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Nanoparticles Based on Quaternary Ammonium Chitosan-methyl-ß-cyclodextrin Conjugate for the Neuropeptide Dalargin Delivery to the Central Nervous System: An In Vitro Study.
Migone, Chiara; Mattii, Letizia; Giannasi, Martina; Moscato, Stefania; Cesari, Andrea; Zambito, Ylenia; Piras, Anna Maria.
Afiliación
  • Migone C; Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.
  • Mattii L; Department of Clinical and Experimental Medicine, University of Pisa, 56126 Pisa, Italy.
  • Giannasi M; Interdepartmental Research Centre "Nutraceuticals and Food for Health", University of Pisa, 56100 Pisa, Italy.
  • Moscato S; Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.
  • Cesari A; Department of Clinical and Experimental Medicine, University of Pisa, 56126 Pisa, Italy.
  • Zambito Y; Interdepartmental Research Centre "Nutraceuticals and Food for Health", University of Pisa, 56100 Pisa, Italy.
  • Piras AM; Department of Chemistry and Industrial Chemistry, INSTM-University of Pisa Research Unit (UdR Pisa), University of Pisa, Via Moruzzi 13, 56124 Pisa, Italy.
Pharmaceutics ; 13(1)2020 Dec 22.
Article en En | MEDLINE | ID: mdl-33374997
ABSTRACT
Peptide oral administration is a hard goal to reach, especially if the brain is the target site. The purpose of the present study was to set up a vehicle apt to promote oral absorption of the neuropeptide dalargin (DAL), allowing it to cross the intestinal mucosal barrier, resist enzymatic degradation, and transport drugs to the brain after crossing the blood-brain barrier. Therefore, a chitosan quaternary ammonium derivative was synthesized and conjugated with methyl-ß-cyclodextrin to prepare DAL-medicated nanoparticles (DAL-NP). DAL-NP particle size was 227.7 nm, zeta potential +8.60 mV, encapsulation efficiency 89%. DAL-NP protected DAL from degradation by chymotrypsin or pancreatin and tripled DAL degradation time compared to non-encapsulated DAL. Use of DAL-NP was safe for either Caco-2 or bEnd.3 cells, with the latter selected as a blood-brain barrier model. DAL-NP could also cross either the Caco-2 or bEnd.3 monolayer by the transepithelial route. The results suggest a potential DAL-NP ability to transport to the brain a DAL dose fraction administered orally, although in vivo experiments will be needed to confirm the present data obtained in vitro.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Pharmaceutics Año: 2020 Tipo del documento: Article País de afiliación: Italia

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Pharmaceutics Año: 2020 Tipo del documento: Article País de afiliación: Italia