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Original Article

J App Pharm Sci. 2022; 12(12): 150-161


Ternary inclusion complex of docetaxel using ß-cyclodextrin and hydrophilic polymer: Physicochemical characterization and in-vitro anticancer activity

Preeti Tanaji Mane, Balaji Sopanrao Wakure, Pravin Shridhar Wakte.




Abstract
Cited by 1 Articles

Docetaxel, one of the highly effective anticancer drugs, cannot be delivered via the oral route to date due to lack of pharmacokinetic cooperation. Poor aqueous solubility of docetaxel is the major barrier for development of its oral formulation. So, the current research aspires to enhance its aqueous solubility with the aid of a complexation technique using ß-cyclodextrin. Therefore, binary and ternary complexes of docetaxel were prepared with ß-cyclodextrin and hydroxypropyl methylcellulose (HPMC) E5 by the freeze-drying technique. Different polymers were screened as ternary agents and HPMC E5 was selected for the final formulation based on its stability constant and complexation efficiency. When compared to pure docetaxel, both binary and ternary inclusion complexes demonstrated 12.77 and 17.02 times rise in aqueous solubility and 2.22- and 2.48-fold enhanced drug release, respectively. Differential scanning calorimetry, powder X-ray diffractometry, Fourier transform infrared, and scanning electron microscopic examinations all confirmed the complex formation. On MCF -7 cell lines, in-vitro anticancer activity investigations of the pure drug and its prepared complexes were carried out, with the results proving 1.66 times enhanced activity with complexes over docetaxel alone.

Key words: Keywords: Docetaxel, β-cyclodextrin, complexation, binary complex, ternary complex.






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