Pharmacy and Pharmaceutical Technology Deparment, Biopharmaceutical and Pharmacokinetics Unit, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
J Pharm Sci. 2012 Oct;101(10):3739-52. doi: 10.1002/jps.23249. Epub 2012 Jul 6.
Oral candidosis is a common opportunistic infection in patients suffering from mucositis (after chemotherapy and radiotherapy administration) and must be treated to prevent infecting other tissue. Nystatin (Nys) is one of the most prescribed drugs to treat this pathology, but because of its physicochemical properties, its pharmaceutical-technological requirements make it a challenge. The purpose of this work was the development and characterization of an optimal Nys delivery system for the potential treatment of oral candidosis avoiding undesirable side effects and toxicity of potential systemic absorption. A nanoemulsion was developed, evaluated, and characterized. It has been formulated successfully as a stable nanoemulsion with a droplet size of 138 nm. Release parameters were estimated using different mathematical approaches, and from the results of ex vivo permeation study of Nys through porcine buccal mucosa, it could be hypothesized that no systemic effects would happen. Microbiologic studies performed revealed an enhanced antifungal effect of the Nys-loaded nanoemulsion. Also, the evaluation of the treated buccal mucosa ultrastructure by transmission electron microscopy revealed a harmless effect. Thus, it could be inferred that the developed formulation could be potentially utilized for candidosis infection under mucositis conditions.
口腔念珠菌病是接受化疗和放疗的患者中常见的机会性感染,必须加以治疗,以防止感染其他组织。制霉菌素(Nys)是治疗这种疾病最常开的药物之一,但由于其物理化学性质,其药物技术要求使其成为一个挑战。本工作的目的是开发和表征一种最佳的制霉菌素传递系统,用于潜在治疗口腔念珠菌病,避免潜在全身吸收的不良副作用和毒性。开发、评估和表征了一种纳米乳剂。它已成功地被配方为一种稳定的纳米乳剂,粒径为 138nm。使用不同的数学方法估计了释放参数,并且从制霉菌素通过猪口腔颊黏膜的体外渗透研究的结果可以假设不会发生全身作用。微生物学研究表明,负载制霉菌素的纳米乳剂具有增强的抗真菌作用。此外,通过透射电子显微镜对经处理的口腔颊黏膜超微结构的评价表明没有有害作用。因此,可以推断所开发的制剂可能可用于在黏膜炎条件下的念珠菌病感染。