Evaluation of the anticandidal activity of clotrimazole using Lactobacillus caseie ghosts as biological drug carrier.

Touba Eslaminejad, Mohammad Hassan Moshafi, Matineh Hasanpore, Seyed Amin Ayatollahi, Mehdi Ansari
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引用次数: 1

Abstract

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. IC50 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.

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以干酪乳杆菌为生物药物载体评价克霉唑的抗念珠菌活性。
背景:白色念珠菌引起口腔和阴道粘膜感染以及血液和深层组织感染。氯霉唑作为一种广谱抗有丝分裂药物,通常用于治疗白色念珠菌感染。细菌幽灵是一种死亡细胞,具有广泛的潜力,可以靶向各种身体组织和细胞作为药物载体。目的:希望利用细菌幽灵负载克霉唑来克服这种耐药性。方法:采用乳酸菌80与乳酸混合制备乳酸菌鬼影,采用纳米滴光度法测定上清液中DNA和蛋白质的含量。采用光镜、扫描电镜、原子力显微镜等检测了Ghost的形态特征。用平板法测定了合成鬼菌的抑菌活性。使用三个独立的垂直Franz细胞评价药物释放谱。将bg -氯霉唑加入乳膏基质中,考察其在皮肤上的可配伍性和均匀性。结果:纳米滴分析结果显示,与对照组相比,处理后的上清液中可见蛋白质和DNA。AFM结果显示干酪乳杆菌鬼影细胞分布均匀,呈杆状。用扫描电镜观察了干酪乳杆菌裂解孔的形成。由于其高装载能力,BGs是一种极好的药物输送系统。在90分钟内,近50%的氯霉唑从BGs中释放出来。100 mg/l的氯霉唑- bg组抗药活性最高,10 mg/l的氯霉唑组也有毒性作用。氯霉唑- bg的IC50为0.001 mg/l。化学稳定性结果表明,复方中约有90%的氯霉唑残留。结论:细菌鬼影具有较高的载药能力,能在6个月内保持和释放药物,可作为一种优良的给药系统。
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