DOI: 10.1021/acsomega.6c03082 ISSN: 2470-1343

Mixed Polymeric Micelles for Paclitaxel Delivery: Preparation and Characterization

Gisele L. Maia, Anna Carolina S. Sousa, Marina X. Teixeira, Angelo Malachias, Maria Victoria H. Machado, Maria Betânia F. Marques, Caroline M. R. Oda, André L. B.de Barros, Elaine A. Leite

Abstract

To address the limitations of commercial vehicles for paclitaxel (PTX) delivery, this study investigated mixed micelles as a novel delivery system for this drug. By incorporating PCL5000-PEG5000 into DSPE-PEG2000 at 99.5:0.5 and 99:1 molar ratios, we aimed to enhance drug loading and biocompatibility. The resulting systems were characterized using a range of physicochemical and biological characterization. The system achieved a low critical micelle concentration (CMC) of 1.9 × 10–5 mol/L, ensuring stability upon dilution. Optimized formulations (99.5:0.5 and 99:1 molar ratios) exhibited a small hydrodynamic diameter (∼11 nm) and near-neutral zeta potential. Small-range X-ray scattering (SAXS) analysis confirmed a spheroidal core–shell structure, where the addition of 0.5% PCL5000-PEG5000 increased drug loading capacity to 3.1 ± 0.05% w/w. Thermal analysis confirmed the successful integration of copolymers and their thermal stability. Notably, the cytotoxicity of this formulation was comparable to that of commercial formulations, while exhibiting negligible hemolysis (<2%), indicating a substantially improved safety profile compared with Cremophor-based vehicles. These findings highlight the potential of these mixed micelles as a biocompatible, high-capacity delivery platform for intravenous cancer chemotherapy.

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