Abstract
One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin.
Highlights
IntroductionThe growing interest in transdermal drug delivery may be ascribed to advantageous features such as easy accessibility, non-invasiveness, prevention from hepatic first-pass metabolism, minimal toxic side effects, and high patient compliance [1,2]
Values equal to 2.5 mg/mL and 2.0 mg/mL, respectively. We investigated their possible application as permeation enhancers for transdermal delivery of a model drug, i.e., hydrocortisone (HC)
The surface-activity, and the critical micellar concentration (CMC) of biosurfactants were determined in a saline solution
Summary
The growing interest in transdermal drug delivery may be ascribed to advantageous features such as easy accessibility, non-invasiveness, prevention from hepatic first-pass metabolism, minimal toxic side effects, and high patient compliance [1,2]. Efficient permeation of therapeutic compounds through the skin is still challenging because of its anatomy, which has evolved to impede the flux of toxins into the body and to minimize water loss. The skin naturally represents a barrier for the penetration of foreign molecules. The outermost layer of the skin, known as the stratum corneum (SC), is mainly responsible for this barrier function and consists of a lipid-rich matrix with embedded nonviable, anucleate, and keratinized cells (keratinocytes). Lipid molecules in the SC, e.g., ceramides, cholesterol, and fatty acids, play a major role in controlling the permeation of chemical and biological drugs [3]
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