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用于提高环丙沙星溶解度和生物利用度的自乳化药物递送系统的设计与开发

Design and Development of Self-Emulsifying Drug Delivery System to Improve the Solubility and Bioavailability of Ciprofloxacin.

作者信息

Akhlaq Muhammad, Azad Abul Kalam, Khan Azmat Ali, Fatima Sabiha, Kumarasamy Vinoth, Subramaniyan Vetriselvan, Miret Mireia Mallandrich

机构信息

Department of Pharmacy, Hazara University.

Faculty of Pharmacy, University MAIWP International.

出版信息

J Vis Exp. 2025 Jun 27(220). doi: 10.3791/66959.

Abstract

Ciprofloxacin, a potent fluoroquinolone antibiotic, is used to treat various bacterial infections. This drug has low aqueous solubility and limited oral bioavailability. To overcome these limitations, this study focused on developing a Self-Emulsifying Drug Delivery System (SEDDS) for Ciprofloxacin, aiming to enhance its solubility and bioavailability. The formulation process involved selecting silicone oil, Tween 80, propylene glycol (PG), and polyethylene glycol (PEG) as the core components based on solubility studies. The optimization of SEDDS formulations was guided by pseudo-ternary phase diagrams, which helped in identifying the effective self-emulsifying regions and determining the optimal ratios of surfactant and co-surfactant. Evaluation of the SEDDS formulations involved droplet size and zeta potential measurements alongside Fourier-transform infrared (FT-IR) spectroscopy, confirming drug-excipient compatibility and successful drug incorporation. The F2 and F5 formulations exhibited droplet sizes of 320 nm and 202 nm, respectively, with corresponding zeta potentials of -11.4 mV and -13.38 mV, indicative of stability. Release studies showed an initial rapid release, with 88.2% released from F5 within the first 2 h, followed by a sustained release, reaching 93.1% after 5 h. The current formulations significantly improve the drug's solubility and bioavailability.

摘要

环丙沙星是一种强效氟喹诺酮类抗生素,用于治疗各种细菌感染。这种药物的水溶性低,口服生物利用度有限。为克服这些局限性,本研究专注于开发一种用于环丙沙星的自乳化药物递送系统(SEDDS),旨在提高其溶解度和生物利用度。制剂工艺基于溶解度研究,选择硅油、吐温80、丙二醇(PG)和聚乙二醇(PEG)作为核心成分。SEDDS制剂的优化以伪三元相图为指导,这有助于确定有效的自乳化区域,并确定表面活性剂和助表面活性剂的最佳比例。对SEDDS制剂的评估包括液滴大小和zeta电位测量以及傅里叶变换红外(FT-IR)光谱,以确认药物与辅料的相容性以及药物的成功包载。F2和F5制剂的液滴大小分别为320 nm和202 nm,相应的zeta电位为-11.4 mV和-13.38 mV,表明具有稳定性。释放研究显示初期快速释放,F5在最初2小时内释放了88.2%,随后是持续释放,5小时后达到93.1%。当前的制剂显著提高了药物的溶解度和生物利用度。

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