The management of retinoblastoma (RB) involves the use of invasive treatment regimens. Paclitaxel (PTX), an effective antineoplastic compound used in the treatment of a wide range of malignant tumors, poses treatment challenges due to systemic toxicity, rapid elimination, and development of resistance. The goal of this work was to develop PTX-loaded, α-tocopherol succinate (αTS)-based, nanostructured lipid carrier (NLCs; αTS-PTX-NLC) and PEGylated αTS-PTX-NLC (αTS-PTX-PEG-NLC) to improve ocular bioavailability. The hot homogenization method was used to prepare the NLCs, and repeated measures ANOVA analysis was used for formulation optimization. αTS-PTX-NLC and αTS-PTX-PEG-NLC had a mean particle size, polydispersity index and zeta potential of 186.2 ± 3.9 nm, 0.17 ± 0.03, −33.2 ± 1.3 mV and 96.2 ± 3.9 nm, 0.27 ± 0.03, −39.15 ± 3.2 mV, respectively. The assay and entrapment efficiency of both formulations was >95.0%. The NLC exhibited a spherical shape, as seen from TEM images. Sterilized (autoclaved) formulations were stable for up to 60 days (last time point checked) under refrigerated conditions. PTX-NLC formulations exhibited an initial burst release and 40% drug release, overall, in 48 h. The formulations exhibited desirable physicochemical properties and could lead to an effective therapeutic option in the management of RB.

中文翻译：

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基于α-生育酚琥珀酸酯的纳米结构脂质载体的开发用于紫杉醇的递送

视网膜母细胞瘤 (RB) 的治疗涉及使用侵入性治疗方案。紫杉醇 (PTX) 是一种有效的抗肿瘤化合物，用于治疗多种恶性肿瘤，但由于全身毒性、快速消除和耐药性的发展，给治疗带来了挑战。这项工作的目标是开发载有 PTX 的、基于α-生育酚琥珀酸酯 (αTS) 的纳米结构脂质载体（NLC；αTS-PTX-NLC）和聚乙二醇化的 αTS-PTX-NLC (αTS-PTX-PEG-NLC)以提高眼部生物利用度。采用热均质法制备 NLC，重复测量方差分析用于处方优化。αTS-PTX-NLC 和 αTS-PTX-PEG-NLC 的平均粒径、多分散指数和 zeta 电位分别为 186.2 ± 3.9 nm、0.17 ± 0.03、-33.2 ± 1.3 mV 和 96.2 ± 3.9 nm、0.27 ± 0.03、-分别为 39.15 ± 3.2 mV。两种制剂的测定和包封效率均 > 95.0%。从 TEM 图像可以看出，NLC 呈球形。灭菌（高压灭菌）的制剂在冷藏条件下可稳定长达 60 天（最后检查的时间点）。PTX-NLC 制剂在 48 小时内表现出初始突释和 40% 的药物释放。这些制剂表现出理想的物理化学特性，并可能成为 RB 管理中的有效治疗选择。