Influence of Hydrophobic Dendrimer Core Structure on the Itraconazole Encapsulation Efficiency. Issue 24 (17th November 2015)

• Record Type: Journal Article
• Authors: Elkin, Igor; Rabanel, Jean‐Michel; Hildgen, Patrice
• Is Part Of: Macromolecular chemistry and physics. Volume 216:Issue 24(2015:Dec.)
• Page Start: 2356
• Page End: 2367
• Publication Date: 2015-11-17
• Subjects: cytotoxicity studies -- dendrimer core flexibility -- in silico simulations -- itraconazole encapsulation -- polyester‐co‐polyether dendrimers; Polymers -- Periodicals; Polymerization -- Periodicals; Synthetic products -- Periodicals; Macromolecules -- Periodicals; 547.7
• DOI: 10.1002/macp.201500211
• Languages: English
• ISSNs: 1022-1352

Abstract

Abstract : New polyester‐ co ‐polyether dendritic macromolecules of first generation characterized by different flexibility of their central part (core) are synthesized and proposed as simplified models of new drug encapsulation agents for itraconazole (ITZ), an antifongic agent. Chemical structures of obtained products are characterized by FTIR, UV–vis, 1 H and 13 C NMR, and GPC techniques, as well as by elemental analysis and mass spectrometry. The absence of cytotoxicity limitation for further applications in drug delivery is evidenced by the results of MTT assay on the murine macrophage cell line RAW‐262.7. To elucidate the role of hydrophobic core structure of dendrimers in the process of ITZ encapsulation, the in silico simulations with reduced model structures are performed. The results of studies in vitro and in silico are found consistent, suggesting that the drug encapsulation efficiency can be determined by the possibility of an effective bending of hydrophobic central core segments of dendrimer around ITZ molecule. Abstract : New polyester‐ co ‐polyether (PEPE) dendritic macromolecules of first generation with different central parts (cores) are synthesized and proposed as new encapsulation systems for itraconazole, an antifongic agent. Consistency obtained between results of experiments performed in real systems and in silico suggests that the drug encapsulation efficiency can be determined by the possibility of an effective bending of hydrophobic central core segments of dendrimer around ITZ molecule.