Abstract
Spironolactone (SP), an aldosterone antagonist with anti-androgen properties, has shown promising results in the treatment of female acne. However, its systemic side effects limit its clinical benefits. This study aimed to prepare and evaluate LeciPlexes for SP topical delivery. LeciPlexes were prepared by a one-step procedure and characterized using various techniques. Optimum LeciPlex preparation was incorporated into 1% methylcellulose gel and SP permeability was tested ex vivo in Sprague-Dawley rat skin. The maximum drug encapsulation efficiency obtained was 93.6 ± 6.9% and was dependent on the drug/phospholipid and surfactant/phospholipid ratios. A zeta potential of +49.3 ± 3.5 to +57.7 ± 3.3 mV and a size of 108 ± 25.3 to 668.5 ± 120.3 nm were observed for the LeciPlexes. FT-IR and DSC studies confirmed the incorporation of SP into the LeciPlexes through hydrophobic and hydrogen bonding interactions. SP release from the LeciPlex formulations was significantly slower than from the drug suspension. Cumulative SP permeated through rat skin from LeciPlex gel was about 2-fold higher than SP control gel. Cumulative SP deposited in the stratum corneum and other skin layers from the LeciPlex gel was about 1.8- and 2.6-fold higher than SP control gel, respectively. This new SP LeciPlex formulation is a promising carrier for the treatment of female acne.
Highlights
Acne vulgaris is a highly prevalent chronic inflammatory condition of the skin affecting more than 80% of teenagers [1]
The cumulative SP amounts deposited in the stratum corneum and other skin layers from the LeciPlex gel were about 1.8- and 2.6-fold higher than that from SP
Fourier transform infrared (FT-IR) and Differential Scanning Calorimetry (DSC) studies confirmed the incorporation of the drug into the LeciPlexes through hydrophobic and hydrogen-bonding interactions
Summary
Acne vulgaris is a highly prevalent chronic inflammatory condition of the skin affecting more than 80% of teenagers [1]. Acne is classified by The Global Burden of Disease Study as the eighth most prevalent disease worldwide and the third most prevalent dermatological condition affecting about 10% of the global population [4,5]. It can persist beyond the age of 25 years, especially in women [2,6]. The pathoetiology of acne is associated with factors that cause changes in the natural skin barrier functions and microorganisms, leading to hyperseborrhea, changed keratinization of the pilosebaceous duct, loss of the skin microbial variety, and inflammation [8]. Increased sebum productions stimulates follicular hyperkeratinization, leading to microcomedo [10]
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