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学科主题: 药学
题名:
Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy
作者: 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
发表日期: 2014-09-01
DOI: 10.1517/17425247.2014.924503
卷: 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
所属项目编号: 062/2013/A2 ; SRG025-ICMS13-CMW ; MYRG2014-00033-ICMS-QRCM ; MYRG 208 (Y3-L4)-ICMS11-WYT ; MRG004/CMW/2014/ICMS ; K20130213
项目资助者: Macao Science and Technology Development Fund ; University of Macau ; State Key Laboratory of Natural and Biomimetic Drugs
WOS记录号: WOS:000340770300004
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56391
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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