壳聚糖纳米颗粒——将药物输送到眼睛前段的系统

EKATERINA V. POPOVA, VICTORIA E. TIKHOMIROVA, OLGA V. BEZNOS, NATALIA B. CHESNOKOVA, YURI V. GRIGORIEV, OLGA A. KOST
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引用次数: 1

摘要

药物渗透到眼睛内部组织的有效性受到角膜屏障作用和泪液冲洗药物的显著限制。为了提高药物的生物利用度,建议将药物加入由5kda壳聚糖和72kda糖醇壳聚糖两种壳聚糖组成的壳聚糖颗粒中。壳聚糖颗粒掺入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,正的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,可延长依那普利特在兔泪液中的滞留时间。
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CHITOSAN NANOPARTICLES - THE DRUG DELIVERY SYSTEM TO THE ANTERIOR SEGMENT OF THE EYE
The effectiveness of drug penetration into the inner tissues of the eye is signi cantly limited by the barrier effect of the cornea and by the washing out of a drug with tear uid. 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 85-125 nm and a positive ζ-potential of +21±3 mV, while particles formed by 72 kDa glycol-chitosan were 440-480 nm by size and had ζ-potential of +10±2 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 uid of rabbits.
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