Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

Abstract

Knowledge of the mechanism of action of skin penetration enhancers is essential to formulators for optimizing formulations and to maximize the efficacy of enhancers. To obtain information about the effects of penetration enhancers as a fast initial screening, investigations have been performed to identify possible correlations of the biological effectiveness of penetration enhancers with their interaction with a well-defined model system consisting of skin mimic lipid bilayers, as determined by calcein release experiments using stratum corneum lipid liposomes (SCLLs). We aimed to investigate the enhancing effects of different concentrations of two chemical penetration enhancers, Kolliphor RH40 and Transcutol on SCLLs. The results obtained by SCLL-based techniques were compared with conventional ex vivo penetration studies in case of Kolliphor RH40 to evaluate the potential of SCLLs as an alternative tool for screening various types and concentrations of penetration enhancers. As a result, calcein leakage assay performed with SCLL was considered to be a good model for the skin penetration enhancing effect. This method could be used as a time-saving and sensitive alternative in vitro screening technique in the early stage of the development of dermal formulations.

Membrane disruption of Fusarium oxysporum f. sp. niveum induced by myriocin from Bacillus amyloliquefaciens LZN01

“…Then, 20 µl of 10% Triton X‐100 (pH 7.4) was added into the mixture at 12 min to determine the maximum fluorescence intensity of 100% calcein leakage. The percentage of calcein leakage induced by myriocin was calculated according to the equation calcein leakage (%) = 100 × ( F – F 0 )/( F t – F 0 ), where F represents the fluorescence intensity acquired after the addition of myriocin, and F 0 and F t represent the fluorescence intensities without myriocin and with Triton X‐100 respectively (Bakonyi et al ., 2018). The statistical data are presented as mean ± standard deviation of three replicates.…”

Current Advances in Lipid Nanosystems Intended for Topical and Transdermal Drug Delivery Applications

“…Despite much investigation into the mechanism of transport of drugs loaded into liposomes, it remains a much-debated concept. Liposomes offer enhanced skin penetration by the following mechanisms: (i) intact vesicular skin permeation, (ii) acting as a penetration enhancer, inducing changes in the stratum corneum’s constituents, structure, and thermodynamic characteristics, (iii) adsorption of liposomes made of skin-like lipids such as ceramides and free fatty acids and (iv) enhanced transport through the transappendageal route guided by particle size of liposomes [ 99 , 100 , 101 , 102 , 103 , 104 , 105 , 106 , 107 ].…”

Biomimetic Stratum Corneum Liposome Models: Lamellar Organization and Permeability Studies

“…We vary chain length, degree of unsaturation, and head group architecture of the CERs and FFAs and assess the sensitivity of the SCLL models when challenged with membrane perturbing agent (Triton X-100). The composition we used for all the SCLLs in this study is based on an established SCLL model with a mixture of CERs (40%), FFA (25%), cholesterol (25%), and cholesteryl sulfate (10%) [ 46 , 47 , 48 , 49 , 50 ]. This lipid composition forms large unilamellar liposomes that are known to be structurally stable at physiological pH [ 48 , 49 , 50 ].…”