title: VB12-coated Gel-Core-SLN containing insulin: Another way to improve oral absorption.
abstract: To improve the oral absorption of insulin, a novel carrier of Vitamin B12 (VB12) gel core solid lipid nanopaticles (Gel-Core-SLN, GCSLN) was designed with a gel core, lipid matrix and VB12-coated surface. VB12-stearate was synthesized and characterized by infrared spectroscopy (IR), nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS). Sol-gel conversion following ultrasonic heating and double emulsion technology were combined to implant the insulin-containing gel into solid lipid nanoparticles (SLN). The influence of the mode of administration, food, the amount of VB12-stearate and the particle size on the oral absorption of insulin incorporated in the VB12-GCSLN was investigated. The determined partition coefficient (LogP) of VB12-stearate in a dichloromethane (DCM)-water system was 3.4. This new structure of VB12-GCSLN had higher insulin encapsulation efficiency (EE) of 55.9%, a lower burst release of less than 10% in the first 2h. In vivo studies demonstrated that stronger absorption of insulin with a relative pharmacological availability (PA) of 9.31% compared with the normal insulin-loaded SLN and GCSLN and fairly stable blood glucose levels up to 12h were maintained without any sharp fluctuations. This study suggests that VB12-GCSLN containing insulin appears to be a promising nano carrier for oral delivery of biomacromolecules with relatively high pharmacological availability.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Puxiu
authors.initials: P
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Cuifang
authors.initials: C
authors.lastname: Cai
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Rui
authors.initials: R
authors.lastname: Yang
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D065546:Drug Liberation; D005782:Gels; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D007408:Intestinal Absorption; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D010316:Particle Size; D017207:Rats, Sprague-Dawley; D013229:Stearic Acids / Q000737:chemistry; D014805:Vitamin B 12 / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D001786:Blood Glucose; D005782:Gels; D007004:Hypoglycemic Agents; D007328:Insulin; D013229:Stearic Acids; C031183:stearic acid; D014805:Vitamin B 12
keywords: Double emulsion technology; Gel-Core-SLN; Insulin; Oral Absorption; Vitamin B(12)