Abstract
Applying Ethosomal Gels (EGs) in transdermal drug delivery systems has evoked considerable interest because of their good water-solubility and biocompatibility. However, there has not been an explicit description of applying EGs as a vehicle for hypertrophic scars treatment. Here, a novel transdermal EGs loaded with 5-fluorouracil (5-FU EGs) was successfully prepared and characterized. The stability assay in vitro revealed that 5-FU EGs stored for a period of 30 days at 4 ± 1 °C had a better size stability than that at 25 ± 1 °C. Furthermore, using confocal laser scanning microscopy, EGs labeled with Rhodamine 6 G penetrated into the deep dermis of the hypertrophic scar within 24 h in the rabbit ear hypertrophic model suggested that the EGs were an optional delivery carrier through scar tissues. In addition, the value of the Scar Elevation Index (SEI) of 5-FU EGs group in the rabbit ear scar model was lower than that of 5-FU Phosphate Buffered Saline gel and Control groups. To conclude, these results suggest that EGs delivery system loaded 5-fluorouracil is a perfect candidate drug for hypertrophic scars therapy in future.
Highlights
Compared to normal skin, hypertrophic scars (HS) have different tissue composition that lacks mature corneocytes, and this leads to stratum corneum barrier dysfunction [1,2]
Our experiments have shown that 5-FU Ethosomal Gels (EGs), stored at 4 ± 1 °C, after 30 days still have good size stability
This provides a feasible condition for hypertrophic scar treatment in the rabbit ear model
Summary
Hypertrophic scars (HS) have different tissue composition that lacks mature corneocytes, and this leads to stratum corneum barrier dysfunction [1,2]. An ethosome is a novel lipid carrier, recently developed by Touitou et al, that exhibits enhanced skin delivery of drugs and with low cytotoxicity in vitro and in vivo studies [8,9,10,11,12]. Gel formulation is defined as a substantially diluted cross-linked system, which exhibits no flow when in the steady-state [16] It is a dispersion of molecules of a liquid within a solid created by the cross-linking of each other to constitute a three-dimensional cross-linked network. Gel formulation has become one of the most relevant routes for treating skin diseases efficaciously [17] It is of practical significance using percutaneous drug delivery and transdermal absorption in clinics. Their therapeutic effects for hypertrophic scar tissues were further evaluated by the rabbit ear hypertrophic scar model
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