Budai Lívia, Hajdú Mária, Budai Marianna, Gróf Pál, Béni Szabolcs, Noszál Béla, Klebovich Imre, Antal István
Semmelweis University, Department of Pharmaceutics, H-1092 Budapest, Hogyes E. u. 7, Hungary.
Int J Pharm. 2007 Oct 1;343(1-2):34-40. doi: 10.1016/j.ijpharm.2007.04.013. Epub 2007 Apr 24.
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.
使用基于凝胶和脂质体的制剂开发了含环丙沙星（CPFX）的治疗系统，以尽量减少泪液驱动的结膜囊稀释，这是眼科长期追求的目标。通过适当的方法研究了制剂的物理化学性质（pH值、渗透压、粘度、膨胀性、膜流动性和体外CPFX释放率）。对于凝胶制剂，应用了不同浓度的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载体系统中，来自卵磷脂和α-L-二棕榈酰磷脂酰胆碱的多层囊泡提供了包封剂。应用电子顺磁共振（EPR）光谱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确保了活性成分的稳定和持续释放。此外，根据囊泡的脂质组成，将CPFX包封到脂质体中延长了抗菌剂的体外释放。
