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首页> 外文期刊>Journal of chemotherapy >Non-invasive endotracheal delivery of paclitaxel-loaded alginate microparticles
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Non-invasive endotracheal delivery of paclitaxel-loaded alginate microparticles

机译:紫杉醇海藻酸盐微粒的非侵入性气管内递送

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摘要

Aerosolized chemotherapeutics leads to higher, localized and continuous concentrations of active agents in lung tissue with lower side effects for other organs. The present study was performed on jugular vein cannulated rats which endothracheally received 4 mg/kg of free paclitaxel powder (Free-PTX), paclitaxel-loaded alginate microparticles (PTX-ALG-MPs) and i.v. paclitaxel (Anzatax (R)). Pharmacokinetic parameters for Free-PTX and PTX-ALG-MPs contain higher AUC, mean residence time (MRT), half-life and bioavailability, with lower elimination constant (k(e)). Statistical analysis showed that the amount of paclitaxel per gram of lung tissue after 0.5, 6 and 24 h after administration of Free-PTX was lower than PTX-ALG-MPs. Lung tissue AUC for Free-PTX was lower than PTX-ALG-MPs. According to the obvious advantages obtained, such as dose lowering and increasing paclitaxel residence time and half-life. It should be noted that cell cytotoxicity test on normal airway cell lines was not examined in this study but due to previous reports on safety of inhaled paclitaxel, it can be suggested that pulmonary delivery of paclitaxel can be a useful non-invasive route of administration compared with i.v administration.
机译:气雾化化学疗法导致肺组织中活性剂的浓度更高,局部且连续不断,而对其他器官的副作用则更低。本研究是在颈静脉插管的大鼠上进行的,该大鼠在气管内接受了4 mg / kg的游离紫杉醇粉(Free-PTX),载有紫杉醇的藻酸盐微粒(PTX-ALG-MPs)和i.v.。紫杉醇(Anzatax(R))。 Free-PTX和PTX-ALG-MP的药代动力学参数包含较高的AUC,平均停留时间(MRT),半衰期和生物利用度,且消除常数较低(k(e))。统计分析表明,在给予Free-PTX后0.5、6和24小时,每克肺组织紫杉醇的含量低于PTX-ALG-MPs。 Free-PTX的肺组织AUC低于PTX-ALG-MPs。根据获得的明显优势,例如降低剂量和增加紫杉醇的停留时间和半衰期。应当指出的是,这项研究并未对正常气道细胞系进行细胞毒性试验,但由于先前有关吸入紫杉醇安全性的报道,可以建议将紫杉醇经肺部给药可作为一种有用的非侵入性给药途径与静脉注射管理。

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