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In vitro release of the mTOR inhibitor rapamycin from poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles.
Forrest, M Laird; Won, Chee-Youb; Malick, A Waseem; Kwon, Glen S.
Afiliación
  • Forrest ML; Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison, 777 Highland Avenue, Madison, WI 53705-2222, USA.
  • Won CY; Hoffmann-La Roche, Inc., Nutley, NJ, USA.
  • Malick AW; Hoffmann-La Roche, Inc., Nutley, NJ, USA.
  • Kwon GS; Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison, 777 Highland Avenue, Madison, WI 53705-2222, USA. Electronic address: gskwon@pharmacy.wisc.edu.
J Control Release ; 110(2): 370-377, 2006 Jan 10.
Article en En | MEDLINE | ID: mdl-16298448
An injectable formulation of rapamycin was prepared using amphiphilic block co-polymer micelles of poly(ethylene glycol)-b-poly(epsilon-caprolactone) (PEG-PCL). Drug-loaded PEG-PCL micelles were prepared by a co-solvent extraction technique. Resulting PEG-PCL micelles were less than 100 nm in diameter and contained rapamycin at 7% to 10% weight and >1 mg/mL. PEG-PCL micelles released rapamycin over several days, t50% 31 h, with no burst release; however, physiological concentrations of serum albumin increased the release rate 3-fold. Alpha-tocopherol, vitamin E, was co-incorporated into PEG-PCL micelles and increased the efficiency of rapamycin encapsulation. The addition of alpha-tocopherol also slowed the release of rapamycin from PEG-PCL micelles in the presence of serum albumin, t50% 39 h.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Sirolimus / Antibacterianos Idioma: En Revista: J Control Release Asunto de la revista: FARMACOLOGIA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Países Bajos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Sirolimus / Antibacterianos Idioma: En Revista: J Control Release Asunto de la revista: FARMACOLOGIA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Países Bajos