Developing ultra deformable vesicular transportation of a bioactive alkaloid in pursuit of vitiligo therapy

Abstract

ObjectiveTo develop transfersomal formulation integrated with piperine intended for vitiligo. MethodsFilm hydration technique was employed in the preparation of transfersomes. Modified diffusion cell, consistency tester were fabricated for ex vivo diffusion studies and spreadability studies respectively while tape stripping method was integrated with tissue extraction in the determination of tissue drug concentration. ResultsWhen film hydration technique was used for, ultradeformable vesicles (transfersomes) of piperine in soabean phosphatidylcholine was formed with (67.11±0.22) to (70.55±3.62) and (60.12±1.04) to (80.43±0.14) mean size (μ) and entrapment efficiency (%) respectively. Transfersomes are capable of crossing the pores in permeability barriers extremely efficient even if the transfersome radius (tr) is much greater than the pore size (rpore) ie., tr/rpore⩾ 0.25 the driven flux rate depends on the transdermal osmotic gradient. The vesicles describes elasto-mechanical character of vesicles while penetrating through the pores. The proviso is that the vesicular membrane elasticity is dynamically to the local stress by the external. Diffusion and Spreadability studies showed maximum diffusion when the lipid was kept minimum. Tape stripping and tissue extraction method for the tissue drug retention showed that (75.25±1.72)% drug was retained in the dermis. ConclusionSpan 80 was preferred over tween 80 in terms of dermal retention. Size and encapsulation was slightly altered by phosphatidylcholine concentration. The kinetics, efficiency and the transfersome mediated transport can be tailored for trans-epidermal, deep tissues and systemic depending on the vesicular composition, dose and form. Thus we have offered a successful drug delivery of piperine targeting the deep epidermis.