Poly(N-vinylcaprolactam-co-methacrylic acid) hydrogel microparticles for oral insulin delivery

被引:78
作者
Mundargi, Raghavendra C. [1 ]
Rangaswamy, Vidhya [1 ]
Aminabhavi, Tejraj M. [1 ]
机构
[1] Reliance Life Sci Pvt Ltd, Ind Biotechnol Grp, Dhirubhai Ambani Life Sci Ctr, Rabale 400701, Navi Mumbai, India
关键词
Methacrylic acid; vinylcaprolactam; oral delivery; insulin; hydrogel; COMPLEXATION POLYMER HYDROGELS; IN-VITRO; DRUG-DELIVERY; NANOPARTICLES; CHITOSAN; BEHAVIOR;
D O I
10.3109/02652048.2011.576782
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
pH-sensitive copolymeric hydrogels prepared from N-vinylcaprolactam and methacrylic acid monomers by free radical polymerization offered 52% encapsulation efficiency and evaluated for oral delivery of human insulin. The in vitro experiments performed on insulin-loaded microparticles in pH 1.2 media (stomach condition) demonstrated no release of insulin in the first 2 h, but almost 100% insulin was released in pH 7.4 media (intestinal condition) in 6 h. The carrier was characterized by Fourier transform infrared, differential scanning calorimeter, thermogravimetry and nuclear magnetic resonance techniques to confirm the formation of copolymer, while scanning electron microscopy was used to assess the morphology of hydrogel microparticles. The in vivo experiments on alloxan-induced diabetic rats showed the biological inhibition up to 50% and glucose tolerance tests exhibited 44% inhibition. The formulations of this study are the promising carriers for oral delivery of insulin.
引用
收藏
页码:384 / 394
页数:11
相关论文
共 36 条
[31]   pH- and thermo-responsive properties of poly(N-vinylcaprolactam-co-acrylic acid) copolymers [J].
Shtanko, NI ;
Lequieu, W ;
Goethals, EJ ;
Du Prez, FE .
POLYMER INTERNATIONAL, 2003, 52 (10) :1605-1610
[32]   Modification of psyllium polysaccharides for use in oral insulin delivery [J].
Singh, Baljit ;
Chauhan, Nirmala .
FOOD HYDROCOLLOIDS, 2009, 23 (03) :928-935
[33]   Bioadhesive Hydrophobic Chitosan Microparticles for Oral Delivery of Insulin: In Vitro Characterization and In Vivo Uptake Studies [J].
Sonia, T. A. ;
Rekha, M. R. ;
Sharma, Chandra P. .
JOURNAL OF APPLIED POLYMER SCIENCE, 2011, 119 (05) :2902-2910
[34]   The use of charge-coupled polymeric microparticles and micromagnets for modulating the bioavailability of orally delivered macromolecules [J].
Teply, Benjamin A. ;
Tong, Rong ;
Jeong, Seok Y. ;
Luther, Gaurav ;
Sherifi, Ines ;
Yim, Christopher H. ;
Khademhosseini, Ali ;
Farokhzad, Omid C. ;
Langer, Robert S. ;
Cheng, Jianjun .
BIOMATERIALS, 2008, 29 (09) :1216-1223
[35]   Complexation hydrogels for oral insulin delivery: Effects of polymer dosing on in vivo efficacy [J].
Tuesca, Anthony ;
Nakamura, Koji ;
Morishita, Mariko ;
Joseph, Jeffrey ;
Peppas, Nicholas ;
Lowman, Anthony .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 97 (07) :2607-2618
[36]  
VARSHOSAZ J, 2007, IMMUNE DRUG DISCOV, V1, P25