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载有莫西沙星的聚乙烯醇-壳聚糖复合膜作为潜在的眼部药物递送系统:全面表征与疗效评估

Moxifloxacin-loaded PVA-chitosan composite films as potential ocular drug delivery systems: A comprehensive characterization and efficacy assessment.

作者信息

Das Swagatika, Behera Amulyaratna, Habibullah Sk, Pattnaik Gurudutta, Mohanty Biswaranjan

机构信息

School of Pharmacy and Life Sciences, Centurion University of Technology and Management, Odisha, India.

School of Pharmacy and Life Sciences, Centurion University of Technology and Management, Odisha, India.

出版信息

Int J Biol Macromol. 2025 Mar;296:139726. doi: 10.1016/j.ijbiomac.2025.139726. Epub 2025 Jan 10.

Abstract

To overcome the barriers often met by traditional ophthalmic formulations, polymeric films can be utilized as an alternative to enhance drug retention duration while managing medication release. In the current investigation, polymeric films made of poly (vinyl) alcohol (PVA) and chitosan (CS) loaded with Moxifloxacin Hydrochloride (M-HCl) and plasticized with Glutaraldehyde were formulated as potential ophthalmic delivery for the treatment of conjunctivitis. The thickness, surface pH, opacity, folding endurance, and % hemolysis were measured, followed by the transparency, microscopy, electrical conductivity, mechanical strength, swelling index, and invitro drug release studies. FTIR spectroscopy further accessed the interactions between the polymers and drug molecules. The thermal behaviour and diffraction pattern of the films were evaluated using DSC and XRD studies. Lastly, the antimicrobial effectiveness of the M-HCl-loaded films was studied against P. aeruginosa and S. aureus. The rabbit eye irritation study conducted in vivo confirmed that the film was comfortable for use in ocular applications. Upon integrating the findings, it was determined that the optimal film formulation was PC3 (PVA: CS = 7:3), exhibiting superior transparency, heightened intermolecular hydrogen bonding, elevated mechanical strength, increased crystallinity, larger crystal size, optimal swelling index, a high percentage of controlled drug release (%CPDR), and the highest antimicrobial activity.

摘要

为克服传统眼科制剂常遇到的障碍,可利用聚合物薄膜作为替代方案,以延长药物滞留时间并控制药物释放。在当前研究中,由聚乙烯醇(PVA)和壳聚糖(CS)制成、负载盐酸莫西沙星(M-HCl)并用戊二醛增塑的聚合物薄膜被制备成用于治疗结膜炎的潜在眼部给药制剂。测定了薄膜的厚度、表面pH值、不透明度、耐折性和溶血百分比,随后进行了透明度、显微镜检查、电导率、机械强度、溶胀指数和体外药物释放研究。傅里叶变换红外光谱(FTIR)进一步研究了聚合物与药物分子之间的相互作用。使用差示扫描量热法(DSC)和X射线衍射(XRD)研究评估了薄膜的热行为和衍射图谱。最后,研究了负载M-HCl的薄膜对铜绿假单胞菌和金黄色葡萄球菌的抗菌效果。在体内进行的兔眼刺激研究证实该薄膜在眼部应用中使用舒适。综合研究结果,确定最佳薄膜配方为PC3(PVA:CS = 7:3),其具有优异的透明度、增强的分子间氢键、提高的机械强度、增加的结晶度、更大的晶体尺寸、最佳的溶胀指数、高百分比的控释药物(%CPDR)以及最高的抗菌活性。

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