چکیده

Abstract Introduction: The receptor of human epidermal growth factor 2 (HER2) is highly expressed in HER2-positive breast cancer. Targeted therapy is required for improved therapeutic outcomes for HER2-positive breast cancers. Lapatinib is a small molecule inhibitor of both HER2 and EGFR. However, it has low oral absorption, which led to a high consumption dose and causes many side effects such as diarrhea, nausea and rash. Lapatinib exhibits strong hydrophobic properties, thus its clinical administration suffers from low solubility. Here, we aimed to encapsulate Lapatinib into Human Serum Albumin (HSA) nanoparticles for the treatment of HER2+ breast cancer in mice model. Materials and Methods: NAB technology has been used to load lapatinib into albumin nanoparticles. Based on the technology, Lapatinib and Phosphatidyl Choline (PC) (w/w 1:4) must be dissolved in a chloroform and ethanol mixture. The lapatinib solution will be added dropwise to the aqueous HSA solution and the mixture will be subjected to high shear forces to form a coarse emulsion. Final emulsification is prepared by passing the coarse emulsion through a Microfluidizer 6-14 times at 100–170 MPa. After evaporation by rotary vacuum to eliminate the organic solvent, the nanoparticles suspension is filtered by filter membranes (Millipore, 220 nm pore diameter), and the obtained nanoparticles are frozen at -80 °C, lyophilized and stored at 20 °C In powder form. Results: FTIR spectrum were obtained from Lapatinib, HSA and HAS-Lapatinib nanoparticles separately. The results were analyzed based on changes in peaks. We found that five hydrogen bonds and a covalent bond (O-S) formed were detected by FTIR. Conclusion: Our results demonstrated that Lapatinib can be effectively loaded into HAS nanoparticles. Based on FTIR analysis, binding of drug to the nanoparticles was associated to hydrogen bonding and a covalent linkage (O-S) between the drug and albumin.

کليدواژه ها

Lapatinib, Human Serum Albumin, NAB technology, FTIR, Nanoparticle

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مصطفی شوریان , 1400 , بررسی اتصال لاپاتینیب به نانوذرات آلبومین توسط FTIR , نخستین همایش بین المللی و سومین همایش ملی ریاضیات زیستی