Fenretinide (4-HPR), a synthetic retinoid with low toxicological profile, is endowed with high an-titumor activity. However, 4-HPR shows poor oral absorption due to its low solubility, and variable blood concentrations for a massive hepatic first pass effect. Here, we prepared nanoparticles (NPs) made of 4-ammoniunbutylstyrene random copolymer (P5) by the anti-solvent co-precipitation technique. The encapsulation led to an increase in drug apparent solubility of 1134 folds with a drug loading of 37%. The NPs showed an extended dissolution rate, a mean diameter of 249 nm, positive Zeta potential, and confirmed an anti-proliferative activity on neuroblastoma cells.
4-Ammoniumbutylstyrene Based-Nanoparticles for the Controlled Release of Fenretinide
Guendalina Zuccari;Eleonora Russo;Carla Villa;Silvana Alfei
2023-01-01
Abstract
Fenretinide (4-HPR), a synthetic retinoid with low toxicological profile, is endowed with high an-titumor activity. However, 4-HPR shows poor oral absorption due to its low solubility, and variable blood concentrations for a massive hepatic first pass effect. Here, we prepared nanoparticles (NPs) made of 4-ammoniunbutylstyrene random copolymer (P5) by the anti-solvent co-precipitation technique. The encapsulation led to an increase in drug apparent solubility of 1134 folds with a drug loading of 37%. The NPs showed an extended dissolution rate, a mean diameter of 249 nm, positive Zeta potential, and confirmed an anti-proliferative activity on neuroblastoma cells.
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