Preparation, Characterization, and Oral Delivery of Insulin Loaded Carboxylated Chitosan Grafted Poly(methyl methacrylate) Nanoparticles

被引：106

作者：

Cui, Fuying ^{[1
,2
]}

Qian, Feng ^{[1
,2
]}

Zhao, Ziming ^{[1
,2
]}

Yin, Lichen ^{[1
]}

Tang, Cui ^{[1
]}

Yin, Chunhua ^{[1
,2
]}

机构：

[1] Fudan Univ, State Key Lab Genet Engn, Dept Pharmaceut Sci, Sch Life Sci, Shanghai 200433, Peoples R China

[2] Fudan Univ, Dept Biochem, Sch Life Sci, Shanghai 200433, Peoples R China

来源：

BIOMACROMOLECULES | 2009年 / 10卷 / 05期

基金：

中国国家自然科学基金;

关键词：

PROTEIN DELIVERY; IN-VITRO; CARBOXYMETHYL CHITOSAN; INTESTINAL-ABSORPTION; DRUG; VIVO; COPOLYMERIZATION; LIPOSOMES; SYSTEMS; DESIGN;

D O I：

10.1021/bm900035u

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

To improve the efficiency of insulin via oral administration, pH-sensitive carboxylated chitosan grafted poly(methyl methacrylate) nanoparticles (CCGN) were prepared. CCGN were characterized by H-1 NMR, dynamic light scattering, zeta potential, and transmission electron microscopy, and the hypoglycemic effect of insulin loaded CCGN via the oral route was evaluated in normal and diabetic rats. CCGN exhibited a homogeneous morphology and a spherical shape with core-shell structure. They were aggregated in simulated gastric fluid while separated in simulated intestinal fluid. Insulin was mainly located in the shell of the CCGN via hydrogen bonding, electrostatic interaction, and Van der Waals force. Insulin release from the CCGN exhibited a pH-sensitive property in that it had a slow release rate at pH 2.0 and a fast release rate at pH 6.8 and 7.4. The pharmacological bioavailability after oral administration of insulin loaded CCGN at a dose of 25 IU/kg was found to be 9.7%. Besides, CCGN showed desirable tissue and blood compatibility. Therefore, the CCGN would be a promising delivery carrier for protein drugs via the oral route.

引用

页码：1253 / 1258

页数：6

共 27 条

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