| PEG-poly(amino acid) block copolymer micelles for tunable drug release. | |
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MedLine Citation:
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PMID: 20372992 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
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PURPOSE: To achieve tunable pH-dependent drug release in tumor tissues. METHODS: Poly(ethylene glycol)-poly(aspartic acid) [PEG-p(Asp)] containing 12 kDa PEG and pAsp (5, 15, and 35 repeating units) were prepared. Hydrazide linkers with spacers [glycine (Gly) and 4-aminobenzoate (Abz)] were introduced to PEG-p(Asp), followed by drug conjugation [doxorubicin (DOX)]. The block copolymer-drug conjugates were either reconstituted or dialyzed in aqueous solutions to prepare micelles. Drug release patterns were observed under sink conditions at pH 5.0 and 7.4, 37°C, for 48 h. RESULTS: A collection of six block copolymers with different chain lengths and spacers was synthesized. Drug binding yields were 13-43.6%. The polymer-drug conjugates formed <50 nm polymer micelles irrespective of polymer compositions. Gly-introduced polymer micelles showed marginal change in particle size (40 ± 10 nm), while the size of Abz-micelles increased gradually from 10 to 40 nm as the polymer chain lengths increased. Drug release patterns of both Gly and Abz micelles were pH-dependent and tunable. The spacers appear to play a crucial role in controlling drug release and stability of polymer micelles in combination with block copolymer chain lengths. CONCLUSION: A drug delivery platform for tunable drug release was successfully developed with polymer micelles possessing spacer-modified hydrazone drug-binding linkers. |
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Authors:
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Andrei Ponta; Younsoo Bae |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-04-06 |
Journal Detail:
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Title: Pharmaceutical research Volume: 27 ISSN: 1573-904X ISO Abbreviation: Pharm. Res. Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2010-10-22 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: United States |
Other Details:
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Languages: eng Pagination: 2330-42 Citation Subset: IM |
Affiliation:
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Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone, Lexington, Kentucky 40536, USA. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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