Study of Polymer Nanofilms Using for High-Throughput Screening in the Development of Transdermal Therapeutic System

Abstract

We investigated polymer nanofilm (PNF) for use in high-throughput screening (HTS) to promote the development of transdermal therapeutic systems (TTS). The drug permeability of PNF with a 1 : 1 weight mix ratio of poly(L-lactic acid) (PLLA) and poly(methylhydrosiloxane) (PMHS) (PLLA/PMHS (1/1) PNF) and Strat-M^® of the transdermal diffusion test membrane, was evaluated using 12 kinds of drugs with the logarithmic value of n-octanol/water partition coefficients of −4.70 to 3.86. The lag time of PLLA/PMHS (1/1) PNF made via polymer alloying was significantly shorter than that of Strat-M^® for 10 drug types, and the formation of a highly diffusible PMHS-rich phase accompanying the formation of a sea–island structure was suggested as a contributing factor. Additionally, a high correlation was confirmed between the measured value for the logarithm of the apparent permeability coefficient of PLLA/PMHS (1/1) PNF and the literature values for the logarithm of the apparent permeability coefficient of human skin (r = 0.929). This study shows that PLLA/PMHS (1/1) PNF can reliably predict drug permeability in human skin and can potentially be used in HTS for developing TTS.