title: Solid lipid nanoparticles modified with stearic acid-octaarginine for oral administration of insulin.
abstract: The aim of this study was to design and characterize solid lipid nanoparticles (SLNs) modified with stearic acid-octaarginine (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 ± 0.79. These results demonstrate that SA-R₈-modified SLNs promote the oral absorption of insulin.
authors: Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China.
authors: Zhen-Hai
authors: ZH
authors: Zhang
authors: Yin-Long
authors: YL
authors: Zhang
authors: Jian-Ping
authors: JP
authors: Zhou
authors: Hui-Xia
authors: HX
authors: Lv
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy / Q000378:metabolism; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D006801:Humans; D007003:Hypoglycemia / Q000139:chemically induced; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry*; D051381:Rats; D013229:Stearic Acids / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D001786:Blood Glucose; D004337:Drug Carriers; D007328:Insulin; D009842:Oligopeptides; D013229:Stearic Acids; C448619:octaarginine; C031183:stearic acid