A liposomal delivery system was developed in an attempt to prolong ocular levels of 5-fluorouracil for glaucoma filtering surgery. The pharmacokinetics of the 5-fluorouracil liposomal delivery system were studied in normal pigmented rabbits with 5-fluorouracil labelled with carbon-14 (C-14). 14C 5-fluorouracil was incorporated into the liposomes at a concentration of 10 g/l and injected subconjunctivally in doses of 5 and 10 mg. Concentrations of 5-fluorouracil were assayed at 10 time intervals from 0.5 to 96 hours in cornea, sclera, and conjunctiva and at six time intervals from 0.5 to 12 hours in aqueous. Two peak concentrations were noted at approximately one and eight hours, with measurable levels present at 96 hours. This study demonstrates the ability of this liposomal delivery system to prolong levels of 5-fluorouracial in normal pigmented rabbits.
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机译：为了延长用于青光眼滤过手术的眼内5-氟尿嘧啶的水平，开发了脂质体递送系统。在具有色素14（C-14）标记的5-氟尿嘧啶的正常色素兔中研究了5-氟尿嘧啶脂质体递送系统的药代动力学。将14C 5-氟尿嘧啶以10 g / l的浓度掺入脂质体中，并以5和10 mg的剂量结膜下注射。在角膜，巩膜和结膜中以0.5到96小时的10个时间间隔，在水溶液中以0.5到12小时的6个时间间隔，测定5-氟尿嘧啶的浓度。在大约一小时和八小时时出现两个峰值浓度，在96小时时出现可测量的浓度。这项研究证明了这种脂质体递送系统能够延长正常色素兔体内5-氟尿嘧啶水平的能力。
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