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
[1]   Polymethyacrylate based microparticulates of insulin for oral delivery: Preparation and in vitro dissolution stability in the presence of enzyme inhibitors [J].
Agarwal, V ;
Reddy, IK ;
Khan, MA .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 225 (1-2) :31-39
[2]   Formation of new glucomannan-chitosan nanoparticles and study of their ability to associate and deliver proteins [J].
Alonso-Sande, Maria ;
Cuna, Margarita ;
Remunan-Lopez, Carmen .
MACROMOLECULES, 2006, 39 (12) :4152-4158
[3]  
Arbit Ehud, 2004, Diabetes Technol Ther, V6, P510, DOI 10.1089/1520915041705929
[4]   Developments in polymeric devices for oral insulin delivery [J].
Babu, V. Ramesh ;
Patel, Pradip ;
Mundargi, Raghavendra C. ;
Rangaswamy, Vidhya ;
Aminabhavi, Tejraj M. .
EXPERT OPINION ON DRUG DELIVERY, 2008, 5 (04) :403-415
[5]   Loading and mobility of spin-labeled insulin in physiologically responsive complexation hydrogels intended for oral administration [J].
Besheer, A ;
Wood, KM ;
Peppas, NA ;
Mäder, K .
JOURNAL OF CONTROLLED RELEASE, 2006, 111 (1-2) :73-80
[6]   In vivo characterization of a polymeric nanoparticle platform with potential oral drug delivery capabilities [J].
Bisht, Savita ;
Feldmann, Georg ;
Koorstra, Jan-Bart M. ;
Mullendore, Michael ;
Alvarez, Hector ;
Karikari, Collins ;
Rudek, Michelle A. ;
Lee, Carlton K. ;
Maitra, Amarnath ;
Maitra, Anirban .
MOLECULAR CANCER THERAPEUTICS, 2008, 7 (12) :3878-3888
[7]   Insulin-loaded calcium pectinate nanoparticles: Effects of pectin molecular weight and formulation pH [J].
Cheng, K ;
Lim, LY .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2004, 30 (04) :359-367
[8]   Oral delivery of insulin associated to polymeric nanoparticles in diabetic rats [J].
Damge, Christiane ;
Maincent, Philippe ;
Ubrich, Nathalie .
JOURNAL OF CONTROLLED RELEASE, 2007, 117 (02) :163-170
[9]   Development of acrylic-based copolymers for oral insulin delivery [J].
Foss, AC ;
Goto, T ;
Morishita, M ;
Peppas, NA .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2004, 57 (02) :163-169
[10]   Oral insulin delivery using nanoparticles based on microemulsions with different structure-types: Optimisation and in vivo evaluation [J].
Graf, Anja ;
Rades, Thomas ;
Hook, Sarah M. .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2009, 37 (01) :53-61