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A novel melphalan polymeric prodrug: preparation and property study.
- Source :
-
Carbohydrate polymers [Carbohydr Polym] 2014 Oct 13; Vol. 111, pp. 928-35. Date of Electronic Publication: 2014 May 20. - Publication Year :
- 2014
-
Abstract
- The clinical application of melphalan (Me), an anticancer drug for the treatment of hematologic malignancies, has been limited due to its poor water solubility, rapid elimination and lack of target specificity. To solve these problems, O,N-carboxymethyl chitosan-peptide-melphalan conjugates were synthesized and characterized. All polymeric prodrugs showed satisfactory water solubility. It was found that the molecular weight of O,N-carboxymethyl chitosan (O,N-CMCS) and the peptide spacer played a crucial role in controlling the drug content, diameter and drug release properties of O,N-carboxymethyl chitosan-peptide-melphalan conjugates. The studies of in vitro drug release and cell cytotoxicity by MTT assay revealed that, employing the polymeric conjugation strategy and using the peptides glycylglycine (Gly-Gly) as a spacer, the conjugates have good cathepsin X-sensitivity and lower toxicity and the drug release behavior improved remarkably. In conclusion, O,N-carboxymethyl chitosan-peptide-melphalan conjugates could be promising prodrugs for anticancer application.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cell Line, Tumor
Cell Survival drug effects
Chitosan chemistry
Glycylglycine chemistry
Humans
Melphalan chemistry
Melphalan pharmacology
Multiple Myeloma drug therapy
Nanoparticles ultrastructure
Polymers chemistry
Prodrugs chemistry
Prodrugs pharmacology
Solubility
Antineoplastic Agents administration & dosage
Drug Carriers chemistry
Melphalan administration & dosage
Nanoparticles chemistry
Prodrugs administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1879-1344
- Volume :
- 111
- Database :
- MEDLINE
- Journal :
- Carbohydrate polymers
- Publication Type :
- Academic Journal
- Accession number :
- 25037433
- Full Text :
- https://doi.org/10.1016/j.carbpol.2014.04.062