Results
Title

Influence of Hydrophobic Dendrimer Core Structure on the Itraconazole Encapsulation Efficiency.

Authors

Elkin, Igor; Rabanel, Jean‐Michel; Hildgen, Patrice

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, 1H and 13C 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.

Subjects

ANTIFUNGAL agents; ITRACONAZOLE; TRIAZOLES; MASS spectrometry; FOURIER transform infrared spectroscopy

Publication

Macromolecular Chemistry & Physics, 2015, Vol 216, Issue 24, p2356

ISSN

1022-1352

Publication type

Academic Journal

DOI

10.1002/macp.201500211