School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Solan, India, 173 212.
School of Applied Sciences and Biotechnology, Shoolini University of Biotechnology and Management Sciences, Solan, Himachal Pradesh, India.
Drug Deliv Transl Res. 2022 Oct;12(10):2501-2517. doi: 10.1007/s13346-021-01092-4. Epub 2021 Nov 15.
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.
壬二酸（AzA）是一种美国食品药品监督管理局批准的用于治疗寻常痤疮的生物活性药物。它具有一些挑战，如水溶性差、皮肤渗透性低以及剂量依赖性副作用，这些问题可以通过与茶树油（TTO）协同组合为微乳液（ME）-水凝胶复合体制剂来克服。AzA-TTO ME 是通过伪三元相图构建来制备的。最佳的 AzA-TTO ME 具有均匀的粒径（多分散指数<0.7）、纳米级（~357.4±2%nm）、高透光率（>90%）和负的 Zeta 电位（-1.42±0.25%mV）。与市售制剂（Aziderm™）相比，具有最佳流变学和质构特性的 ME 水凝胶复合体制剂在 Wistar 大鼠皮肤中的渗透、保留和皮肤顺应性方面表现更好。通过琼脂平板扩散和肉汤稀释试验评估了在细菌菌株，即金黄色葡萄球菌、痤疮丙酸杆菌和表皮葡萄球菌中的体外抗菌效果。ME 水凝胶在抑制 P. acnes 方面表现出了两倍的抑菌圈增加和八倍的最小抑菌浓度（MIC）降低，与 AzA 相比。最后，与 Aziderm™（72.69±4.67%）相比，ME 水凝胶复合体制剂在诱导睾酮引起的大鼠痤疮中显示出更好的丘疹密度降低（93.75±1.64%）。因此，所开发的 AzA-TTO ME 水凝胶复合体制剂有望成为治疗寻常痤疮的有效且相对更安全的局部给药系统。
