Transnasal nimodipine-loaded mucoadhesive nanoliposomes: Preparation and in-vitro evaluation

Abstract

Background and objective: Nimodipineis effective in the treatment of various cerebrovascular impairment, but its clinical potential is limited due to several undesirable characteristics such as low bioavailability which caused by first pass effect in the liver and low aqueous solubility. The main purpose of this study was to prepare nimodipine-loaded nanoliposomes for intranasal delivery and performing in-vitro studies. Methods: The nimodipine loaded nanoliposome formula was prepared by ethanol-based proliposome method and characterized in term of particle size and size distribution, zeta potential, entrapment efficiency, and permeability studies. In addition, mucoadhesive nanoliposomes loaded nimodipine was prepared using chitosan as a mucoadhesive agent. Results: The in-vitro studies explored particle size increased (122.48nm±0.002) for chitosan coated formulation after sonication in comparison to non-coated formulations (114.09 nm ± 0.025). Also, the zeta potential was positive for the sonicated chitosan-coated formulation (5.286 mV ±0.341) while for non-coated formulations with chitosan were found to be negative (-1.317 mV ± 0.153). The entrapment efficiency (76.033 % ± 0.094 %) and drug permeability (2.53 μg/ml in the duration of 240 min) were significant for chitosan-coated liposome compared to other formulations. Conclusion: This study concludes that chitosan glutamate (PROTASAN® UPG213)coatednimodipine-loaded liposomes can be considered as a promising novel formulation for an efficient intranasal delivery of nimodipine. Additionally, changes in the size of liposomes and zeta potential confirmed the existence of a coating layer on the surface of liposome pellets. Chitosan was found to significantly enhance the drug entrapment and could also be considered as a permeability enhancer.