| Preparation and pharmacodynamics of stearic acid and poly (lactic-co-glycolic acid) grafted chitosan oligosaccharide micelles for 10-hydroxycamptothecin. | |
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MedLine Citation:
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PMID: 20420886 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Stearic acid (SA) and poly (lactic-co-glycolic acid) (PLGA) grafted chitosan oligosaccharide (SA-CSO-PLGA SCP) tripolymer was synthesized via the reaction between the carboxyl group of SA or PLGA with carboxylic side group, and the amine group of CSO in the presence of 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC). The degrees of amino-substitution for SA and PLGA were assayed through 2, 4, 6-trinitrobenzene sulfonic acid (TNBS) test and (13)C NMR spectrum, which were 8.15% and 5.82%, respectively; the critical micelle concentrations of SCP in PBS (pH 7.4) and deionized water (DI water) were about 34.9 and 14.5 microg/ml, respectively. Using 10-hydroxycamptothecin (HCPT) as a model drug, the drug-loaded micelles showed above 86% encapsulation efficiency, which not only enhanced the solubility of HCPT in aqueous medium markedly, but also protected the lactone ring of HCPT. Cellular uptakes of SCP micelles against A549, MCF-7 and HepG-2 tumor cells showed a faster cellular internalization. Comparing to the commercial HCPT injection, HCPT-loaded micelles showed higher cytotoxicities against A549, MCF-7 and HepG-2 cells. The increased folds were 22, 18 and 15, respectively. These results suggested the SCP could be applied as a carrier for hydrophobic drugs. |
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Authors:
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Yue-Yu Zhou; Yong-Zhong Du; Ling Wang; Hong Yuan; Jian-Ping Zhou; Fu-Qiang Hu |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-04-24 |
Journal Detail:
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Title: International journal of pharmaceutics Volume: 393 ISSN: 1873-3476 ISO Abbreviation: Int J Pharm Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-06-01 Completed Date: 2010-09-03 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: 143-51 Citation Subset: IM |
Copyright Information:
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2010 Elsevier B.V. All rights reserved. |
Affiliation:
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Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang Road, Nanjing 210009, PR China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents, Phytogenic
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chemistry,
metabolism,
pharmacology* Biological Transport Camptothecin / analogs & derivatives*, chemistry, metabolism, pharmacology Carbodiimides / chemistry Cell Survival / drug effects Chemistry, Pharmaceutical Chitosan / analogs & derivatives, chemical synthesis* Dose-Response Relationship, Drug Drug Carriers* Drug Compounding Drug Stability Hep G2 Cells Humans Hydrophobicity Kinetics Lactic Acid / chemical synthesis* Magnetic Resonance Spectroscopy Micelles* Particle Size Polyglycolic Acid / chemical synthesis* Solubility Stearic Acids / chemical synthesis* Technology, Pharmaceutical / methods |
| Chemical | |
Reg. No./Substance:
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0/1-ethyl-3-(3-(diethylamino)propyl)carbodiimide; 0/Antineoplastic Agents, Phytogenic; 0/Carbodiimides; 0/Drug Carriers; 0/Micelles; 0/Stearic Acids; 0/polylactic acid-polyglycolic acid copolymer; 26009-03-0/Polyglycolic Acid; 50-21-5/Lactic Acid; 57-11-4/stearic acid; 67656-30-8/10-hydroxycamptothecin; 7689-03-4/Camptothecin; 9012-76-4/Chitosan |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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