Abstract
The present research work was planned to formulate and characterize Thymoquinone (TMQ) loaded chitosan vesicle (CHVs) for the effective treatment of the liver disorder. The formulations were prepared using solvent evaporation and probe sonication method. The formulation (F3) with appropriate characteristics (size = 372.8 nm; zeta potential = 13.12 mV; encapsulation efficiency = 81.38 ± 3.85%; PDI = 0.192 ± 0.015) was selected as optimized thymoquinone chitosan vesicle (TMQCHVopt). The stability study results revealed the non-significant changes in vesicle size, PDI, and encapsulation efficiency. The formulation showed higher drug release (85.11% ± 4.12) and followed Higuchi release mechanism. TMQCHVopt showed significant enhancement in mucoadhesive property (4.4 times) and intestinal permeation (1.9 times) vis-a-vis TMQ suspension. The enhancement in permeation was further confirmed by CLSM study and result supports the permeation result. The pharmacodynamic results exhibited a significant (*P < 0.001) changes in all the parameters of liver function test in the serum biomarker enzymes (SGOT, SGPT, and ALP) and lipid profile (TC, LDL, HDL). The histopathology of liver treated with toxic control revealed inflammatory cells, ballooning of hepatocytes and portal tract representing the occurrence of hepatitis whereas TMQCHVopt treated showed minimal central vein inflammation. The novelty of the work lies in the successful formulation of thymoquinone loaded chitosan lipid vesicle for improved oral delivery. The overall data suggest that the developed formulation is a potential oral delivery system for the management of hyperlipidemia.
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•Thymoquinone chitosan vesicles (TMQCHVs) were prepared to get better therapeutic efficacy by enhancing the absorption.•Chitosan was used as mucoadhesive polymer to retain the TMQ chitosan vesicles for prolonged time in the intestine.•The optimized formulation has shown nano size, high drug encapsulation and release.•Enhanced permeation and mucoadhesive property was achieved.•TMQCHVopt showed better anti-hyperlipidemic efficacy than standard simvastatin.