以结冷胶与氧氟沙星配合物为基础的眼科给药系统

IF 0.3 Q4 CHEMISTRY, MULTIDISCIPLINARY Chemical Bulletin of Kazakh National University Pub Date : 2022-06-20 DOI:10.15328/cb1239
G. Tatykhanova, V. Aseyev, M. Vamvakaki, V. Khutoryanskiy, S. Kudaibergenov
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引用次数: 0

摘要

研究了天然多糖结冷胶与抗菌药物氧氟沙星在水溶液中形成的络合物。电导和电位滴定曲线表明,结冷胶与氧氟沙星形成了一种由离子键和氢键稳定的水溶性络合物,其组成为2:1 mol/mol。通过红外光谱、动态光散射、ζ电位和热重分析证实了胶凝-氧氟沙星配合物的形成。配合物的平均水动力尺寸为307±5 nm, ζ电位为负,为-15 mV。用0.3 wt.%的CaCl2凝胶化的凝胶-氧氟沙星配合物薄膜,研究了氧氟沙星在蒸馏水和磷酸盐缓冲液中的释放动力学。在λmax = 289 nm处用紫外可见光谱评价药物释放动力学,用Ritger-Peppas模型计算药物释放动力学符合蒸馏水中的非菲克扩散和磷酸盐缓冲液中的Case II转运(零级动力学)。凝胶-氧氟沙星膜在磷酸盐缓冲液和蒸馏水中的累积释放量分别为96±2%和36±2%。预计胶凝-氧氟沙星复合物能够在眼表面形成原位凝胶,并延长药物在泪液中的停留时间。
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Ophthalmic drug delivery system based on the complex of gellan and ofloxacin
Complex formation between a natural polysaccharide – gellan and an antimicrobial drug – ofloxacin was studied in aqueous solution. Conductimetric and potentiometric titration curves revealed that gellan and ofloxacin forms a water-soluble complex of composition 2:1 mol/mol stabilized by ionic and hydrogen bonds. The formation of the gellan-ofloxacin complex was confirmed by FTIR spectroscopy, dynamic light scattering, zeta-potential and thermogravimetric analysis. The average hydrodynamic size of the complex was found 307±5 nm and its zeta-potential was negative and equal to -15 mV. Thin films of the gellan-ofloxacin complex, gelled in 0.3 wt.% of CaCl2, were used to study the release kinetics of ofloxacin in distilled water and phosphate buffer. The drug release kinetics evaluated by UV-Vis spectroscopy at λmax = 289 nm and calculated by the Ritger-Peppas model correspond to non-Fickian diffusion in distilled water and Case II transport (zero-order kinetics) in phosphate buffer. The cumulative release of ofloxacin from the gellan-ofloxacin films was equal to 96±2% and 36±2% in phosphate buffer and distilled water, respectively. It is expected that the gellan-ofloxacin complex is able to form in situ gel on the surface of the eye and to prolong the drug residence time in the tear fluid.
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