Document Detail


Enhancing alendronate release from a novel PLGA/hydroxyapatite microspheric system for bone repairing applications.
MedLine Citation:
PMID:  18979188     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: The goal of this study was to exploit the multifunction of PLGA based microsphere as efficient alendronate delivery and also as potential injectable cell carrier for bone-repairing therapeutics. MATERIALS AND METHODS: Novel poly (lactic-co-glycolic acid) (PLGA)-hybridizing -hydroxyapatite (HA) microspheres loaded with bisphosphonate-based osteoporosis preventing drugs, alendronate (AL), are prepared with solid/oil/water (s/o/w) or water/oil/water (w/o/w) technique. Macrophage resistance was evaluated by MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay, DNA assay and Live/dead staining, and osteoblast proliferation and maturation was assessed by MTT assay, Alkaline phosphatase (ALP) activity assay and Real time-PCR. RESULTS: In such fabricated AL laden PLGA/HA microspheric composites (abbreviated "PLGA/HA-AL"), the introduction of HA component has been proven capable of largely enhancing drug encapsulation efficiency especially when the single emulsion protocol is adopted. The in-vitro drug (AL) releasing profile of PLGA/HA-AL system was plotted basing over 30 days' data collection. It indicates a sustained releasing tendency despite a minimal burst at the very beginning. The in-vitro bone-repairing efficacy of PLGA/HA-AL system was first tested with macrophages that are identified as precursors of osteoclasts and potentially responsible for osteoporosis. The results indicated that the AL release significantly inhibited the growth of macrophages. Additionally, as a central executor for osteogenesis, osteoblasts were also treated with PLGA/HA-AL system in vitro. The outcomes confirmed that this controlled release system functions to improve osteoblast proliferation and also enables upregulation of a key osteogenic enzyme ALP. CONCLUSIONS: By pre-resisting osteoclastic commitment and promoting osteoblastic development in vitro, this newly designed PLGA/HA-AL controlled release system is promoting for bone-repairing therapeutics.
Authors:
Xuetao Shi; Yingjun Wang; Li Ren; Yihong Gong; Dong-An Wang
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-11-01
Journal Detail:
Title:  Pharmaceutical research     Volume:  26     ISSN:  0724-8741     ISO Abbreviation:  Pharm. Res.     Publication Date:  2009 Feb 
Date Detail:
Created Date:  2009-01-19     Completed Date:  2009-03-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  422-30     Citation Subset:  IM    
Affiliation:
School of Materials Science & Engineering, South China University of Technology, Guangzhou, 510641, People's Republic of China.
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MeSH Terms
Descriptor/Qualifier:
Alendronate / chemistry,  pharmacology*
Alkaline Phosphatase / metabolism
Bone Density Conservation Agents / chemistry,  pharmacology*
Bone Regeneration / drug effects*
Cell Proliferation / drug effects
Cells, Cultured
Chemistry, Pharmaceutical
Delayed-Action Preparations
Drug Carriers*
Drug Compounding
Durapatite / chemistry*
Emulsions
Humans
Kinetics
Lactic Acid / chemistry*
Macrophages / drug effects
Microspheres
Osteoblasts / drug effects,  enzymology
Osteogenesis / drug effects
Polyglycolic Acid / chemistry*
Solubility
Surface Properties
Chemical
Reg. No./Substance:
0/Bone Density Conservation Agents; 0/Delayed-Action Preparations; 0/Drug Carriers; 0/Emulsions; 0/polylactic acid-polyglycolic acid copolymer; 1306-06-5/Durapatite; 26009-03-0/Polyglycolic Acid; 50-21-5/Lactic Acid; 66376-36-1/Alendronate; EC 3.1.3.1/Alkaline Phosphatase

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


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