Possibility of using the B-cyclodextrin in the formation of a complex with darunavir

KOGAWA, A.C.; ZOPPI, A.; LONGHI, M. R.; NUNES SALGADO, H.R.

Campos do Jordão

Encuentro; XII Encuentro de la Sociedad Brasilera de Materiales (SBPMat); 2013

Darunavir (DRV), a protease inhibitor used in the treatment of HIV infection, presents low water solubility and poor bioavailability, therefore require administration in relatively high doses for a successful therapeutic effect [1]. The B-cyclodextrin (B-CD) is an excipient and it has been used in the development of pharmaceuticals, particularly because of complexing properties, which provide increased solubility and consequent increase in the rate of dissolution of poorly soluble drugs [2]. Therefore, the complexation of DRV to B-CD was investigated and their formation was proven through the techniques of thermogravimetry (TG) and infrared (IR). Variations in the physicochemical properties of host-molecules can be identified by analytical methods, which can detect the formation of complexes. To characterize the formation of inclusion complex (IC) in the solid state can be used thermal methods and IR spectroscopy [2]. The analysis of IR showed different spectra of DRV, physical mixture of DRV with B-CD (PM) and supposed IC, showing great chances of complexation occurred successfully (Figure 1a). TG spectra of the DRV, B-CD, PM and IC were different, confirming the formation of a new compound (Figure 1b). The IC showed decomposition temperature equal to the free drug, so the complexation does not affect the characteristics of DRV. The use of the CDs in pharmaceutical systems is a reality, thus it is expected that the application of this material expand considerably in the next years. Acknowledgments: CNPq, FAPESP, CAPES, PADC/FCF/FUNDUNESP. References: [1] A. Sosnik, D.A. Chiappetta, A.M. Carcaboso, Drug delivery systems in HIV pharmacotherapy: What has been done and the challenges standing ahead, J Control Release. 138 (2009) 2-15. [2] M.A. Lyra, L.D.S. Alves, D.A.F. Fontes, J.L. Soares-Sobrinho, P.J. Rolin-Neto, Ferramentas analíticas aplicadas à caracterização de complexos de inclusão fármaco-ciclodextrina, Rev. Ciênc. Farm. Básica Apl. 31 (2010) 117-124.