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学科主题: 药学
题名:
N-octyl-N-arginine-chitosan (OACS) micelles for gambogic acid oral delivery: preparation, characterization and its study on in situ intestinal perfusion
作者: Yu, Fan1,2; He, Chenghua1; Waddad, Ayman Y.1; Munyendo, Were L. L.1; Lv, Huixia1; Zhou, Jianping1; Zhang, Qiang3
关键词: Absorption enhancer ; arginine ; gambogic acid ; micelle ; N-octyl-N-arginine-chitosan
刊名: DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
发表日期: 2014-06-01
DOI: 10.3109/03639045.2013.786723
卷: 40, 期:6, 页:774-782
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: RAT ; NANOPARTICLES ; PERMEABILITY ; ABSORPTION ; DRUG ; DERIVATIVES ; CANCER ; MODEL
英文摘要:

Context: Gambogic acid (GA) can inhibit the growth of various cancer cells. However, the low bioavailability caused by insolubility, limits its clinical application. L-arginine is always used with GA to form a complex to obtain the higher solubility. Moreover, guanidyl group from arginine, which can facilitate the cellular uptake, was identified.

Objective: In this study, L-arginine and chitosan (CS) were used for the first time to prepare N-octyl-N-arginine CS (OACS), a novel amphiphilic carrier for GA with solubility- and absorption-enhancing functions; the characterization of the GA loaded OACS micelles (GA-OACS) and its absorption-enhancing effect were also investigated.

Materials and methods: GA-OACS were prepared by the dialysis method. The formed micelles were characterized and evaluated by atomic force microscope (AFM), dynamic light scattering, differential scanning calorimeter (DSC), solubility test, in vitro release and in situ intestinal perfusion.

Results: The GA-OACS micelles were successfully prepared attaining a 35.3% drug loading and 82.2% entrapment efficiency. GA-OACS had a homogeneous particle size of 160.3 nm; +21.8 mv zeta potential with smooth continuous surface was observed by using AFM. DSC diagram suggested that GA was encapsulated in the micelles. Meanwhile, GA encapsulated in micelles exhibited a desirable slow release in vitro experiment. The solubility of GA in OACS micelles was increased up to 3.16 +/- 0.13 mg/mL, 2320 times than that of free GA. The single pass perfusion showed that the absorption of GA-OACS micelles was enhanced 3.6-fold, 2.1-fold and 2.2-fold for jejunum, ileum and colon, respectively.

Discussion and conclusion: OACS provided excellent ability of drug loading, increasing solubility and enhanced absorption for GA, which indicated that OACS micelles as an oral drug delivery carrier may have potential research and application values.

语种: 英语
所属项目编号: 30973649 ; 30901867 ; 81102817 ; 81202929 ; 81273469 ; 20090096110002 ; 20110096110005 ; CX10B-373 Z ; JKQ2011016 ; 2009CB903300
项目资助者: National Natural Science Foundation of China ; Research Fund for the Doctoral Program of Higher Education of China ; National Basic Research Program of China ; Fundamental Research Funds for the Central University ; National Basic Research Program of China (973 Program)
WOS记录号: WOS:000336447100010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64912
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.China Pharmaceut Univ, Dept Pharmaceut, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
2.Yancheng Teachers Univ, Coll Pharm, Yancheng, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China

Recommended Citation:
Yu, Fan,He, Chenghua,Waddad, Ayman Y.,et al. N-octyl-N-arginine-chitosan (OACS) micelles for gambogic acid oral delivery: preparation, characterization and its study on in situ intestinal perfusion[J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,2014,40(6):774-782.
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