Objective: In the present investigation, amino acid coupled liposome bearing dopamine-HCl were prepared to deliver drug to the brain utilizing receptor-mediated transcytosis for effective management of parkinsonism.

Background: Parkinson is a Neurodegenerative disease in which there is dopamine deficiency in Basal ganglia. The delivery of drug and sustaining it in effective concentration in brain is challenging due to blood brain barrier (BBB).

Methods: L-lysine stearylamine conjugate (LSC) was synthesized & LSC coupled liposomes bearing dopamine HCl was prepared by lipid cast film method. Formulations were analyzed for average vesicle size measured through Laser diffraction particle analyser (CILAS 1064 L, France), shape through Transmission Electron Microscopy, drug entrapment determined using Sephadex G- 75 minicolumn centrifugation method, in-vitro drug release and in-vivo efficacy of the formulations was assessed by measuring the reduction in the degree of drug induced catatonia in albino rats.

Results: Average particle size was found in the range of 1.92-0.80 mm. There was increase in the size for coupled liposomes due to the inclusion of LSC in liposomal bilayers. The percent encapsulation efficiency decreased from 46.82±2.17% in uncoupled to 38.13±1.18% in coupled liposomes. The in-vitro drug release after 24hrs was 58.9±2.94% with uncoupled while the coupled liposomes showed 43.7±2.18% drug release. The lower value for coupled formulation could be due to the retardation of drug release caused due to the incorporation of LSC in the liposomal bilayers, which enhanced the structural integrity of the bilayer. In-vivo study reveals that the animals receiving uncoupled liposomes showed partial reduction and animals that received coupled liposomes showed almost complete reduction in catatonia.

Conclusions: Fluoresence study clearly indicates the uptake of 6-CF in blood vessels and accumulated in brain. This could be due to enhanced uptake of Lysine coupled liposomes through amino acid transporters present at BBB surface.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/carrier-mediated-delivery-system-bearing-dopamine-for-effective-management-of-parkinsonism-2/