Comparative pharmacokinetics and tissue distribution analysis of systemically administered 17-ß-estradiol and its metabolites in vivo delivered using a cationic nanoemulsion or a peptide-modified nanoemulsion system for targeting atherosclerosis.
J Control Release
; 180: 117-24, 2014 Apr 28.
Article
em En
| MEDLINE
| ID: mdl-24556419
The primary objective of this study was to compare the biodistribution and pharmacokinetic profile of 17-ß-estradiol (17-ßE) on systemic delivery using either the cationic or the CREKA-peptide-modified (Cysteine-Arginine-Glutamic-acid-Lysine-Alanine) omega-3-fatty acid oil containing nanoemulsion system in vivo in the wild type C57BL/6 mice. Higher blood concentrations of 17-ßE, higher accumulation in the tissues of interest - heart and aorta, and higher accumulation within the other tissues - liver and kidney was observed on delivering 17-ßE using the CREKA-peptide-modified nanoemulsion system (AUClast in plasma - 263.89±21.81min*%/injected dose/ml) as compared to the cationic nanoemulsion (AUClast in plasma - 20.2±1.86min*%/injected dose/ml) and solution form (AUClast in plasma - 44.9±1.24min*%/injected dose/ml) respectively. Both, the cationic nanoemulsion and the CREKA-peptide-modified nanoemulsion showed a higher relative targeting efficiency of 4.57 and 4.86 respectively for 17-ßE than the relative targeting efficiency of 1.78 observed with the solution form. In conclusion, since the maximum exposure (highest AUClast for plasma and tissues) for 17-ßE was observed with the CREKA-peptide-modified nanoemulsion system, the study shows that CREKA-peptide-modified nanoemulsion system was the most suitable vehicle for systemic delivery of 17-ßE in the wild type C57BL/6 mice.
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Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Oligopeptídeos
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Portadores de Fármacos
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Ácidos Graxos Ômega-3
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Emulsões
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Estradiol
Limite:
Animals
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article