Low Molecular Weight Chitosan-Insulin Complexes Solubilized in a Mixture of Self-Assembled Labrosol and Plurol Oleaque and Their Glucose Reduction Activity in Rats

• Main Authors: Amani M. Elsayed, Aseel H. Khaled, Mayyas M. Al Remawi, Nidal A. Qinna, Hussam Abu Farsakh, Adnan A. Badwan
• Format: Article
• Language: English
• Published: MDPI AG 2018-01-01
• Series: Marine Drugs
• Subjects: chitosan; insulin; oral; solubilization
• Online Access: http://www.mdpi.com/1660-3397/16/1/32

Oral insulin delivery that better mimics physiological pathways is a necessity as it ensures patient comfort and compliance. A system which is based on a vehicle of nano order where positively charged chitosan interacts with negatively charged insulin and forms a polyelectrolyte complex (PEC) solubilizate, which is then solubilized into an oily phase of oleic acid, labrasol, and plurol oleaque-protects insulin against enzymatic gastrointestinal reduction. The use of an anionic fatty acid in the oily phase, such as oleic acid, is thought to allow an interaction with cationic chitosan, hence reducing particle size. Formulations were assessed based on their hypoglycaemic capacities in diabetic rats as compared to conventional subcutaneous dosage forms. 50 IU/kg oral insulin strength could only induce blood glucose reduction equivalent to that of 5 IU/kg (1 International unit = 0.0347 mg of human insulin). Parameters that influence the pharmacological availability were evaluated. A preliminary investigation of the mechanism of absorption suggests the involvement of the lymphatic route.