Assessing Topical Bioavailability and Bioequivalence: A Comparison of the In vitro Permeation Test and the Vasoconstrictor Assay

2014 ◽  
Vol 31 (12) ◽  
pp. 3529-3537 ◽  
Author(s):  
Paul A. Lehman ◽  
Thomas J. Franz
2021 ◽  
Vol 14 (12) ◽  
pp. 1233
Author(s):  
Quoc Lam Vu ◽  
Chih-Wun Fang ◽  
Muhammad Suhail ◽  
Pao-Chu Wu

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm2·h up to 20.00 μg/cm2·h and 4.90 up to 53.52 μg/cm2, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.


Materials ◽  
2021 ◽  
Vol 14 (21) ◽  
pp. 6678
Author(s):  
Joanna Klebeko ◽  
Paula Ossowicz-Rupniewska ◽  
Anna Nowak ◽  
Ewa Janus ◽  
Wiktoria Duchnik ◽  
...  

This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel® had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel® formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 μg IBU cm−2, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 μg IBU cm−2. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system.


2019 ◽  
Vol 1 (1) ◽  
Author(s):  
Rugun Clara Samosir ◽  
Iyan Sopyan ◽  
Dolih Gozali

Permeation is a measurable profile in drug penetration in skin. Adding increasing permeation substance (enhancer) in drug formulation is an important thing in pharmaceutical and toxicology in nowadays. The purpose of this research was to evaluate the effect of sesame oil, soybean oil, and oleic acid as enhancer in ketoprofen gel permeation. Six formula were prepared by varying concentration of sesame oil, soybean oil, and oleic acid respectively 5% and 10% and one blank, without enhancer. Permeation test was evaluated by in vitro permeation test using Franz diffusion cell method and shed snake skin of reticulated python as a membrane. Permeation test were carried out for 6 hours. The result showed that sesame oil, soybean oil, and oleic acid were able to increase ketoprofen permeation. B1 formula that contain 5% sesame oil had greatest percent permeation after 6 hours is 5.913%, while blank that contain no enhancer is 0.623%.Keywords: ketoprofen, permeation, enhancer, soybean oil, sesame oil, oleic acid.


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