| Preparation and evaluation of biodegradable microspheres containing a new potent osteogenic compound and new synthetic polymers for sustained release. | |
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MedLine Citation:
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PMID: 20227474 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Nobuo Umeki; Takayuki Sato; Masahiro Harada; Junko Takeda; Shuji Saito; Yasunori Iwao; Shigeru Itai |
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Publication Detail:
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Type: Journal Article Date: 2010-03-20 |
Journal Detail:
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Title: International journal of pharmaceutics Volume: 392 ISSN: 1873-3476 ISO Abbreviation: Int J Pharm Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-05-14 Completed Date: 2010-09-07 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7804127 Medline TA: Int J Pharm Country: Netherlands |
Other Details:
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Languages: eng Pagination: 42-50 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier B.V. All rights reserved. |
Affiliation:
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Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Shizuoka, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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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