Document Detail


What are determining factors for stable drug incorporation into polymeric micelle carriers? Consideration on physical and chemical characters of the micelle inner core.
MedLine Citation:
PMID:  17716772     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Partially benzyl-esterified poly(ethylene glycol)-b-poly(aspartic acid) (PEG-P(Asp(Bzl))) having different hydrophobic inner-core structure were synthesized and analyzed. We obtained two types of the block copolymers for formation of polymeric micelle drug carriers; one had an amide-bond ratio of 1:3 (alpha/beta) in the poly(aspartic acid) residues through alkaline hydrolysis, and the other one had 100% of the alpha-amide through acid hydrolysis. Subsequently, we prepared partially benzyl-esterified block copolymers with an esterification degree of 40 to 100% in the aspartic acid residue. Regarding camptothecin (CPT) incorporation into polymeric micelles, we evaluated effects that block copolymers' inner hydrophobic block structures have on CPT behavior. Regarding CPT-incorporation stability, PEG-P(alpha,beta-Asp(Bzl) block copolymers with the alpha and beta-amides were found to exhibit higher CPT-incorporation stability. Using fluorescent probes, we evaluated the properties of inner-core blocks such as hydrophobicity and mobility/rigidity, and the findings implied that stable CPT incorporation could be obtained by an adequate balance between the micelle inner core's hydrophobicity and the micelle inner core's rigidity or between the micelle inner core's hydrophobicity and steric configuration of the hydrophobic block chain.
Authors:
Tatsuhiro Yamamoto; Masayuki Yokoyama; Praneet Opanasopit; Akihiro Hayama; Kumi Kawano; Yoshie Maitani
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-07-29
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  123     ISSN:  1873-4995     ISO Abbreviation:  J Control Release     Publication Date:  2007 Oct 
Date Detail:
Created Date:  2007-09-28     Completed Date:  2007-11-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  11-8     Citation Subset:  IM    
Affiliation:
Yokoyama Project, Kanagawa Academy of Science and Technology, KSP East 404, Sakado 3-2-1, Takatsu-ku, Kawasaki, Kanagawa 213-0012, Japan.
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MeSH Terms
Descriptor/Qualifier:
Camptothecin / administration & dosage,  chemistry
Drug Carriers / administration & dosage,  chemistry*
Drug Stability
Lactates / administration & dosage,  chemistry
Micelles*
Polyethylene Glycols / administration & dosage,  chemistry
Polymers / administration & dosage,  chemistry*
Chemical
Reg. No./Substance:
0/Drug Carriers; 0/Lactates; 0/Micelles; 0/Polyethylene Glycols; 0/Polymers; 0/poly(lactic acid-ethylene glycol); 7689-03-4/Camptothecin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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