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Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy
Zhang, Jinming1; Li, Yingbo2; Gao, Wei2; Repka, Michael A.3; Wang, Yitao1; Chen, Meiwan1
关键词Andrographolide Breast Cancer Mad-mb-231 Cells Micelles Pharmacokinetics Poly (d L-lactide-co-Glycolide)-b-poly (Ethylene Glycol)-b-poly (d L-lactide-co-glycolide) Triblock Copolymer
刊名EXPERT OPINION ON DRUG DELIVERY
2014-09-01
DOI10.1517/17425247.2014.924503
11期:9页:1367-1380
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]SOLID LIPID NANOPARTICLES ; BREAST-CANCER CELLS ; IN-VITRO ; DRUG-DELIVERY ; ORAL DELIVERY ; PANICULATA ; RELEASE ; VIVO ; PHARMACOKINETICS ; FORMULATIONS
英文摘要

Background: Andrographolide (ADG) isolated from Andrographis paniculata exhibits anti-inflammatory and anticancer activities, but high hydrophobicity and poor bioavailability greatly restricts its clinical application.

Objectives: In this study, ADG was encapsulated in a micelle formulation based on poly (D,L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly(D,L-lactide-co-glycolide) (PLGA-PEG- PLGA) amphiphilic triblock copolymers, in order to enhance the anticancer efficacy and bioavailability in vivo.

Methods: The physicochemical properties of the ADG-loaded PLGA-PEG-PLGA micelles were investigated for encapsulation efficiency, particle size, zeta potential and critical micelle concentration. These micelles were further evaluated for in vitro cytotoxicity, including proliferation inhibition, cell cycle arrest and pro-apoptosis effects against human breast cancer MAD-MB-231 cells, cellular uptake and pharmacokinetics study in rat.

Results: ADG-loaded PLGA-PEG-PLGA micelles had a high encapsulation and loading efficiency of about 92 and 8.4% (w/w), respectively, and a stable particle size of 124.3 +/- 6.4 nm. In vitro cytotoxicity testing demonstrated that ADG-loaded PLGA-PEG-PLGA micelles exhibited higher proliferation inhibition, cell cycle arrest at the G2/M phase and pro-apoptosis effects in MAD-MB-231 cells, which would be contributed to higher efficiency of cellular uptake and intracellular transport. Further, the plasma AUC((0 - infinity)) and mean resident time of ADG-loaded PLGA-PEG-PLGA micelles were increased by 2.7- and 2.5-fold, respectively, when compared to the raw suspension.

Conclusion: All of these investigations suggest that PLGA-PEG-PLGA micelles may be a potential drug delivery strategy for improving ADG bioavailability and efficacy in cancer therapy.

语种英语
WOS记录号WOS:000340770300004
项目编号062/2013/A2 ; SRG025-ICMS13-CMW ; MYRG2014-00033-ICMS-QRCM ; MYRG 208 (Y3-L4)-ICMS11-WYT ; MRG004/CMW/2014/ICMS ; K20130213
资助机构Macao Science and Technology Development Fund ; University of Macau ; State Key Laboratory of Natural and Biomimetic Drugs
引用统计
被引频次:17[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/400002259/56391
专题北京大学药学院
北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学第三临床医学院_心血管内科
作者单位1.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Taipa 999078, Macau, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
3.Univ Mississippi, Sch Pharm, Dept Pharmaceut & Drug Delivery, University, MS 38677 USA
推荐引用方式
GB/T 7714
Zhang, Jinming,Li, Yingbo,Gao, Wei,et al. Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy[J]. EXPERT OPINION ON DRUG DELIVERY,2014,11(9):1367-1380.
APA Zhang, Jinming,Li, Yingbo,Gao, Wei,Repka, Michael A.,Wang, Yitao,&Chen, Meiwan.(2014).Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy.EXPERT OPINION ON DRUG DELIVERY,11(9),1367-1380.
MLA Zhang, Jinming,et al."Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy".EXPERT OPINION ON DRUG DELIVERY 11.9(2014):1367-1380.
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