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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preliminary in vivo studies of a new lecithin-based formulation of paclitaxel
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Preliminary in vivo studies of a new lecithin-based formulation of paclitaxel

机译：新型基于卵磷脂的紫杉醇制剂的体内初步研究

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摘要

Amorphous paclitaxel dissolves rapidly (1 mg mL~(-1)) in an isotonic aqueous dispersion of egg lecithin (5% w/w), a new biocompatible submicron drug carrier consisting of structured aggregates with average size 0.5 μm The solution is physically stable for at least 24 h and can be administered as an intravenous infusion. After a 5 h infusion in rabbits (0.66 mg kg~(-1) h~(-1)), changes in blood morphology were comparable to those observed in rabbits that received the commercial product Taxol~R . No changes in the enzyme profiles (alanine/aspartate aminotransferase or alkaline phosphatase) were observed. However, during infusion of the new formulation plasma concentration of paclitaxel (292 ±182 ngmL~(-1)) was lower than observed after Cremophor-containing Taxol~R (540 ± 262 ng mL~(-1)). This result may indicate that the tissue distribution is different for the two drug formulations. Daily intraperitoneal administrations (3 doses/day) in mice demonstrated that the new carrier solution was non-toxic and, relative to Taxol, the new formulation exhibited similar or less toxicity.
机译：非晶紫杉醇快速溶解（1 mg mL〜（-1））溶于卵磷脂（5％w / w）的等渗水分散液中，卵磷脂是一种新的生物相容性亚微米药物载体，由平均大小为0.5μm的结构化聚集体组成，该溶液具有物理稳定性持续至少24小时，可以静脉输注方式给药。在兔子（0.66 mg kg〜（-1）h〜（-1））中输注5 h后，血液形态的变化与接受商业产品Taxol_R的兔子所观察到的相当。没有观察到酶谱变化（丙氨酸/天冬氨酸转氨酶或碱性磷酸酶）。然而，在新配方的输注过程中，紫杉醇的血浆浓度（292±182 ngmL〜（-1））低于含Cremophor的Taxol_R后的血浆浓度（540±262 ngmL〜（-1））。该结果可能表明两种药物制剂的组织分布不同。小鼠每天腹膜内给药（3剂量/天）表明，新的载体溶液是无毒的，相对于紫杉醇，新制剂显示出相似或更低的毒性。

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