质量源于设计辅助开发用于治疗白色念珠菌感染的卢利康唑经溶胶体。

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Assay and drug development technologies Pub Date : 2024-01-01 Epub Date: 2023-12-29 DOI:10.1089/adt.2023.059
Gurmeet Singh, Raj Kumar Narang
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引用次数: 0

摘要

本研究旨在开发和评估一种新型的卢立康唑(LUL)囊泡制剂,用于通过局部途径治疗白色念珠菌感染。研究人员采用薄膜水合法制备了装载卢立康唑的透硫体(LUL-TE),并采用方框-贝肯设计法对各种自变量和因变量进行了优化。选定的关键材料属性包括磷脂含量(X1)、乙醇浓度(X2)和胆酸钠含量(X3)。对配制的 LUL-TE 进行了夹持效率百分比、药物负载百分比、囊泡大小和多分散指数(PDI)的表征,并将其加入卡波姆凝胶基质中,进一步进行凝胶表征评估。对制备的反式硫糖体凝胶(LUL-TE-CHG)进行了 pH 值、铺展性、粘度、抗真菌活性和体外研究评估。观察结果表明,所制备的 LUL-TE-CHG 具有理想的 pH 值(6.2 ± 0.45)、铺展性[8.3 ± 0.42 g/(cm-s)]、粘度(236.1-19.2.26 mPa-s)、纳米粒子尺寸(252 ± 9.82)、夹带效率(85% ± 5.24%)、Zeta 电位(-34.05 ± 3.52 mV)和 PDI(0.233 ± 0.002)。抑菌区结果表明,LUL-TE-CHG 制剂的抗真菌活性最高,为 5.83 ± 0.15 mm3。体外实验结果表明,2 小时内药物释放率为 18.1% ± 2.0%,8 小时内药物持续释放率为 83.2% ± 1.7%。最后,为了证实所开发制剂的疗效,使用白僵菌诱导 Wistar 大鼠感染真菌。在疾病诱导模型中进行了体内皮肤刺激性研究和组织病理学研究。动物实验表明,LUL-TE-CHG 能明显改善 Wistar 大鼠的疾病状况。从皮肤渗透和皮肤沉积曲线观察到的结果表明,与 LUL-CHG 相比,制备的新型 LUL-loaded TE 系统具有更高的渗透率和更长的保留时间。含有 LUL 的水凝胶可能是一种安全有效的治疗真菌的新方法。
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Quality by Design Assisted Development of Luliconazole Transethosomes in Gel for the Management of Candida albicans Infection.

The objective of this study was to develop and evaluate a novel vesicular formulation of luliconazole (LUL) for the management of Candida albicans infection through a topical route. LUL-loaded transethosomes (LUL-TE) were prepared by the film hydration method and various independent and dependent variables were optimized using the Box-Behnken design. Selected critical material attributes were the content of phospholipids (X1), concentration of ethanol (X2), and amount of sodium cholate (X3). Formulated LUL-TE were characterized for percent entrapment efficiency, percent drug loading, vesicle size, and polydispersity index (PDI) and were incorporated into the carbomer gel base and further evaluated for gel characterizations. The prepared transethosomal gel (LUL-TE-CHG) was evaluated for pH, spreadability, viscosity, antifungal activity, and in vitro study. From the observed results, it was evident that the prepared LUL-TE-CHG was in the desired pH (6.2 ± 0.45), spreadability [8.3 ± 0.42 g/(cm·s)], viscosity (236.1-19.2.26 mPa·s), nanovesicle size (252 ± 9.82), entrapment efficiency (85% ± 5.24%), zeta potential (-34.05 ± 3.52 mV), and PDI (0.233 ± 0.002). The zone of inhibition results suggested that the LUL-TE-CHG formulation has the highest antifungal activity, that is, 5.83 ± 0.15 mm3. The in vitro results showed that drug release within 2 h was 18.1% ± 2.0% and after that sustained release action, 83.2% ± 1.7% within 8 h. Finally, to confirm the therapeutic efficacy of the developed formulation, fungal infection was induced by using C. albicans in Wistar rats. In vivo, skin irritation study and histopathology studies were performed in the disease-induced model. Animal experiments revealed that LUL-TE-CHG has significantly improved the diseased condition in Wistar rats. The results observed from the skin permeation and skin deposition profile ensure that the prepared novel LUL-loaded TE system had a higher permeation rate and increased retention time compared with LUL-CHG. The hydrogel incorporated with LUL could be a novel approach with safe and effective fungal treatment.

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来源期刊
Assay and drug development technologies
Assay and drug development technologies 医学-生化研究方法
CiteScore
3.60
自引率
0.00%
发文量
33
审稿时长
>12 weeks
期刊介绍: ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts
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