Paclitaxel-loaded elastic liposomes synthesised by microfluidics technique for enhance transdermal delivery

Abstract

AbstractThe inherent flexibility of elastic liposomes (EL) allows them to penetrate the small skin pores and reach the dermal region, making them an optimum candidate for topical drug delivery. Loading chemotherapy in ELs could improve chemotherapy’s topical delivery and localise its effect on skin carcinogenic tissues. Chemotherapy-loaded EL can overcome the limitations of conventional administration of chemotherapies and control the distribution to specific areas of the skin. In the current studies, Paclitaxel was utilised to develop Paclitaxel-loaded EL. As an alternative to the conventional manufacturing methods of EL, this study is one of the novel investigations utilising microfluidic systems to examine the potential to enhance and optimise the quality of Els by the microfluidics method. The primary aim was to achieve EL with a size of < 200 nm, high homogeneity, high encapsulation efficiency, and good stability. A phospholipid (DOPC) combined with neutral and anionic edge activators (Tween 80 and sodium taurocholate hydrate) at various lipid-to-edge activator ratios, was used for the manufacturing of the ELs. A preliminary study was performed to study the size, polydispersity (PDI), and stability to determine the optimum microfluidic parameters and lipid-to-edge activator for paclitaxel encapsulation. Furthermore, physiochemical characterisation was performed on the optimised Paclitaxel–loaded EL using a variety of methods, including Dynamic Light Scattering, Fourier Transform Infrared Spectroscopy, Atomic force microscopy, elasticity, encapsulation efficiency, and In vitro release. The results reveal the microfluidics’ significant impact in enhancing the EL characteristics of EL, especially small and controllable size, Low PDI, and high encapsulation efficiency. Moreover, the edge activator type and concentration highly affect the EL characteristics. The Tween 80 formulations with optimised concentration provide the most suitable size and higher encapsulation efficiency. The release profile of the formulations showed more immediate release from the EL with higher edge activator concentration and a higher % of the released dug from the Tween 80 formulations. Graphical Abstract