Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel

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, alpha-tocopherol succinate (alpha TS)-based, nanostructured lipid carrier (NLCs; alpha TS-PTX-NLC) and PEGylated alpha TS-PTX-NLC (alpha TS-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. alpha TS-PTX-NLC and alpha TS-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.

Automated summary

This study aimed to develop PTX-loaded NLCs to improve ocular bioavailability, with formulations demonstrating desirable physicochemical properties and stability under refrigerated conditions.