Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel.
Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel.
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DOI：
10.3390/pharmaceutics14051034
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发表时间：
2022-05-11
期刊：
影响因子：
5.4
通讯作者：
Majumdar, Soumyajit
中科院分区：
文献类型：
--
作者：
Marathe, Sushrut;Shadambikar, Gauri;Mehraj, Tabish;Sulochana, Suresh P.;Dudhipala, Narendar;Majumdar, Soumyajit
视网膜母细胞瘤(RB)的治疗包括侵入性治疗方案的使用。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产生，给治疗带来了挑战。本研究的目的是开发以α-生育酚琥珀酸酯(αTS)为载体的纳米脂质载体(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。采用热均质法制备纳米晶胶囊，采用重复测量方差分析进行处方优化。αTS-PTX-NLC和αTS-PTX-PEGNLC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、−39.15±3.2 mV。两种制剂的含量测定和包封率均为95.0%。从透射电子显微镜图像可以看出，NLC呈球形。灭菌(高压灭菌)配方在冷藏条件下最长可稳定60天(最后检查时间点)。PTX-NLC制剂在48h内具有初始的突释和40%的药物释放。该制剂具有良好的物理化学性质，可能为RB的治疗提供有效的选择。
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.
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影响因子：
3.4
作者：
Arnold, Yvonne E.;Imanidis, Georgios;Kuentz, Martin
通讯作者：
Kuentz, Martin
DOI：
10.3390/molecules26247538
发表时间：
2021-12-13
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Dudhipala N;Ettireddy S;Youssef AAA;Puchchakayala G
通讯作者：
Puchchakayala G
影响因子：
1.3
作者：
Choudhury, Hira;Gorain, Bapi;Pal, Tapan Kumar
通讯作者：
Pal, Tapan Kumar
影响因子：
5.2
作者：
Drago-Ferrante, Rosa;Santulli, Andrea;Vento, Renza
通讯作者：
Vento, Renza
影响因子：
4.7
作者：
Duhem, Nicolas;Danhier, Fabienne;Preat, Veronique
通讯作者：
Preat, Veronique