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Ekaterina V. Popova, Victoria E. Tikhomirova, Olga V. Beznos, Natalia B. Chesnokova, Yuri V. Grigoriev, Olga A. Kost

Chitosan nanoparticles the drug delivery system to the anterior segment of the eye


Abstract. The effectiveness of drug penetration into the inner tissues of the eye is significantly limited by the barrier effect of the cornea and by the washing out of a drug with tear fluid. To increase the bioavailability of the drug, it was proposed to include the drug in chitosan particles formed by two types of chitosan 5 kDa chitosan and 72 kDa glycol-chitosan. Chitosan particles with incorporated angiotensin-converting enzyme inhibitor enalaprilat, capable to reduce intraocular pressure, were characterized by dynamic light scattering and scanning electron microscopy. Particles formed by 5 kDa chitosan had an average hydrodynamic diameter of 85125 nm and a positive ζ-potential of +213 mV, while particles formed by 72 kDa glycol-chitosan were 440480 nm by size and had ζ-potential of +102 mV. The percentage of inclusion of enalaprilat in chitosan particles was 25% and 40%, respectively. In vivo experiments have shown that the inclusion of the drug in chitosan particles increased the retention time of enalaprilat in the lacrimal fluid of rabbits.
Key words: mucoadhesiveness, chitosan, angiotensin-converting enzyme inhibitor, intraocular pressure, delivery to the eye, lacrimal fluid
Moscow University Chemistry Bulletin.
2023, Vol. 64, No. 2, P. 141

Copyright (C) Chemistry Dept., Moscow State University, 2002
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