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采用逆相蒸发法制备了道诺霉素脂质体,测得脂质体包裹率为31.6%,终浓度为100μg/ml,直径为60～125nm。用荧光分光光度法在24只兔进行了道诺霉索及其脂质体玻璃体内药物清除率测定。18只兔用于ERG、光镜和透射电镜检查以评价药物的视网膜毒性。结果道诺霉素在玻璃体内的半衰期为145.5min;道诺霉素脂质体在眼内的头两天清除较快,但在14d仍可测出平均浓度为0.64μg/ml。电镜观察表明道诺霉素剂量超过5μg,或其脂质体超过20μg出现光感受器毒性。提示道诺霉素脂质体能明显延长有效浓度时间并减低眼内毒性反应。
Daunomycin liposomes were prepared by reverse phase evaporation. The encapsulation rate of liposomes was 31.6%, the final concentration was 100μg / ml and the diameter was 60 ~ 125nm. The determination of doxorubicin and liposome vitrectomy in 24 rabbits was performed by fluorescence spectrophotometry. Eighteen rabbits were used for ERG, light and transmission electron microscopy to evaluate the retinal toxicity of the drug. Results The half-life of daunorubicin in the vitreous was 145.5min. The daunorubicin liposome cleared rapidly in the first two days in the eye, but the average concentration was 0.64μg / ml at 14d. Electron microscopy showed phototoxicity of daunorubicin at doses above 5 μg, or more than 20 μg at liposomes. Tip daunomycin liposomes can significantly extend the effective concentration of time and reduce intraocular toxicity.