Freeze dried Multicomponent Inclusion Complexes of Piperine with Cyclodextrin and Hydrophilic Polymers: Physicochemical Characterization and In vivo Anti-inflammatory Activity

In order to improve the physicochemical properties and anti-inflammatory activity of piperine (PIP), its multicomponent inclusion complexes were prepared with β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) in presence of a ternary component such as polyvinylpyrrolidone K30 (PVP) and poloxamer 188 (POLO) by lyophilization. The initial phase solubility studies were carried out for determination of the stability and complexation efficiency of the prepared complexes. The complexes were evaluated for the saturation solubility, drug content and in-vitro dissolution, and characterized using ATR-FTIR, DSC, XRPD and SEM. Phase solubility studies revealed that PIP-βCD and PIP-HPβCD complexes exhibited 1:1 stoichiometry. The ternary systems showed good solubilizing and dissolution efficiency than the binary systems. The ATR-FTIR and DSC analysis showed interaction of polymers with PIP and cyclodextrins whereas XRPD analysis revealed amorphization of the ternary complexes. The PIP-HPβCD-POLO ternary complex showed high solubility and improved dissolution than the binary complexes. The in vivo anti-inflammatory activity of the PIP-HPβCD-POLO ternary complex was found to be maximum than pure PIP. Overall results indicated that freeze dried PIP-HPβCD-POLO ternary system can enhance the anti-inflammatory activity of PIP than the binary complexes.