%0 Journal Article %T Solid lipid nanoparticles modified with stearic acid¨Coctaarginine for oral administration of insulin %A Zhang ZH %A Zhang YL %A Zhou JP %A Lv HX %J International Journal of Nanomedicine %D 2012 %I %R http://dx.doi.org/10.2147/IJN.S31711 %X lid lipid nanoparticles modified with stearic acid¨Coctaarginine for oral administration of insulin Original Research (2816) Total Article Views Authors: Zhang ZH, Zhang YL, Zhou JP, Lv HX Published Date July 2012 Volume 2012:7 Pages 3333 - 3339 DOI: http://dx.doi.org/10.2147/IJN.S31711 Received: 11 March 2012 Accepted: 05 April 2012 Published: 03 July 2012 Zhen-Hai Zhang,1,2 Yin-Long Zhang,2 Jian-Ping Zhou,2 Hui-Xia Lv2 1Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China; 2Department of Pharmaceutics, China Pharmaceutical University, Nanjing, China Abstract: The aim of this study was to design and characterize solid lipid nanoparticles (SLNs) modified with stearic acid¨Coctaarginine (SA-R8) as carriers for oral administration of insulin (SA-R8-Ins-SLNs). The SLNs were prepared by spontaneous emulsion solvent diffusion methods. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the SA-R8-Ins-SLNs were 162 nm, 29.87 mV, 3.19%, and 76.54%, respectively. The zeta potential of the SLNs changed dramatically, from -32.13 mV to 29.87 mV, by binding the positively charged SA-R8. Morphological studies of SA-R8-Ins-SLNs using transmission electron microscopy showed that they were spherical. In vitro, a degradation experiment by enzymes showed that SLNs and SA-R8 could partially protect insulin from proteolysis. Compared to the insulin solution, the SA-R8-Ins-SLNs increased the Caco-2 cell's internalization by up to 18.44 times. In the in vivo studies, a significant hypoglycemic effect in diabetic rats over controls was obtained, with a SA-R8-Ins-SLN pharmacological availability value of 13.86 ¡À 0.79. These results demonstrate that SA-R8-modified SLNs promote the oral absorption of insulin. %K solid lipid nanoparticles %K cell penetration peptides %K stearic acid octaarginine %K insulin %K oral administration %U https://www.dovepress.com/solid-lipid-nanoparticles-modified-with-stearic-acidndashoctaarginine--peer-reviewed-article-IJN