Tocopheryl phosphate mixture TPM as a novel lipi

Authors: Paul D Gavin Mahmoud ElTamimy Hooi Hong Keah Ben J Boyd

Publish Date: 2016/09/26

Volume: 7, Issue: 1, Pages: 53-65

PDF Link

Abstract

Transdermal drug delivery is a useful route of administration that avoids firstpass metabolism and more invasive delivery options However many drugs require enhancers to enable sufficient drug absorption to reach therapeutic effect Alphatocopheryl phosphate TP and dialphatocopheryl phosphate T2P are two phosphorylated forms of vitamin E which form tocopheryl phosphate mixture TPM when combined and have been proposed to enhance the dermal and transdermal delivery of actives of interest Here we report the physicochemical characteristics and morphological properties of TPM formulations including particle size deformability and morphology and its ability to facilitate the transport of carnosine vitamin D3 CoEnzyme Q10 and caffeine into and across the skin Results demonstrate that TPM selfassembles to form vesicular structures in hydroethanolic solutions ranging in mean size from 101 to 162 nM depending on the amount of TPM and ethanol present in the formulation The ratio of TP to T2P in TPM formulations altered vesicle size and elasticity with vesicles high in TP found to be more deformable than those rich in T2P TPM produced a significant p  005 24–34fold increase in the absorption of carnosine vitamin D3 CoEnzyme Q10 and caffeine into or through the skin The TPM delivery platform was able to deliver a diverse range of actives with differing size and solubility profiles and therefore has significant potential to expand the number and types of drugs available for topical application and transdermal deliveryWe thank Dr Nicholas Kennedy Mr Giacinto Gaetano and Dr Billie Nikolovski for the conduct of in vitro permeation studies and Ms Gisela Ramirez and Mr Mathew Parsons for the conduct of HPLC analysis Lynne Waddington CSIRO Australia is also thanked for the provision of cryoTEM services

Keywords: