In vitro evaluation of PLA nanoparticles containing a lipophilic drug in water-soluble or insoluble form.
Int J Pharm
; 278(1): 133-41, 2004 Jun 18.
Article
en En
| MEDLINE
| ID: mdl-15158956
Cloricromene (AD6), an anti-ischemic drug, is rapidly metabolised into a stable and active metabolite (cloricromene acid, AD6-acid) poorly soluble in water and less lipophilic than cloricromene. The aim of this study was to evaluate which of the two forms has more possibility to be efficiently encapsulated in nanoparticles based on poly(D,L-lactide) and prepared using the nanoprecipitation method. Increasing the theoretical loading of AD6, an increase in drug actual loading and in the mean particle size occurred, while no formation of nanoparticles was observed when the highest theoretical loading (50 mg) was employed. Changing the pH of the aqueous phase the drug content dramatically increased. However, at a pH value of 11 a more rapid hydrolysis of AD6 occurred. When AD6-acid was embedded in the nanoparticles, suitable results concerning both drug content and encapsulation efficiency were achieved. A good control in the release of AD6 from the AD6-loaded nanoparticles was observed while the liberation of AD6-acid from the AD6-acid-loaded nanoparticles was faster than the dissolution of the AD6-acid free. These results confirm that the most easy encapsulable form in nanoparticles is AD6-acid probably owing to its poor water solubility. Further studies will be carried out in order to evaluate if the increase in the liberation of AD6-acid by nanoencapsulation may have outcomes in its bioavaibility in vivo.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Poliésteres
/
Agua
/
Cromonar
/
Nanotecnología
/
Lípidos
Idioma:
En
Revista:
Int J Pharm
Año:
2004
Tipo del documento:
Article
País de afiliación:
Italia
Pais de publicación:
Países Bajos