Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne

Abstract

Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (−1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris. Graphical abstract

Indonesian Mangrove Sonneratia caseolaris Leaves Ethanol Extract Is a Potential Super Antioxidant and Anti Methicillin-Resistant Staphylococcus aureus Drug

“…Several examples known to have an overlap in strong antioxidant activity and potential for antibacterial activity against S. aureus or anti-MRSAs are the phenolic compounds aspirin and azelaic acid. Both compounds were reported to exhibit low anti-MRSA activity compared to antibiotics; however, when used together they synergistically support other antimicrobial and antibiotic compounds [ 50 , 51 ].…”

Essential Oils in the Treatment of Various Types of Acne—A Review

“…It is usually used in various topical preparations. It contains over 80–90% of monoterpenes, including terpinen-4-ol, p-cymene, α-terpinene, 1,8-cineole, limonene, α-terpineol, terpinolene, sabinene and α-pinene [ 20 , 28 , 29 ]. Furthermore, it exhibits antioxidant, anti-inflammatory, analgesic, and anticancer activity [ 20 ].…”

Medical Applications of Hydrogels in Skin Infections: A Review

“…By introduction of the ME system, AzA-and TTO-loaded ME hydrogels could have a better zone of inhibition and low minimum inhibitory concentration (MIC) values against pathogens such as S. aureus, S. epidermidis, and P. acnes. 13 In addition, chitosan-based hydrogel might be a potential approach for acne treatment in combination with photodynamic therapy (PDT). 14 Figure 1 shows the detailed mechanisms underlying the possible medical applications of hydrogels in skin infections.…”

“…19,20 It is essential to co-administer AZA and TTO for reducing the risk of dose-responsive adverse effects and achieving synergistic effects. Bisht et al 13 combined AZA and TTO for co-delivery in the form of a microemulsion (ME) system with hydrogel. As drug delivery systems, MEs offer unique advantages such as a better drug-release profile and increased skin permeation and targeting.…”