Development of a docetaxel micellar formulation using poly(ethylene glycol)–polylactide–poly(ethylene glycol) (PEG–PLA–PEG) with successful reconstitution for tumor targeted drug delivery

Docetaxel (DTX)-loaded polymeric micelles (DTBM) were formulated using the triblock copolymer, poly(ethylene glycol)–polylactide–poly(ethylene glycol) (PEG–PLA–PEG), to comprehensively study their pharmaceutical application as anticancer nanomedicine. DTBM showed a stable formulation of anticancer nanomedicine that could be reconstituted after lyophilization (DTBM-R) in the presence of PEG 2000 and D-mannitol (Man) as surfactant and protectant, respectively. DTBM-R showed a particle size less than 150 nm and greater than 90% of DTX recovery after reconstitution. The robustly formed micelles might minimize systemic toxicity due to their sustained drug release and also maximize antitumor efficacy through increased accumulation and release of DTX from the micelles. From the pharmaceutical development point of view, DTBM-R showing successful reconstitution could be considered as a potent nanomedicine for tumor treatment.

以三嵌段共聚物（triblock copolymer）聚乙二醇-聚乳酸-聚乙二醇（PEG–PLA–PEG）为载体材料，制备载多西他赛（Docetaxel，DTX）的聚合物胶束（DTBM），以全面研究其作为抗肿瘤纳米药物（nanomedicine）的药学应用。DTBM具备稳定的抗肿瘤纳米药物制剂属性，在以聚乙二醇2000（PEG 2000）作为表面活性剂、D-甘露醇（D-mannitol，Man）作为保护剂的条件下，经冻干后可复溶（复溶后制剂记为DTBM-R）。DTBM-R的粒径小于150 nm，复溶后多西他赛的回收率高于90%。该制备得到的稳定胶束可通过持续释药降低全身毒性（systemic toxicity），同时通过提升多西他赛在胶束中的蓄积与释放水平，最大化其抗肿瘤疗效（antitumor efficacy）。从药学开发视角来看，成功实现复溶的DTBM-R可被视为一种极具应用潜力的肿瘤治疗用纳米药物。