Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement

2016 ◽  
Keyword(s):  
Penetration Enhancers ◽  
Percutaneous Penetration ◽  
Penetration Enhancement ◽  
Chemical Methods

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

2016 ◽  
Author(s):  
Wei-Jie Xie ◽  
Yong-Ping Zhang ◽  
Jian Xu ◽  
Xiao-Bo Sun ◽  
Fang-Fang Yang
Keyword(s):  
Cupping Therapy ◽  
Penetration Enhancers ◽  
Percutaneous Penetration ◽  
Control Group ◽  
Penetration Enhancement ◽  
Transdermal Administration ◽  
Significance Level ◽  
Penetration Effect

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 respectively 47.36% and 54.58%, ER at 9h were separately 3.58X and 8.39X; thirdly, pharmacokinetic studies showed that in-vivo indomethacin percutaneous absorption of the FCTs was higher than that of the control group, that of the FCTM group was slightly higher than that of the CPEs group, and that of the FCTM group was significantly higher than that of the others. Meanwhile, the variance analysis indicated that the combination of the FCT penetration enhancement method and the CPE method had beneficial effects in penetration enhancing of the skin: the significance level of the CPE method was 0.0004, which was apparently lower than the 0.001, meaning the difference was markedly significant; the significance level of the FCT was under 0.0001, its difference markedly significant; and the significance level of factor interaction A×B was lower than 0.0001, indicating that its difference of the synergism was markedly significant. Moreover, SEM and TEM images showed that the SC surfaces of SD rats treaded with FCT-PPT was damaged, and hard to observe the complete surface structure with its SC pores growing bigger and its special “brick structure” becoming looser, indicating that it broke the barrier function of skin, which revealed potentially a major route of skin penetration. Conclusion: FCT, as percutaneous penetration new technologies, has penetration effects significantly, with Chinese characteristics and highly clinical value, worth promoting development.

Percutaneous penetration enhancement activity of aromatic S,S-dimethyliminosulfuranes

1999 ◽  
Vol 187 (2) ◽  
pp. 219-229 ◽  
Author(s):  
N. Kim ◽  
M. El-Khalili ◽  
M.M. Henary ◽  
L. Strekowski ◽  
B.B. Michniak
Keyword(s):  
Percutaneous Penetration ◽  
Penetration Enhancement ◽  
Percutaneous Penetration Enhancement

scholarly journals Liposome percutaneous penetration in vivo

2017 ◽  
Vol 1 ◽  
pp. 239784731772319 ◽  
Author(s):  
A Lymberopoulos ◽  
C Demopoulou ◽  
M Kyriazi ◽  
MS Katsarou ◽  
N Demertzis ◽  
...  
Keyword(s):  
Stratum Corneum ◽  
Rhodamine B ◽  
Transdermal Delivery ◽  
Penetration Enhancers ◽  
Percutaneous Penetration ◽  
Hairless Mice ◽  
Liposomal Form ◽  
Multilamellar Vesicles ◽  
Small Unilamellar Vesicles

Objectives: Liposomes are reported as penetration enhancers for dermal and transdermal delivery. However, little is known about their percutaneous penetration and as to at which level they deliver encapsulated drugs. The penetration of multilamellar vesicles (MLVs) and small unilamellar vesicles (SUVs), in comparison to one of their lipid components, was investigated. Methods: Using the fluorescent lipid, Lissamine Rhodamine B-PE (R), as a constituent, MLV and SUV liposomes were prepared, tested, and R, MLV, or SUV were applied in vivo on the back of hairless mice. Absorption of each was evaluated at the levels of stratum corneum, living skin, and blood by fluorometry. Results: Penetration of the lipid R in stratum corneum in the nonliposomal form exceeded that in the liposomal form and only R penetrates the living skin in a statistically significant manner. No statistical significant absorption into blood was observed with either form. Conclusions: Liposomes size did not play an important role in penetration to stratum corneum. The lipid constituent in the nonliposomal form penetrated at higher rates into stratum corneum and living skin. Even though these liposomes entered stratum corneum, they were not significantly absorbed into viable skin or blood.

Classification of percutaneous penetration enhancers: A conceptional diagram

1990 ◽  
Vol 42 (1) ◽  
pp. 71-72 ◽  
Author(s):  
Mitsuhiko Hori ◽  
Susumu Satoh ◽  
Howard I. Maibach
Keyword(s):  
Penetration Enhancers ◽  
Percutaneous Penetration
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