Cyclodextrin-Efavirenz Complexes Investigated by Solid State and Solubility Studies
This short paper investigates the solubilizing ability of various cyclodextrins with efavirenz as well as the formation of solid inclusion complexes of efavirenz with β-CD and γ-CD. (1) Background: Efavirenz is a non-nucleoside reverse transcriptase inhibitor used as first-line treatment for adult and pediatric human immunodeficiency virus type 1 infection (HIV-1). Belonging to class II of Biopharmaceutical Classification System (BCS), efavirenz is poorly water-soluble. Inclusion into cyclodextrins is a possible strategy for increasing its solubility. (2) Methods: Solubility modulation was investigated by the phase solubility method; inclusion of efavirenz with β- and γ-cyclodextrins was attempted by co-dissolution with co-precipitation; the precipitates were studied by DSC, FT-IR, powder X-ray diffraction and optical microscopy. (3) Results: Solid state analysis of the precipitates shows evidence of separate recrystallization of β-cyclodextrin and efavirenz, whereas in the case of γ-cyclodextrin, a single new phase was observed. (4) Conclusion: Results show that the cavity of β-cyclodextrin is too narrow to accommodate efavirenz and only γ-cyclodextrin, the largest of native cyclodextrins, is able to form a true inclusion complex with this bulky guest.