The Effect and Mechanism of Transdermal Penetration Enhancement of Fu’s Cupping Therapy: A New Physical Penetration Technology for Transdermal Administration with TCM Characteristics

Background: in this paper, a new physical penetration technology for transdermal administration with traditional Chinese medicine (TCM) characteristics Fu’s cupping therapy (FCT) was established and studied by in-vitro and in-vivo experiments; the penetration effect and mechanism of FCT physical penetration technology (FCT-PPT) was preliminarily discussed. Method: Indomethacin (IM) as a model drug,by transdermal in vitro tests the establishment of the high,medium and low reference were finished as the chemical permeation system; chemical penetration enhancers and iontophoresis as a reference, the percutaneous penetration effect of FCT for IM patch was evaluated with 7 species diffusion kinetics model and in vitro drug distribution;naproxen as an internal standard,using UPLC-MS/MS technology , the IM quantitative analysis method in vivo was established , and pharmacokinetic parameters (AUC0-t,AUC0-∞,AUMC0-t,AUMC0-∞, Cmax and MRT) as indicators were used evaluate to FCT penetration role in vivo;in the same time,the group used 3K factorial design to study joint synergistic penetration effect on FCT and chemical penetration enhancers (CPEs);by SEM and TEM,the skin micro and ultrastructural changes of the stratum corneum (SC) surface were observed, to explore pay tank penetration mechanism. Results: In vitro and in-vivo skin permeation experiments revealed that both the total cumulative percutaneous amount and in-vivo percutaneous absorption amount (AUC and AUMC) of indomethacin that permeated SD mouse skin using FCT techniques were greater than the amount observed using CPE and iontophoresis: Firstly, in contrast to the control group, the indomethacin percutaneous rate (PR) of the FCT lower group (FCTL) was 35.52%, and the enhancement ratio (ER) at 9h was 1.76X, which was roughly equivalent to the penetration enhancing effect of the CPEs and iontophoresis; secondly, the indomethacin PR of the FCT middle (FCTM) group and the FCT high intensity group (FCTH) were Preprints (www.preprints.org) | NOT PEER-REVIEWED | Posted: 15 December 2016 doi:10.20944/preprints201612.0082.v1