Cross-linked chitosan microspheres for oral delivery of insulin: Taguchi design and in vivo testing

被引:84
作者
Jose, S. [2 ]
Fangueiro, J. F. [1 ]
Smitha, J. [2 ]
Cinu, T. A. [2 ]
Chacko, A. J. [2 ]
Premaletha, K. [3 ]
Souto, E. B. [1 ,4 ]
机构
[1] Fernando Pessoa Univ, Fac Hlth Sci, P-4200150 Oporto, Portugal
[2] Mahatma Gandhi Univ, Dept Pharmaceut Sci, Ettumanoor 686631, Kerala, India
[3] Pariyaram Med Coll, Acad Pharmaceut Sci, Kannur, Kerala, India
[4] Univ Tras Os Montes & Alto Douro CGB UTAD IBB, Inst Biotechnol & Bioengn, Ctr Genom & Biotechnol, P-5001801 Vila Real, Portugal
关键词
Chitosan; Cross-linking; Factorial design; Insulin; Microspheres; Taguchi design; PHTHALATE MICROSPHERES; OPTIMIZATION; CHALLENGES; LIPOSOMES; SYSTEMS; TYPE-1; VITRO;
D O I
10.1016/j.colsurfb.2011.11.040
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
Insulin-loaded chitosan microspheres were engineered by emulsion cross-linking method using glutaraldehyde as cross-linker. Taguchi orthogonal method was applied to optimize the production time and reduce the number of experiments required to obtain an optimized formulation. Three variables were evaluated, i.e. chitosan and glutaraldehyde concentrations, and cross-linking time at three levels. The dependent variables were the mean particle size and the encapsulation efficiency. The optimal formulation was obtained with chitosan 3% (w/v), glutaraldehyde 3.5% (v/v), and cross-linking time of 5 h, characterized by microspheres with a mean particle size of 29.5 mu m, and insulin encapsulation efficiency of 71.6 +/- 1.3%. In vivo studies were carried out using male Wistar albino rats, revealing a significant reduction in blood glucose level after administration of the optimized formulation, in comparison to a subcutaneous insulin injection. Chitosan microspheres were superior in terms of sustaining protein release over conventional insulin therapy. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:175 / 179
页数:5
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