positive and relatively stable in serum after loading rHV2. The cationic liposomes induced sustained release of rHV2 in the presence of plasma, significantly prolonged the antithrombotic efficacy and plasma level of rHV2 after intravenous injection in rats in comparison with neutral lipid liposomes, especially for stearylamine group. Both clotting times correlated well with plasma rHV2 levels. No serious adverse events were observed and physical state of rats was satisfactory for all the formulations. Electrostatic interaction between negative charge of rHV2 and cationic liposomes was confirmed and it might affect all the characteristics of rHV2 loaded cationic vehicles. The findings suggest that cationic liposomes may be a potential sustained-release delivery system for parenteral administration of hydrophilic proteins or peptides with low isoelectric point to prolong efficacy and improve bioavailability. (C) 2008 Elsevier B.V. All rights reserved.

语种: 英语
WOS记录号: WOS:000256955200002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60459
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Meng, Meng,Liu, Yu,Wang, Yi-Bo,et al. Increase of the pharmacological and pharmacokinetic efficacy of negatively charged polypeptide recombinant hirudin in rats via parenteral route by association with cationic liposomes[J]. JOURNAL OF CONTROLLED RELEASE,2008,128(2):113-119.
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