Liposome-Based Mucoadhesive Formulations for Oral Delivery of Macromolecules

Abstract

The design and evaluation of liposome-based mucoadhesive dosage form containing mucoadhesive polymers (e.g., chitosan, pectin, carbopol, and PVA-R) have been described. Liposomes with different compositions were prepared and surface-modified by various polymers. The surface coating or complexation of liposomes was confirmed by monitoring the changes in surface charge before and after surface modification. The mucoadhesion of the liposome-based formulations has been examined both in vitro and in vivo. Using CLSM, the penetration of polymer-coated liposomes or polymer–liposome complexes into a layer of mucus in the rats after oral administration was confirmed. The pharmacological action of the macromolecular drugs (e.g., insulin and calcitonin) was observed after oral administration. In most cases, the polymer-coated liposomes and/or polymer–liposome complexes showed superior pharmacological action compared to other systems without mucoadhesive polymers.