评价利用干酪乳杆菌 ghost 作为生物药物载体的克霉唑抗真菌活性。
Evaluation of the anticandidal activity of clotrimazole using Lactobacillus caseie ghosts as biological drug carrier.
机构信息
Pharmaceutics Research Centre, Institute of Neuropharmacology, Kerman University of, Medical Sciences, Kerman, Iran.
Departments of Drug and Food Control, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
出版信息
Daru. 2022 Jun;30(1):67-73. doi: 10.1007/s40199-022-00432-0. Epub 2022 Mar 15.
BACKGROUND
Candida albicans cause oral and vaginal mucosa infections as well as bloodstream and deep-tissue infections. Commonly, clotrimazole as a broad-spectrum antimitotic drug applied for treatment of Candida albicans infections. Bacterial ghosts are dead cells that have the broad potential to target the various body tissues and cells as drug vector.
OBJECTIVES
We hope to conquest this resistance by using clotrimazole loaded on bacterial ghosts.
METHODS
Lactobacillus ghosts were produced by using tween 80 and lactic acid according to the protocol and the amount of the DNA and protein in supernatant was measured by Nano-drop spectrophotometry. Ghost's morphological characteristics were detected by using light microscopy, SEM and AFM. Antifungal activities of the synthesized ghosts were measured by plate methods. Three independent vertical Franz cells were used to evaluate drug release profile. BG-clotrimazole was added into cream base and was examined for dispensability as well as uniformity of the formulation on the skin.
RESULTS
Results of the Nano-drop analysis showed that protein and DNA was seen in supernatant of treatment compared to control groups. AFM results showed well-dispersed and rod-shaped L. casei ghost cells. Lysis pores formation in the L. casei ghosts was indicated by SEM micrographs. BGs represent an excellent drug delivery system because of the high loading capability. Nearly, 50% of clotrimazole was released from BGs during 90 min. Highest anticandidal activity occurred using 100 mg/l clotrimazole-BG, while toxic effects were also seen with 10 mg/l clotrimazole. IC clotrimazole-BG was found at 0.001 mg/l. Chemical stability results showed that about 90% of clotrimazole remained in the formulation.
CONCLUSION
It could be concluded that the bacterial ghosts are very talented to high loading capability, keeping and releasing drug during six months, therefore these could act as an excellent drug delivery system.
背景
白色念珠菌会引起口腔和阴道黏膜感染，以及血液和深部组织感染。通常，克霉唑作为一种广谱抗有丝分裂药物，用于治疗白色念珠菌感染。细菌细胞碎片是一种死细胞，具有广泛的靶向各种身体组织和细胞的潜力，可以作为药物载体。
目的
我们希望通过使用负载克霉唑的细菌细胞碎片来克服这种耐药性。
方法
根据方案，使用吐温 80 和乳酸生产乳杆菌细胞碎片，并用纳诺-drop 分光光度计测量上清液中的 DNA 和蛋白质含量。用光镜、SEM 和 AFM 检测细胞碎片的形态特征。通过平板法测量合成细胞碎片的抗真菌活性。使用三个独立的垂直 Franz 细胞评估药物释放曲线。将 BG-克霉唑加入乳膏基质中，并检查制剂在皮肤上的可分配性和均匀性。
结果
Nano-drop 分析结果表明，与对照组相比，处理组上清液中可见蛋白质和 DNA。AFM 结果显示，L. casei 细胞碎片分散良好，呈杆状。SEM 显微照片显示，L. casei 细胞碎片中形成了裂解孔。由于具有高载药能力，BG 代表了一种优秀的药物传递系统。在 90 分钟内，几乎有 50%的克霉唑从 BG 中释放出来。当使用 100mg/l 克霉唑-BG 时，BG 表现出最高的抗真菌活性，而当使用 10mg/l 克霉唑时，也观察到了毒性作用。IC 克霉唑-BG 为 0.001mg/l。化学稳定性结果表明，约 90%的克霉唑保留在制剂中。
结论
可以得出结论，细菌细胞碎片具有很高的载药能力，能够在六个月内保持和释放药物，因此它们可以作为一种优秀的药物传递系统。
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