Experimental, molecular docking investigations and bioavailability study on the inclusion complexes of finasteride and cyclodextrins.

ABSTRACT: Finasteride (FIN) is a Class II candidate of the Biopharmaceutics Classification System (BCS). The lipophilic cavity of cyclodextrins (CyDs) enables it to construct a non-covalent inclusion complex with different insoluble drugs. Only ?-cyclodextrin (?-CyD) and hydroxypropyl-?-CyD (HP-?-CyD) have been previously examined with FIN. This study aimed to investigate the consistence of FIN with different kinds of ?-CyDs, including dimethyl-?-cyclodextrin (DM-?-CyD), carboxymethyl-?-cyclodextrin (CM-?-CyD), HP-?-CyD, sulfobutyl ether-?-cyclodextrin (SBE-?-CyD), and ?-CyD, by the coprecipitation method. The resultant inclusion systems were characterized by differential scanning calorimetry, infrared spectroscopy, X-ray diffractometry, and dissolution studies. Moreover, molecular docking for the selected inclusion systems was carried out to explore the suitable arrangements of FIN in the cavity of ?-CyD or its derivatives. The results suggested that the DM-?-CyD inclusion system gave the higher complexation efficiency for improvement in solubility of FIN and hence enhancement of its bioavailability. Pharmacokinetic parameters displayed a higher absorption rate and higher area under the curve of the FIN/DM-?-CyD inclusion complex when compared with the drug alone, which indicates an improvement in the absorption and bioavailability of FIN in the DM-?-CyD inclusion system.

SUBMITTER: Mady FM 

PROVIDER: S-EPMC5472428 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature