期刊
JOURNAL OF NANOBIOTECHNOLOGY
卷 18, 期 1, 页码 -出版社
BMC
DOI: 10.1186/s12951-020-00662-x
关键词
Insulin; Oral delivery system; Colon targeting; Nano-carrier; Aminoclay
资金
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [2019R1A2C2004873, 2018R1A5A2023127]
- National Research Foundation of Korea [2019R1A2C2004873, 2018R1A5A2023127] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
This study aimed to develop a ternary nanocomposite system of organoclay, glycol-chitosan, and Eudragit(R)S100 as an effective colon targeted drug delivery carrier to enhance the oral absorption of insulin. A nanocomplex of insulin and aminoclay was prepared via spontaneous co-assembly, which was then coated with glycol-chitosan and Eudragit S(R)100 (EGAC-Ins). The double coated nanocomplex, EGAC-Ins demonstrated a high entrapment efficiency of greater than 90% and a pH-dependent drug release. The conformational stability of insulin entrapped in EGAC-Ins was effectively maintained in the presence of proteolytic enzymes. When compared to a free insulin solution, EGAC-Ins enhanced drug permeability by approximately sevenfold in Caco-2 cells and enhanced colonic drug absorption in rats. Accordingly, oral EGAC-Ins significantly reduced blood glucose levels in diabetic rats while the hypoglycemic effect of an oral insulin solution was negligible. In conclusion, EGAC-Ins should be a promising colonic delivery system for improving the oral absorption of insulin.
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