Ciprofloxacin (CPFX) containing therapeutic systems were developed using gel- and liposome-based formulations to minimize tear-driven dilution in the conjunctival sac, a long-pursued objective in ophthalmology. Physicochemical properties (pH, osmolarity, viscosity, expansivity, membrane fluidity and in vitro CPFX release rate) of the preparations were studied by the appropriate methods. For gel preparation, the bio-adhesive poly(vinyl alcohol) and polymethacrylic acid derivatives were applied in various concentrations. In our liposome-supported carrier systems, multilamellar vesicles from lecithin and alpha-L-dipalmithoyl-phosphatidylcholine provided the encapsulating agent. Electron paramagnetic resonance (EPR) spectroscopy was applied to study the molecular interactions in the ophthalmic formulations. The polymer hydrogels used in our preparations ensured a steady and prolonged active ingredient release. In addition, encapsulation of the CPFX into liposomes prolonged the in vitro release of the antibacterial agent depending on the lipid composition of the vesicles.

译文

:含有环丙沙星(CPFX)的治疗系统是使用基于凝胶和脂质体的制剂开发的,以最大程度地减少眼结膜囊中眼泪驱动的稀释作用,结膜囊是眼科长期以来追求的目标。通过适当的方法研究了制剂的理化性质(pH,摩尔渗透压浓度,粘度,膨胀性,膜流动性和体外CPFX释放速率)。为了制备凝胶,以各种浓度施加生物粘附性聚乙烯醇和聚甲基丙烯酸衍生物。在我们的脂质体支持的载体系统中,卵磷脂和α-L-二棕榈酰-磷脂酰胆碱的多层囊泡提供了包封剂。电子顺磁共振(EPR)光谱用于研究眼科制剂中的分子相互作用。我们制剂中使用的聚合物水凝胶可确保稳定和延长活性成分的释放。另外,取决于囊泡的脂质组成,将CPFX包封到脂质体中延长了抗菌剂的体外释放。

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