Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles.

Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Research Abstract Details 

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Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Abstract Text:

M Laird Forrest,Anni Zhao,Chee-Youb Won,A Waseem Malick,Glen S Kwon,

A solvent and Cremephor free formulation of the anticancer chemotherapeutic geldanamycin was prepared using amphiphilic block co-polymer micelles of poly(ethylene glycol)-b-poly(epsilon-caprolactone) (PEG-b-PCL). Although geldanamycin was not solubilized by PEG-b-PCL micelles, fatty acid prodrugs of geldanamycin were encapsulated in PEG-b-PCL micelles by a co-solvent extraction technique. Resulting PEG-b-PCL micelles were <120 nm in diameter and solubilized >20% w/w geldanamycin prodrugs increasing aqueous solubility to >2 mg/mL. PEG-b-PCL micelles released the geldanamycin prodrugs over several days, t(1/2) 2.2 to 9.6 days. The free prodrugs hydrolyzed rapidly, t(1/2)<6 h, into the geldanamycin analogue 17-beta-hydroxyethylamino-17-demethoxygeldanamycin, which has high activity against MCF-7 breast cancer cells, IC(50) 240 nM.

Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Publishing Authors By Initials

ML Forrest,A Zhao,CY Won,AW Malick,GS Kwon,

For similar natural sciences: chemistry: chemistry, physical: solubility research abstracts see: natural sciences: chemistry: chemistry, physical: solubility research

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Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of controlled release : official journal o

VOLUME: 116

Page Numbers: 139-49

Journal Abbreviation:

ISSN: 0168-3659

DAY: 8

MONTH: 07

YEAR: 2006

Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 8607908

Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Keywords Mesh Terms:

KEYWORDS: Solubility

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. Information

Substance Name: geldanamycin

Registry Number: 30562-34-6

Grant and Affiliation Information for Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles.

AFFILIATION: Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison, 777 Highland Avenue, Madison, WI 53705-2222, USA.

Country: Netherlands

AGENCY: United States NIAID

GRANT: R01 AI-43346-08

ACRONYM: AI

MEDLINETA: J Control Release

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