Recent Advances in the Synthesis of Fe 3O4@Au Core/Shell Nanoparticles -[62 refs.]. -(SALIHOV, S. V.; IVANENKOV, Y. A.; KRECHETOV, S. P.; VESELOV, M. S.; SVIRIDENKOVA, N. V.; SAVCHENKO, A. G.; KLYACHKO, N. L.; GOLOVIN, Y. I.; CHUFAROVA, N. V.; BELOGLAZKINA, E. K.; et al.; J. Magn. Magn. Mater. 394 (2015) 173-178, http://dx.
Purpose: Reducing the undesirable systemic effect of photodynamic therapy (PDT) can be achieved by incorporating a photosensitizer in microparticles (MPs). This study is devoted to the preparation of biocompatible biodegradable MPs with the inclusion of the natural photosensitizer Radachlorin (RС) and an assessment of the possibility of their use for PDT. Methods: RC-containing MPs (RС MPs) with poly(lactic-co-glycolic acid) copolymer (PLGA) matrix were prepared by a double emulsion solvent evaporation methods. The size and morphology of RC MPs were surveyed using scanning electron microscopy, confocal laser scanning microscopy, and dynamic light scattering. The content of RC, its release from RC MPs, and singlet oxygen generation were evaluated by the optical spectroscopy. Cellular uptake and cytotoxic photodynamic effect of RC MPs were investigated with in vitro assays. Results: The average diameter of the prepared RC MPs was about 2-3 μm. The RC MPsprepared by the water/oil/oil method had a significantly higher inclusion of RC (1.74 μg/mg) then RC MPs prepared by the water/oil/water method (0.089 μg/mg). Exposure of the prepared RC MPs to PDT light radiation was accompanied by the singlet oxygen generation and a cytotoxic effect for tumor cells. The release of the RC from the RC MPs was prolonged and lasted at least two weeks. Conclusion: PLGA RC MPs were found to cause a photoactivated cytotoxic effect for tumor cells and can be used for local application in PDT of tumors.
Introduction. Resveratrol is of scientific interest as a substance with a wide range of biological effects. However, its low bioavailability leads to limited use when administered orally. Therefore, the objective was to increase its solubility using various groups of excipients and create a solid dosage form. As a result of research, a group of twins was selected and the technology of manufacturing capsules containing 40 mg of resveratrol as a active substance was developed.Aim. The development of a solid dosage form – capsules containing resveratrol, tween 80 as a solubilizer and other excipients.Materials and methods. A composition with resveratrol, tween 80, glycerin, citric and ascorbic acids as stabilizers was developed. Methanol was used as a common solvent and was distilled off after complete dissolution of all components and obtaining a homogeneous mass. After adding olive oil (as a filler) to the resulting composition and a mixture of nipazole and nipagin (0.03 % by weight of the contents), the composition was manually mixed and poured into subsequently gelatin coated capsules for tightness. The quality indicators of the obtained capsules were studied in accordance with the requirements of the State pharmacopoeia XIV of Russian Federation (description, disintegration, dissolution, uniformity of dosage, residual organic solvents), as well as oxidation indicators.Results and discussion. During the research it was found that the obtained samples of capsules containing resveratrol 40 mg/caps. as an active substance, and tween 80 as a solubilizer, had a good disintegration. The substance is well soluble in hydrochloric acid condition, which indicates its high bioavailability.Conclusion. To produce capsules with resveratrol (40 mg/caps.) containing tween 80, glycerin, citric and ascorbic acids, excipients were selected according to studies that confirm the improvement of resveratrol bioavailability. The quality of the dosage form was assessed in accordance with the State Pharmacopoeia XIVth edition: it was shown that the use of Tween 80 as a solubilizer increases the release of resveratrol in the environment of gastric juice.
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