Physicochemical Properties of Intravitreal Implant Based on Chitosan/Polyvinyl Alcohol Saturated with 5-Fluorouracil

The aim of the investigation was to evaluate the possibility of using intravitreal introduction of the implant based on chitosan-polymer film saturated with 5-fluorouracil.

Materials and Methods. There was performed a study of physicochemical properties of chitosan/polyvinyl alcohol-based implant saturated with 5-fluorouracil (5-FU) in concentrations of 0.05 and 0.1 ml. The implant size was 8.0×1.0×0.35 mm. The process of drug release was studied by UV spectroscopy based on the characteristic absorption maximum. To assess the sterilization ability of chitosan films, their thermal stability was studied. The possibilities of interaction between chemical groups of chitosan, polyvinyl alcohol and 5-FU were studied by analyzing the infrared spectra of these substances.

Results. It was established that the process of drug release from the system occurs in three stages: 1) sorption of water by the film and swelling; 2) the drug diffusing in the film to the interphase boundary between the polymer system and the environment; 3) the drug diffusing into the solvent volume. Release of 5-FU from the implant to Ringer–Locke solution occurs almost completely within 7–8 h without undergoing any change. Thermal degradation of the implant begins at the temperature of 200°C. Infrared spectroscopy data evidence that 5-FU immobilized on chitosan film with polyvinyl alcohol undergoes no chemical changes and, consequently, does not lose its pharmacological properties.

Conclusion. The study of physicochemical properties of chitosan/polyvinyl alcohol-based implant saturated with 5-FU cytostatic proves the feasibility of its use in ophthalmology to reduce the initial peak concentration of 5-FU and, consequently, eliminate its toxic effects and prolong the drug action.

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Baiyrkhanova A.O., Botabekova T.K., Semenova Y.M., Ismailova A.B., Rakhypbekov T.K. Physicochemical Properties of Intravitreal Implant Based on Chitosan/Polyvinyl Alcohol Saturated with 5-Fluorouracil. Sovremennye tehnologii v medicine 2017; 9(3): 102, https://doi.org/10.17691/stm2017.9.3.14