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用于莫西沙星持续眼部给药的工程化聚乙烯醇-罗望子胶基生物复合材料:纳米纤维素对物理化学、机电和渗透动力学的影响。

Engineered PVA-tamarind gum-based biocomposite for sustained ophthalmic delivery of moxifloxacin: Effect of nanocellulose on physicochemical, mechanoelectrical and permeation kinetics.

作者信息

Habibullah Sk, Swain Rakesh, Das Mouli, Bhuyan Sisir Kumar, Mohanty Biswaranjan, Mallick Subrata

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be) University, Bhubaneswar 751003, Odisha, India.

Department of Pharmaceutics, Institute of Pharmacy and Technology, Salipur-754202, Cuttack, Odisha, India.

出版信息

Int J Biol Macromol. 2024 Dec;283(Pt 2):137712. doi: 10.1016/j.ijbiomac.2024.137712. Epub 2024 Nov 16.

Abstract

Widely used polysaccharide-based films in ophthalmic drug delivery have major limitations of inadequate mechanical strength, poor electrical conductivity, and insufficient ocular drug permeability. Moxifloxacin (MFX) biocomposite film of adequate mechanoelectrical properties was developed for sustained ophthalmic drug delivery. Nanocellulose (NC) incorporated (2.5, 5.0, 7.5, and 10.0 %) PVA-tamarind gum-based moxifloxacin composite was prepared using solvent casting method. The addition of NC improved the mechanical properties of the film, demonstrating its ability to strengthen the structure. Stress relaxation (SR) of the film has been augmented (64.67±7.55 to 73.15±0.34 %) due to increased content of NC (0 to 10 %) respectively. Film containing 5 % NC showed the critical edge of tensile strength (11.9±0.39 MPa), and also the threshold limit of electrical conductivity (4.5*10 Ω). The same film exhibited continued drug release as well as erosion-controlled sustained ocular permeation (pH 7.4) and revealed the highest antibacterial activity (ZOI of disc diffusion, cm) with Pseudomonas aeruginosa (4.63±0.15) and Staphylococcus aureus (4.30±0.26) of MFX (≈224 μg). Notably, incorporating NC produced non-irritating and safe for corneal delivery as confirmed by the Draize model test. Our findings suggested that the NC-containing PVA-tamarind gum-based composite film holds a promising approach for sustained ophthalmic delivery of MFX.

摘要

眼科药物递送中广泛使用的多糖基薄膜存在机械强度不足、导电性差和眼部药物渗透性不足等主要局限性。为实现眼科药物的持续递送,开发了具有适当机电性能的莫西沙星(MFX)生物复合薄膜。采用溶液浇铸法制备了含有纳米纤维素(NC)(2.5%、5.0%、7.5%和10.0%)的聚乙烯醇-罗望子胶基莫西沙星复合材料。NC的加入改善了薄膜的机械性能,表明其具有强化结构的能力。由于NC含量分别从0%增加到10%,薄膜的应力松弛(SR)得到增强(从64.67±7.55%增加到73.15±0.34%)。含有5%NC的薄膜显示出拉伸强度的临界值(11.9±0.39MPa),以及电导率的阈值(4.5×10Ω)。同一薄膜表现出持续的药物释放以及侵蚀控制的持续眼部渗透(pH7.4),并对约224μg的莫西沙星对铜绿假单胞菌(抑菌圈直径,cm为4.63±0.15)和金黄色葡萄球菌(抑菌圈直径,cm为4.30±0.26)显示出最高的抗菌活性。值得注意的是,经Draize模型试验证实,加入NC后制成的薄膜对角膜递送无刺激性且安全。我们的研究结果表明,含NC的聚乙烯醇-罗望子胶基复合薄膜是莫西沙星持续眼科递送的一种有前景的方法。

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