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A nanocomposite material formed by benzofulvene polymer nanoparticles loaded with a potent 5-HT3 receptor antagonist (CR3124) |
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| Authors: | Andrea Cappelli Simone Galeazzi Iacopo Zanardi Valter Travagli Maurizio Anzini Raniero Mendichi Stefania Petralito Adriana Memoli Eugenio Paccagnini Walter Peris Antonio Giordani Francesco Makovec Massimo Fresta Salvatore Vomero |
| Affiliation: | 1. Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Università Degli Studi di Siena, Via A. Moro, 53100, Siena, Italy 2. Istituto per lo Studio delle Macromolecole (CNR), Via E. Bassini 15, 20133, Milan, Italy 3. Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza – Università di Roma, Piazzale Aldo Moro 5, 00185, Rome, Italy 4. Dipartimento di Biologia Evolutiva, Università di Siena, Via A. Moro, 53100, Siena, Italy 5. Rottapharm SpA, via Valosa di Sopra 9, 20052, Monza, Italy 6. Dipartimento di Scienze Farmacobiologiche, Università “Magna Gr?cia” di Catanzaro, Campus Universitario “Salvatore Venuta”, 88100, Germaneto, Catanzaro, Italy |
| Abstract: | Poly-BF3a, a new hydrophobic polymer obtained by spontaneous polymerization of 1-methylene-3-phenyl-1H-indene, was found to give nanoparticles characterized by favorable shape and dimensions. Poly-BF3a nanoparticles were loaded with CR3124, a potent 5HT3 antagonist, as a drug model by desolvation methods either in the absence or in the presence of polyethylene glycol (PEG1000) as a wetting agent. The SEM studies showed that the introduction of CR3124 into the preparation led to a variable degree of aggregation–cementation, which afforded a sort of nanocomposite material. In the absence of PEG1000, the drug molecule was found to stay in the amorphous state (DSC studies) when its percentage is not higher than 10% by weight. In vitro release experiments showed that the formation and stability of the dispersion as well as the drug release were remarkably affected by the presence of PEG1000, demonstrating its beneficial effect to the nanoparticle morphology and disaggregation. |
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