紫杉醇载药体系及其抗肿瘤活性和临床应用

紫杉醇是临床上常用的抗肿瘤药物,主要作用机制为促进细胞微管聚合并抑制微管解聚,导致细胞纺锤体失去正常功能,抑制肿瘤细胞的有丝分裂,进而诱导细胞凋亡,目前已被用于治疗卵巢癌、乳腺癌、肺癌等恶性肿瘤。紫杉醇难溶于水,临床上常采用聚氧乙烯蓖麻油和乙醇助溶,而聚氧乙烯蓖麻油易引起过敏反应。为提高紫杉醇在水中的溶解度,减少毒副作用的发生,并提高紫杉醇的抗肿瘤活性,国内外学者对紫杉醇的不同载药体系、制剂剂型及临床用药方式等进行了广泛的研究。现在,纳米技术与生物医学结合产生的纳米载药体系已经用于改善紫杉醇的水溶性和临床疗效。

Anti-Cancer Effects of Paclitaxel Delivery Systems and Their Clinical Applications

Paclitaxel is a cell cycle-specific agent that binds with high-affinity to microtubules,stabilizing and enhancing tubulin polymerization and suppressing spindle microtubule dynamics.This effectively inhibits mitosis,motility,and intracellular transport within cancerous cells,leading to apoptotic cell death.Paclitaxel is widely used for the treatment of breast,lung,and advanced ovarian cancers.Because paclitaxel has low solubility in water,Cremophor and ethanol are used to increase paclitaxel aqueous solubility in clinical applications.However,Cremophor EL-containing paclitaxel formulation causes severe hypersensitivity reactions in humans.To address this problem,a variety of formulations and delivery systems are being investigated to administer paclitaxel in a more safe and convenient manner.In this account,a review of the various formulations of paclitaxel and their clinical applications was provided.