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Article Dans Une Revue Journal of Biomedical Materials Research Part B: Applied Biomaterials Année : 2006

Busulfan loading into poly (alkyl cyanoacrylate) nanoparticles : physico-chemistry and molecular modeling

Résumé

The busulfan is an alkylating agent widely used for the treatment of haematological malignancies and nonmalignant disorders. For a long time, it has been available only in an oral form. This treatment leads to a wide variability in bioavailability and side effects such as the veino-occlusive disease. Thus, an intravenous formulation of busulfan-loaded nanoparticles may be considered as a major progress. This study deals with busulfan entrapment by nanoprecipitation into five different types of poly(alkyl cyanoacrylate) polymers. The polymers leading to the highest busulfan loading efficiencies were poly(isobutyl cyanoacrylate) (PIBCA) and poly(ethyl cyanoacrylate). Molecular modeling along with energy minimization process was employed to identify the nature of the interactions occurring between busulfan and PIBCA. Further, optimization studies enabled to obtain PIBCA nanoparticles displaying busulfan loading ratios equal to 5.9% (w/w) together with nanoparticle yields of 71% (w/w). Since busulfan is a highly reactive molecule, we performed 1H-NMR spectroscopy experiments showing that chemical integrity of the drug was preserved after loading into nanoparticles. The in vitro release studies under sink conditions, in water, or in rat plasma showed a fast release in the first 10 min followed by a slower one over 6 h. This phenomenon could be explained by the semi-polar characteristics of busulfan. © 2006 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006

Dates et versions

hal-00142889 , version 1 (23-04-2007)

Identifiants

Citer

Anne-Magali Layre, Patrick Couvreur, Hélène Chacun, C. Aymes-Chodur, Nour-Eddine Ghermani, et al.. Busulfan loading into poly (alkyl cyanoacrylate) nanoparticles : physico-chemistry and molecular modeling. Journal of Biomedical Materials Research Part B: Applied Biomaterials, 2006, 79B (2), pp.254-262. ⟨10.1002/jbm.b.30536⟩. ⟨hal-00142889⟩
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