Monday, June 16, 2008
Room 1 (McKimmon Conference Center)
193

Cationic Chitosan/ Poly (D, L-lactide-co-glycolide) Particles for Improved Oral Delivery of Alpha-Tocopherol

Abitha Murugeshu and Cristina M. Sabliov. Louisiana State University, Baton Rouge, LA

This project aims to increase bioavailability and bioaccessibility of lipophilic vitamins in the human body by entrapping the vitamins in mucoadhesive cationic poly (D, L- Lactide-co-glycolide) (PLGA)/chitosan particles. Entrapping the bioactive vitamins in a lecithin stabilized polymeric matrix, of well characterized release kinetics, ensures that the vitamin is released from the matrix and becomes available for absorption, thus, increasing its bioaccessibility. Chitosan induces particle attachment to mucus tissue (mucoadhesion) and increases retention time of vitamins in the gastrointestinal tract, close to the absorptive cells to ensure an increase in the bioavailability. Mucoadhesive particle systems are desired for oral delivery because they decrease translocation of the particles into the cells by elimination of the particles during mucus turnover. This will ensure reduced toxicity from by-products of degradation. For added safety, the major reagents used in the synthesis are Food and Drug Administration (FDA) approved as generally regarded as safe (GRAS)for food or pharmaceutical uses such as lecithin, ethyl acetate, and PLGA. The objectives of the research were: 1. To synthesize and characterize 16% w/w α-tocopherol entrapped PLGA/chitosan particles stabilized by lecithin, and 2. To study the release profile of α-tocopherol from the PLGA/chitosan particles in simulated intestinal environment, as a function of size and charge. Mucoadhesive cationic particle system consisting of PLGA, chitosan and lecithin were synthesized by emulsion evaporation method. Morphology, size, size distribution, and zeta potential were measured by Transmission Electron Microscopy (TEM) and Dynamic Light Scattering (DLS). Stable spherical particles ranging from 113.3 nm to 640 nm in diameter were synthesized, with surface charges ranging between -45.9 and +56.4 mV, as a result of different lecithin:chitosan ratios. The polydispersity of the samples varied from 0.50 to 0.17 and the entrapment efficiency was greater than 90 %. The release profile showed a burst release followed by a constant release, similar to what was reported in the literature for similar systems. Future studies involve in-vivo animal model studies to confirm the improved vitamin uptake from the mucoadhesive PLGA/Chitosan particle system developed herein.