Usach Iris, Martínez-Álvarez Paula, Peris José-Esteban
Department of Pharmacy and Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Avda. V. Andrés Estellés, s/n, 46100 Burjassot, Valencia, Spain.
Department of Pharmacy and Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Avda. V. Andrés Estellés, s/n, 46100 Burjassot, Valencia, Spain.
Int J Pharm. 2023 Sep 25;644:123287. doi: 10.1016/j.ijpharm.2023.123287. Epub 2023 Aug 2.
WHO classified Candida albicans as one of the four critical priority fungi for public health worldwide in 2022. Conventional topical formulations commercially available for the treatment of cutaneous candidiasis are associated with low drug bioavailability at the infection site and the lack of a sustained therapeutic effect. The main objectives of this work were to develop new topical administration systems of clotrimazole (CLT) and study the influence of surfactants on the antifungal inhibitory efficacy. Therefore, the minimum concentration of CLT required to inhibit 50 % of growth (MIC) was determined, obtaining a value of approximately 15 ng/mL. A non-ionic emulsion type 1, Beeler base cream, hydrogel and liposomes containing CLT were designed, prepared, characterized and their antifungal activity against C. albicans was tested. CLT loaded liposomes were small in size (102 nm), homogeneous (polydispersity index = 0.3) and uncharged (+0.07 mV), showing higher antifungal activity against C. albicans than that of the commercially available cream Canesten®. Furthermore, the antifungal activity of CLT was reduced in combination with surfactants such as Tween-80/Span-80 or Brij-S10. Sodium lauryl sulphate showed a fungicidal effect that disappeared when formulated as part of the Beeler base cream.
2022年,世界卫生组织将白色念珠菌列为全球公共卫生领域四大关键优先真菌之一。目前市售的用于治疗皮肤念珠菌病的传统局部用制剂在感染部位的药物生物利用度较低,且缺乏持续的治疗效果。这项工作的主要目的是开发克霉唑(CLT)的新型局部给药系统,并研究表面活性剂对其抗真菌抑制效果的影响。因此,测定了抑制50%生长所需的CLT最低浓度(MIC),得出的值约为15 ng/mL。设计、制备、表征了含CLT的非离子型1型乳剂、比勒基础乳膏、水凝胶和脂质体,并测试了它们对白色念珠菌的抗真菌活性。载有CLT的脂质体尺寸小(102 nm)、均匀(多分散指数 = 0.3)且不带电(+0.07 mV),对白色念珠菌的抗真菌活性高于市售的Canesten®乳膏。此外,CLT与吐温80/司盘80或Brij-S10等表面活性剂联合使用时,其抗真菌活性降低。月桂醇硫酸酯钠表现出杀菌作用,但当作为比勒基础乳膏的一部分配制时,这种作用消失了。