Document Detail


Preparation and evaluation of biodegradable microspheres containing a new potent osteogenic compound and new synthetic polymers for sustained release.
MedLine Citation:
PMID:  20227474     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In order to achieve the sustained release of 3-ethyl-4-(4-methylisoxazol-5-yl)-5-(methylthio) thiophene-2-carboxamide (BFB0261), a new potent osteogenic compound for the treatment of bone disorders, we prepared microspheres containing BFB0261 and newly synthesized three poly (D, L-lactic acid) (PLA), four poly (D, L-lactic acid-co-glycolic acid) (PLGA), and eight poly (D, L-lactic acid)-block-poly(ethylene glycol) (PLA-PEG) biodegradable polymers or copolymers, and evaluated the release pattern of BFB0261 from the microspheres in vitro and in vivo. The mean particle size of the microspheres, except for the microspheres constructed from PLA-PEG with a greater than 20% PEG component, was in the range of approximately 10-50 microm, and the preparations showed a spherical shape with a smooth surface. In an in vitro release study, the release of BFB0261 from PLA-1 (Mw: 36 kDa), PLAPEG9604H (PLA/PEG ratio: 96:4, Mw: 181 kDa), or PLAPEG8317 (PLA/PEG ratio: 83:17, Mw: 106 kDa) microspheres occurred in a zero-order manner with a slow release, and more than 50% of BFB0261 remained in each type of microsphere at 12 weeks after incubation. When the BFB0261 microspheres constructed from various polymers were intramuscularly administered to the rat femur, the microspheres constructed from PLA-1 or PLAPEG9604H were able to achieve a sustained release of BFB0261 at the injection site for 6 weeks. The present information indicates that microspheres constructed from PLA-1 or PLAPEG9604H may be feasible for bone engineering.
Authors:
Nobuo Umeki; Takayuki Sato; Masahiro Harada; Junko Takeda; Shuji Saito; Yasunori Iwao; Shigeru Itai
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Publication Detail:
Type:  Journal Article     Date:  2010-03-20
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  392     ISSN:  1873-3476     ISO Abbreviation:  Int J Pharm     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-05-14     Completed Date:  2010-09-07     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  42-50     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier B.V. All rights reserved.
Affiliation:
Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Shizuoka, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Biocompatible Materials / chemical synthesis,  chemistry*
Delayed-Action Preparations
Drug Carriers / chemical synthesis,  chemistry*
Drug Compounding
Female
Femur / drug effects,  metabolism
Fibula / drug effects,  metabolism
Isoxazoles / administration & dosage*,  chemistry,  pharmacokinetics
Microscopy, Electron, Scanning
Microspheres
Osteogenesis / drug effects*
Particle Size
Polymers / chemical synthesis,  chemistry*
Rats
Rats, Wistar
Solubility
Surface Properties
Thiophenes / administration & dosage*,  chemistry,  pharmacokinetics
Tissue Distribution
Chemical
Reg. No./Substance:
0/3-ethyl-4-(4-methylisoxazol-5-yl)-5-(methylthio)thiophene-2-carboxamide; 0/Biocompatible Materials; 0/Delayed-Action Preparations; 0/Drug Carriers; 0/Isoxazoles; 0/Polymers; 0/Thiophenes

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


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