Chitosan Nanoparticles: The Drug Delivery System to the Anterior Segment of the Eye

IF 0.7 Q4 CHEMISTRY, MULTIDISCIPLINARY

Moscow University Chemistry Bulletin Pub Date : 2023-04-24 DOI:10.3103/S0027131423020062

E. V. Popova, V. E. Tikhomirova, O. V. Beznos, N. B. Chesnokova, Y. V. Grigoriev, O. A. Kost

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Abstract

The effectiveness of drug penetration into the inner tissues of the eye under local application is significantly limited by the barrier effect of the cornea and by the washout of the drug with the lacrimal fluid. To increase the bioavailability of a drug, it is proposed to include the drug in the chitosan particles formed by two types of chitosan: 5 kDa chitosan and 72 kDa glycol-chitosan. Chitosan particles with the loaded angiotensin-converting enzyme inhibitor enalaprilat, capable to reduce intraocular pressure, are characterized by dynamic light scattering and scanning electron microscopy. Particles formed by 5 kDa chitosan have an average hydrodynamic diameter from 85 to 125 nm and a positive ζ potential of +21 ± 3 mV, while particles formed by 72 kDa glycol-chitosan have a size from 440 to 480 nm and are characterized by a ζ potential of +10 ± 2 mV. The percentage of enalaprilat inclusion in the chitosan particles is 25% and 40%, respectively. In vivo experiments showed that the inclusion of the drug int the chitosan particles can increase the retention time of enalaprilat in the lacrimal film of rabbits.

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壳聚糖纳米颗粒:眼睛前段的药物输送系统

角膜的屏障作用和泪液对药物的冲洗，严重限制了局部应用药物渗入眼内组织的有效性。为了提高药物的生物利用度，建议将药物掺入由两种类型的壳聚糖(5kda壳聚糖和72kda糖基壳聚糖)制成的壳聚糖颗粒中。壳聚糖颗粒载血管紧张素转换酶抑制剂依那普利特，具有降低眼压的作用，采用动态光散射和扫描电镜对其进行了表征。5 kDa的壳聚糖形成的颗粒的平均水动力直径为85 ~ 125 nm，正ζ电位为+21±3 mV; 72 kDa的乙二醇壳聚糖形成的颗粒的平均水动力直径为440 ~ 480 nm， ζ电位为+10±2 mV。依那普利在壳聚糖颗粒中的包合率分别为25%和40%。体内实验表明，将依那普利特包裹在壳聚糖颗粒中可以延长依那普利特在兔泪膜中的滞留时间。

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来源期刊

Moscow University Chemistry Bulletin CHEMISTRY, MULTIDISCIPLINARY-

CiteScore

1.30

自引率

14.30%

发文量

期刊介绍： Moscow University Chemistry Bulletin is a journal that publishes review articles, original research articles, and short communications on various areas of basic and applied research in chemistry, including medical chemistry and pharmacology.