Edge activated ultradeformable liposomes of psoralen and its derivatives: Development and comparative evaluation for vitiligo therapy

Abstract

In present work, a comparative study was carried out to investigate the biological activity and effectiveness of parent compound psoralen (PSR) and its derivatives 5-methoxypsoralen (5-MOP) and 8-methoxypsoralen (8-MOP) in the form of ultradeformable liposomes (UDL) for improved drug delivery and therapeutic potential in vitiligo management. Undesirable side effects of PSR have led a path for the investigators to develop new PSR derivatives that are more tolerable and less phototoxic with good pigmentation capacity than PSR. UDL were prepared by thin film hydration method and ethanol injection method. UDL were characterized by dynamic light scattering, scanning electron microscopy, transmission electron microscopy and compared for their relative efficacy in mouse melanoma cell line (B16F10). Qualitative and quantitative cellular uptake studies revealed enhanced penetration of nanocarrier into cells. 5-MOP UDL showed enhanced stimulation of melanin and tyrosinase at low concentration compared to 8-MOP UDL, PSR UDL and control that were in agreement with Fontana-Masson silver staining results. Our experimental findings suggested that 5-MOP UDL followed by 8-MOP UDL revealed superior efficacy over PSR UDL and can serve as a promising approach for vitiligo. Efficacy of PSR derivatives at low dose can address the tolerability and safety issues in future.