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Self-microemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice
Lu, Juan-Li1,4; Wang, Jian-Cheng1; Zhao, Shu-Xin1; Liu, Xiao-Yan5; Zhao, Hui1; Zhang, Xuan1; Zhou, Shu-Feng3; Zhang, Qiang1,2
关键词9-nitrocamptothecin Self-microemulsifying Drug Delivery System (Smedds) Pharmacokinetic Antitumor Activity
刊名EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
2008-08-01
DOI10.1016/j.ejpb.2008.02.023
69期:3页:899-907
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]PHASE-II ; BIOAVAILABILITY ; ABSORPTION ; FORMULATIONS ; FEASIBILITY ; ENHANCEMENT ; PACLITAXEL ; RUBITECAN ; DOGS
英文摘要

9-Nitrocamptothecin (9-NC) is an orally administered topoisomerase-I inhibitor for the treatment of pancreatic carcinoma, but its oral absorption and bioavailability are poor. The main objective Of this Study was to develop optimal 9-nitrocarriptothecin (9-NC) microemulsion prepared by self-microemulsifying drug delivery system (SMEDDS). Two SMEDDS formulations of 9-NC prepared from a mixture of ethyl oleate, Tween-80 (T-form) or Cremophor EL (C-form), and PEG-400/ethanol were formed as microemulsions under dilution with aqueous phase. The resulting microemulsions were evaluated in vitro and in vivo, including the kinetics and antitumor effects in SKOV-3 human ovarian cancer xenograft in nude mice. Following 1:10 aqueous dilution Of Optimal 9-NC SMEDDS, the droplet sizes of resulting microemulsions were (30.8 +/- 4.6) nm and (39.8 +/- 8.2) nm for SMEDDS T-Form and C-form, respectively. and the zeta potential values were -(4.3 +/- 0.5) mV and -(5.7 +/- 0.5) mV, respectively. In SKOV-3 cells, the growth inhibition (IC(50)) of various 9-NC formulations was greatest with SMEDDS T-form (3.5 +/- 0.7 nM) followed by SMEDDS C-form (4.6 +/- 0.4 nM). 9-NC solution (6.6 +/- 1.4 nM) and 9-NC suspension (26.0 +/- 2.9 nM) (P < 0.01). It was indicated that the area under the plasma concentration-time Curve (AUC(0 ->)8h) values of various formulations of 9-NC after oral administration ranked as the following sequence: SMEDDS T-form (360.12 +/- 19.44 ng h/ml) approximate to SMEDDS C-form (351.71 +/- 33.66 ng h/ml) > 9-NC solution (241.21 +/- 24.67 np h/ml) > 9-NC suspension (161.24 +/- 24.31 ng h/ml). The 9-NC SMEDDS formulations also produced significantly more tumor shrinkage (P < 0.01) when compared to 9-NC Suspension in nude mice bearing human ovarian cancer xenografts. The results suggest that SMEDDS is a promising drug delivery system to increase the oral bioavailability and antitumor effects of 9-NC and may be applied to other lipophilic drugs. 9-NC SMEDDS represents a novel 9-NC therapy for cancer patients. (C) 2008 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000258882200012
引用统计
被引频次:46[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52583
专题北京大学药学院_药剂学系
作者单位1.Gen Hosp Armed Police Force, Dept Pharm, Beijing, Peoples R China
2.Peking Univ, Dept Pharmaceut, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
4.RMIT Univ, Sch Hlth Sci, Div Chinese Med, Bundoora, Vic, Australia
5.Peking Univ, Dept Cellular Pharmacol, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
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Lu, Juan-Li,Wang, Jian-Cheng,Zhao, Shu-Xin,et al. Self-microemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice[J]. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,2008,69(3):899-907.
APA Lu, Juan-Li.,Wang, Jian-Cheng.,Zhao, Shu-Xin.,Liu, Xiao-Yan.,Zhao, Hui.,...&Zhang, Qiang.(2008).Self-microemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice.EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,69(3),899-907.
MLA Lu, Juan-Li,et al."Self-microemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice".EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 69.3(2008):899-907.
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