Screening of Excipients for Lipid Based Drug Delivery Systems of Ibrutinib By Validated HPLC

Author(s): K. Anie Vijetha and M. Sunitha Reddy

Abstract: Ibrutinib is an anticancer drug which binds irreversibly to Bruton’s tyrosine kinase (BTK) receptor that binds to a cysteine residue and inhibits BTK active site. Ibrutinib is used for the treatment of mantle cell lymphoma. Mantle cell lymphoma is a fast-growing cancer which begins in the cells of immune system. A new HPLC method has been proposed for the quantification of Ibrutinib. A simple, rapid, accurate, sensitive, reproducible and feasible reverse-phase high-performance liquid chromatographic method (RP-HPLC) has been developed and validated for Ibrutinib and the developed method is applied to quantitatively assess the solubility of Ibrutinib in various oils and surfactants. The separation was achieved on a C18-reverse phase column (SunFire C18 5μm, 4.6×250mm column) using a mobile phase composed of Acetonitrile and 0.1% orthophosphoric acid solution in a ratio of 70:30 v/v at a flow rate of 1ml/min. The injection volume of 10μl and the wavelength is 286nm.The retention time of Ibrutinib was observed at 2.5 minutes. The method was validated for specificity, accuracy, precision, linearity, limit of detection (LOD), limit of quantification (LOQ) and robustness. LOD and LOQ were 0.376 μg/ml and 1.128 μg/ml, respectively. The calibration curve was linear in the concentration range of 2-32μg/ml with correlation coefficient of 0.9995. The proposed method is validated according to ICH guidelines Q2 (R1). Ibrutinib showed the highest solubility in Capryol 90 (56.4 mg/ml), Kolliphor EL (39.5 mg/ml) and Transcutol HP (65.7 mg/ml) at 25˚C.

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