Dissolution improvement of binary solid dispersions of erlotinib prepared by one-step electrospray method

Abstract

Abstract Erlotinib hydrochloride, a selective tyrosine kinase inhibitor approved for treatment of non-small cell lung cancer firstly. Erlotinib classified as class II drugs in the Biopharmaceutical Classification System (BCS), which characterized by low solubility and high permeability. The aim of this study was to enhance the dissolution rate of this drug. The binary solid dispersions of erlotinib: PVP prepared at different ratios (1:3, 1:5, and 1:8) by electrospray technique. The characterization of formulations performed using differential scanning calorimetery (DSC), Fourier transform infrared spectroscopy (FT-IR) and dissolution rate test. The dissolution results showed that the dissolution rate of erlotinib from binary solid dispersions improved in comparison to pure drug. FTIR spectrum results showed that all peaks of erlotinib functional groups are also observable in the prepared solid dispersions. The FTIR results demonstrated that there was no interaction between drug and polymer. DSC thermograms of the prepared solid dispersions showed no drug-related peak, which is probably related to reduced crystallinity and drug amorphization. Based on the obtained results, it can be concluded that the erlotinib solid dispersion systems displayed improved dissolution rate compared to the pure drug. This will likely lead to increased drug bioavailability.