Dopamine delivery to the central nervous system (CNS) undergoes the permeability limitations of the -blood-brain barrier (BBB). Condensation of dopamine with neutral amino acids could afford potential prodrugs able to interact with the BBB endogenous transporters and easily enter the brain. To improve the bio-availability of the dopamine prodrug, 2-amino-N-[2-(3,4-dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide (DOPH), it was encapsulated in unilamellar liposomes of dimiristoylphosphatidylcholine (DMPC) and cholesterol. Vesicles were characterized by dynamic light scattering in order to evaluate their dimensions and vesicle stability, by zeta-potential measurements, by means of electronic microscopy after freeze-fracture and differential scanning calorimetry. The influence of vesicle composition on DOPH chemical and enzymatic stability was also evaluated. The formulated liposome suspensions were found to be stable, monodisperse systems with a negative zeta potential. From the obtained results, it is possible to conclude that, in studied samples, DOPH inclusion in liposomes offers the possibility of preventing photodegradation and of enhancing in vitro plasma stability. These studies suggest the potential of these formulations as a method to prevent DOPH chemical degradation and enzymatic metabolism.

Potential dopamine prodrug-loaded liposomes: preparation, characterization, and in vitro stability studies / Carafa, Maria; Marianecci, Carlotta; L., Di Marzio; V., De Caro; Giulia, Giandalia; Libero Italo, Giannola; Santucci, Eleonora. - In: JOURNAL OF LIPOSOME RESEARCH. - ISSN 0898-2104. - 20:3(2010), pp. 250-257. [10.3109/08982100903384129]

Potential dopamine prodrug-loaded liposomes: preparation, characterization, and in vitro stability studies

CARAFA, Maria;MARIANECCI, CARLOTTA;SANTUCCI, Eleonora
2010

Abstract

Dopamine delivery to the central nervous system (CNS) undergoes the permeability limitations of the -blood-brain barrier (BBB). Condensation of dopamine with neutral amino acids could afford potential prodrugs able to interact with the BBB endogenous transporters and easily enter the brain. To improve the bio-availability of the dopamine prodrug, 2-amino-N-[2-(3,4-dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide (DOPH), it was encapsulated in unilamellar liposomes of dimiristoylphosphatidylcholine (DMPC) and cholesterol. Vesicles were characterized by dynamic light scattering in order to evaluate their dimensions and vesicle stability, by zeta-potential measurements, by means of electronic microscopy after freeze-fracture and differential scanning calorimetry. The influence of vesicle composition on DOPH chemical and enzymatic stability was also evaluated. The formulated liposome suspensions were found to be stable, monodisperse systems with a negative zeta potential. From the obtained results, it is possible to conclude that, in studied samples, DOPH inclusion in liposomes offers the possibility of preventing photodegradation and of enhancing in vitro plasma stability. These studies suggest the potential of these formulations as a method to prevent DOPH chemical degradation and enzymatic metabolism.
2010
chemical stability; dopamine prodrug; enzymatic stability; liposomes
01 Pubblicazione su rivista::01a Articolo in rivista
Potential dopamine prodrug-loaded liposomes: preparation, characterization, and in vitro stability studies / Carafa, Maria; Marianecci, Carlotta; L., Di Marzio; V., De Caro; Giulia, Giandalia; Libero Italo, Giannola; Santucci, Eleonora. - In: JOURNAL OF LIPOSOME RESEARCH. - ISSN 0898-2104. - 20:3(2010), pp. 250-257. [10.3109/08982100903384129]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/229695
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