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开发、优化并评价一种负载米康唑的芝麻油纳米结构脂质载体,用于治疗口腔念珠菌病。

Development, optimization, and evaluation of a nanostructured lipid carrier of sesame oil loaded with miconazole for the treatment of oral candidiasis.

机构信息

Faculty of Pharmacy, Department of Pharmaceutics, King Abdulaziz University, Jeddah, Saudi Arabia.

Faculty of Dentistry, Department of Oral Diagnostic Sciences, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Drug Deliv. 2022 Dec;29(1):254-262. doi: 10.1080/10717544.2021.2023703.

DOI:10.1080/10717544.2021.2023703
PMID:35014929
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8757592/
Abstract

is the fungus responsible for oral candidiasis, a prevalent disease. The development of antifungal-based delivery systems has always been a major challenge for researchers. This study was designed to develop a nanostructured lipid carrier (NLC) of sesame oil (SO) loaded with miconazole (MZ) that could overcome the solubility problems of MZ and enhance its antifungal activity against oral candidiasis. In the formulation of this study, SO was used as a component of a liquid lipid that showed an improved antifungal effect of MZ. An optimized MZ-loaded NLC of SO (MZ-SO NLC) was used, based on a central composite design-based experimental design; the particle size, dissolution efficiency, and inhibition zone against oral candidiasis were chosen as dependent variables. A software analysis provided an optimized MZ-SO NLC with a particle size of 92 nm, dissolution efficiency of 88%, and inhibition zone of 29 mm. Concurrently, the permeation rate of the sheep buccal mucosa was shown to be significantly ( < .05) higher for MZ-SO NLC (1472 µg/cm) as compared with a marketed MZ formulation (1215 µg/cm) and an aqueous MZ suspension (470 µg/cm). Additionally, an efficacy study in terms of the ulcer index against found a superior result for the optimized MZ-SO NLC (0.5 ± 0.50) in a treated group of animals. Hence, it can be concluded that MZ, through an optimized NLC of SO, can treat candidiasis effectively by inhibiting the growth of .

摘要

是引起口腔念珠菌病的真菌,这是一种普遍存在的疾病。开发基于抗真菌的递药系统一直是研究人员面临的主要挑战。本研究旨在开发一种负载咪康唑(MZ)的芝麻油(SO)纳米结构脂质载体(NLC),以克服 MZ 的溶解度问题并增强其抗口腔念珠菌病的活性。在本研究的配方中,SO 被用作液体脂质的成分,显示出 MZ 的改善抗真菌作用。基于基于中心复合设计的实验设计,使用了优化的负载 MZ 的 SO NLC(MZ-SO NLC);选择粒径、溶解效率和对口腔念珠菌病的抑制区作为因变量。软件分析提供了优化的 MZ-SO NLC,粒径为 92nm,溶解效率为 88%,对口腔念珠菌病的抑制区为 29mm。同时,与市售 MZ 制剂(1215µg/cm)和水性 MZ 混悬液(470µg/cm)相比,MZ-SO NLC 的羊口腔颊黏膜透过率显著更高( < .05)。此外,在针对溃疡指数的功效研究中,优化的 MZ-SO NLC (0.5±0.50)在动物治疗组中表现出更好的结果。因此,可以得出结论,通过优化的 SO NLC,MZ 可以通过抑制的生长有效治疗念珠菌病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/4ed660581ba1/IDRD_A_2023703_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/97c4b4491b9d/IDRD_A_2023703_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/4d364032cb67/IDRD_A_2023703_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/61d4cb1a8b33/IDRD_A_2023703_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/a3bd22646685/IDRD_A_2023703_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/3c5af25f4bf2/IDRD_A_2023703_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/4ed660581ba1/IDRD_A_2023703_F0006_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/97c4b4491b9d/IDRD_A_2023703_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/4d364032cb67/IDRD_A_2023703_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/61d4cb1a8b33/IDRD_A_2023703_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/a3bd22646685/IDRD_A_2023703_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/3c5af25f4bf2/IDRD_A_2023703_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/910a/8757592/4ed660581ba1/IDRD_A_2023703_F0006_B.jpg

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