Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles

Abstract

Phenazine is known to regroup planar nitrogen-containing heterocyclic compounds. It was used here to enhance the bioavailability of the biologically important compound iodinin, which is near insoluble in aqueous solutions. Its water solubility has led to the development of new formulations using diverse amphiphilic α-cyclodextrins (CDs). With the per-[6-desoxy-6-(3-perfluorohexylpropanethio)-2,3-di-O-methyl]-α-CD, we succeeded to get iodinin-loaded nanoformulations with good parameters such as a size of 97.9 nm, 62% encapsulation efficiency and efficient control release. The study presents an interesting alternative to optimizing the water solubility of iodinin by chemical modifications of iodinin.

Keywords:

• Iodinin
• solubility
• amphiphilic α-cyclodextrin
• nanoparticles
• encapsulation

Acknowledgements

Pr. Marc Le Borgne thanks Mr. Christophe Villard (Student Exchange Office of the Faculty of Pharmacy of Lyon) for his precious help. Dr. Florent Perret thanks Pr. Julien Leclaire for his financial help and Dr. Yves Chevalier from LAGEP laboratory for zeta sizer experiments. Pr. Stein O. Døskeland and Lars Herfindal thank Ing. Nina Lied Larsen for assistance with cell experiments.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The present work was supported by the “Partenariats Hubert Curien” (PHC) (Campus France, Programme Aurora, Grant Agreement No. 27460VC), by the Norwegian Research Council [Grant Agreement No. 213191/F11] and the Norwegian Cancer Society (Project no.: 4529447). Pr. Marc Le Borgne also thanks the “Institut français d’Oslo” for their support via the Åsgard Programme 2010. This scientific work was also supported by financial support from Rhône-Alpes region through an Explo’ra Sup scholarship (academic year 2012–2013).