Liposomal Citalopram HBr for Targeted Brain Delivery.

摘要

The efficacy and ability of Central Nervous System (CNS) acting medications are limited to cross the blood brain barrier (BBB); therefore, the challenge is in designing delivery systems targeted to cross the BBB. Toward this objective, the current study proposed pegylated Citalopram hydrobromide (Cit-HBr) liposomes coated with N-acetyl glucosamine (NAG) as a targeting moiety. The multicomponent liposomes were evaluated for drug encapsulation, vesicular size, size distribution, conductivity and drug release characteristics. Moreover, the interaction among the employed components was evaluated by FTIR, DSC and XRD analysis. Through a systematic screening design of formulation and process variables in the optimization phase, an improvement of Cit-HBr loading, fine vesicular size with narrow size distribution, greater stability and sustained release features were achieved.. The compatibility studies unveiled a significant interaction between Cit-HBr and dicetylphosphate to control drug encapsulation and release properties. The optimization process showed a minimal range of design space to achieve the preset desirability; more precisely, dicetyl phosphate, polyethylene glycol, NAG, and freeze-thaw cycles of 3%, 5%, 4%, and 2 cycles, respectively, were used. Thus, the current study has proposed an optimized pegylated and glycosylated vector as a starting point for the biological internalization, targeting ability and cytotoxicity study.