Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

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.

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

“…The thermogram of the liposome physical mixture shows a sharp melting endotherm centered at 146.5 • C, which is probably due to anthralin melting endotherm. This downward shift in anthralin melting is probably due to lipid melting prior to the drug leading to drug solubilization and rapid melting [57]. Anthralin-loaded liposome thermogram shows endothermic peaks at 139.6 and 173.1 • C attributed, respectively to the melting of cholesterol and anthralin.…”

“…The thermogram of anthralin-loaded ethosomes shows the disappearance of the drug melting peak ( Figure 2B). Change of the position or disappearance of the drug and/or excipients thermal events is often suggestive of interactions between various components of a certain delivery system [31,57]. However, in the case of anthralin liposomes and ethosomes there were changes in the drug melting in the physical mixture, as well as in liposomes and ethosomes.…”

“…The FT-IR spectrum of anthralin shows characteristic bands for OH bending and C=O stretching at 1633 cm −1 , C-C stretching, OH bending and CH bending at 1615 cm −1 , C-C stretching, C=O stretching and OH bending at 1598 cm −1 [58]. The spectrum of PL-90G shows C-H stretching bands at 2925 cm -1 and 2854 cm −1 , a stretching band of Change of the position or disappearance of the drug and/or excipients thermal events is often suggestive of interactions between various components of a certain delivery system [31,57]. However, in the case of anthralin liposomes and ethosomes there were changes in the drug melting in the physical mixture, as well as in liposomes and ethosomes.…”

“…This model is used to describe drug release from spherical matrices with an emphasis on nanoparticle shape in controlling the drug release process [66]. Our previous studies showed that the release of another hydrophobic drug, spironolactone from liposomes and liposomes dispersed in methylcellulose gel was best described by the Baker-Lonsdale model [57]. Liposome PL-127 gel had the highest R 2 for the Higuchi model indicating that the drug release process was controlled by diffusion.…”

Foray into Concepts of Design and Evaluation of Microemulsions as a Modern Approach for Topical Applications in Acne Pathology

“…The lipidic envelope will surround a hydrophilic core, resulting in spherical vesicles [ 144 ]. For the rest of vesicular systems above mentioned, structural differences are specific considering the presence of non-ionic surfactants [ 145 ], cathionic surfactants [ 146 ], alcohols [ 147 , 148 ], terpenes [ 148 ] or amphiphilic lipids [ 149 ] beside phospholipids and/or cholesterol found in liposomes. The possibility to entrap hydrophilic or lipophilic substances is considered an advantage that led to multiple designs of anti-acne formulations.…”