优化的D-α-生育酚聚乙二醇琥珀酸酯/磷脂自组装混合胶束:增强氟康唑抗真菌活性的有前途的脂质纳米平台。

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY Acta Pharmaceutica Pub Date : 2022-12-01 DOI:10.2478/acph-2022-0028
Shaimaa M Badr-Eldin, Hibah M Aldawsari, Usama A Fahmy, Osama A A Ahmed, Nabil A Alhakamy, Mahmoud A Elfaky, Alaa Sirwi, Salman A Hawsawi, Ali H Alzahrani, Abdulrahman Y Yaseen, Mohannad Qassim, Sabna Kotta
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引用次数: 0

摘要

氟康唑(Fluconazole, FLZ)是治疗皮肤念珠菌病最广泛使用的抗真菌药物。虽然口服FLZ已被证明是有效的,但副作用的发生率需要开发一种有效的配方,可以超越与全身可得性相关的陷阱。因此,本研究旨在开发一种自组装的混合胶束局部递送系统,以增强药物的局部递送。用D-α-生育酚聚乙二醇1000琥珀酸酯和磷脂制备了自组装混合胶束,并采用Box-Behnken设计优化。然后在免疫功能低下小鼠体内测试了最小尺寸的优化配方对白色念珠菌的抗真菌活性。与原始的FLZ负载凝胶相比,使用优化的配方治疗可以减少周围红斑以及真菌感染引起的病变。因此,该制剂被认为是治疗皮肤念珠菌病的一种有前途的载体。
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Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole.

Fluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availability. Accordingly, this research aimed at developing a self-assembled mixed micelles topical delivery system to enhance the topical delivery of the drug. Self-assembled mixed micelles were developed using D-α-tocopheryl polyethylene glycol 1000 succinate and phospholipids and optimized using Box-Behnken design. The optimized formulation with minimized size was then tested in vivo for the antifungal activity against C. albicans in immunocompromised mice. Treatment with the optimized formulation led to decreased peripheral erythema as well as lesions due to fungal infection in comparison to raw FLZ loaded gel. Therefore, the developed formulation was found to be a promising vehicle for the treatment of cutaneous candidiasis.

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来源期刊
Acta Pharmaceutica
Acta Pharmaceutica PHARMACOLOGY & PHARMACY-
CiteScore
5.20
自引率
3.60%
发文量
20
审稿时长
>12 weeks
期刊介绍: AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.
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