Pharmacokinetics and antitumor efficacy of paclitaxel-cyclodextrin complexes loaded in mucus-penetrating nanoparticles for oral administration

The authors report a novel approach for enhancing the oral absorption of paclitaxel (PTX) by encapsulation in poly(anhydride) nanoparticles (NPs) containing cyclodextrins and poly(ethylene glycol). Materials & methods: Formulations were prepared using the solvent displacement method. Subsequentl...

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Detalles Bibliográficos
Autores: Calleja, P. (Patricia)|||/items/ace0469f-1278-4224-ae64-5620cc933add, Espuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964c, Corrales, L. (Leticia)|||/items/25c2d48d-8ffb-42b9-adab-dd66b9660e88, Pio, R. (Rubén)|||/items/d5c409b3-dbed-4f0c-8bad-94c31e0e5a95, Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173
Tipo de recurso: artículo
Fecha de publicación:2014
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/37240
Acceso en línea:https://hdl.handle.net/10171/37240
Access Level:acceso abierto
Palabra clave:Oral chemotherapy
Pharmacokinetics
Antitumor efficacy
Paclitaxel
Poly(anhydride) nanoparticles
Cyclodextrins
Poly(ethylene glycol) 2000
Descripción
Sumario:The authors report a novel approach for enhancing the oral absorption of paclitaxel (PTX) by encapsulation in poly(anhydride) nanoparticles (NPs) containing cyclodextrins and poly(ethylene glycol). Materials & methods: Formulations were prepared using the solvent displacement method. Subsequently, pharmacokinetics and organ distribution assays were evaluated after oral administration into C57BL/6J mice. In addition, antitumor efficacy studies were performed in a subcutaneous tumor model of Lewis lung carcinoma. Results: PTX-loaded NPs displayed sizes between 190–300 nm. Oral NPs achieved drug plasma levels for at least 24 h, with an oral bioavailability of 55–80%. Organ distribution studies revealed that PTX, orally administered in NPs, underwent a similar distribution to intravenous Taxol® (Bristol-Myers-Squibb, NJ, USA). For in vivo antitumor assays, oral strategy maintained a slower tumor growth than intravenous Taxol. Conclusion: PTX orally administered in poly(anhydride) NPs, combined with cyclodextrins and poly(ethylene glycol), displayed sustained plasma levels and significant antitumor effect in a syngenic tumor model of carcinoma in mice.