Preparation and Characterization of Multicomponent Particles for Controlled and Tunable Release of Citicoline

Abstract

Background: Memory disorders require a steady-state balance of choline and cytidine. Citicoline is prescribed as an exogenous source of choline and cytidine. Objective: The present study proposes a mucoadhesive multiparticulate sustained delivery of citico-line as a supportive control for memory loss. Methods: The formulation of citicoline sodium microparticles was done by ionotropic gelation method using alginate and hydroxypropyl methylcellulose (HPMC) in three different ratios. The three formulations were preliminary evaluated for the in vitro drug release study. Depending on their release pattern, a simplex lattice mixture design of 21 trial runs, with a set of possible combi-nations of each component of the three formulations, was employed to get an optimized ratio that could attend a predetermined release of drug at 1st, 4th, 6th, and 8th h. The optimized product was characterized for physicochemical evaluation, thermal analysis, in vitro drug release, surface mor-phology, and stability study. Results: Optimization of the design yielded a ratio that could prolong the release as predicted by design. The release mechanism followed non-Fickian diffusion. Differential thermal analysis exhib-ited high drug entrapment in the microparticles. Surface morphology studies revealed that drug re-lease took place by the formation of channels. Stability studies indicated there was no change in the properties even after six months and the moisture retention was meagre. Conclusion: The employed simplex lattice design could be successfully used to make microparti-cles of predetermined release characteristics with a steady-state release of the drug and can be a promising approach to provide an affordable therapy of citicoline to improve its effectivity.