| Summary: | Abstract Background Lapatinib ditosylate, an efficient tyrosine kinase inhibitor for breast cancer, poses pharmacokinetic issues, hence developing its oral delivery system is troublesome. The poor aqueous solubility of this medicament is a key impediment in developing its successful formulation. So, the current study aims to improve water solubility of Lapatinib ditosylate by using complexation technique with β-cyclodextrin and a suitable ternary agent. Results Binary and ternary complexes of Lapatinib ditosylate were synthesized by means of kneading and lyophilization using β-cyclodextrin and PVP K30. As a ternary agent, various hydrophilic polymers, as well as organic acids, were assessed, and PVP K30 was chosen for the final formulation based on its stability constant and complexation efficiency. When compared to pure Lapatinib ditosylate, both inclusion complexes demonstrated improved solubility, and drug dissolution. Differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), Fourier transform infrared (FTIR), and scanning electron microscopic (SEM) techniques, all validated the complex formation. Docking studies picturized the geometry of Lapatinib ditosylate in β-cyclodextrin cavity. Using MCF-7 cell lines, investigation of anticancer activity of the pure drug and its synthesized complexes was carried out and the results revealed that the complexes had stronger anticancer activity than Lapatinib ditosylate alone. Conclusions Overall, it can be concluded that Lapatinib ditosylate complexation increased its aqueous solubility, resulting in its increased dissolution and in vitro anticancer activity in a breast cancer cell line.
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