A novel polyamidoamine dendrimer based nano-carrier for oral delivery of imatinib

• Published in: Journal of polymer research 2022-12, Vol.29 (12), Article 523
• Main Authors: Fakhari, Shabnam, Jamzad, Mina, Nouri, Azita, Arab-Salmanabadi, Samira, Falaki, Foujan
• Format: Article
• Language: English
• Subjects: Calorimetry; Cancer; Care and treatment; Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Colorectal cancer; Differential scanning calorimetry; Drug carriers; Drug delivery systems; Drugs; Entrapment; Folic acid; Health aspects; In vitro methods and tests; Industrial Chemistry/Chemical Engineering; Lung cancer; Original Paper; Pharmacology; Photon correlation spectroscopy; Physiological aspects; Polyethylene glycol; Polymer Sciences; Polyols; Scanning electron microscopy; Spectrum analysis; Sustained release; Vehicles; Zeta potential
• ISSN: 1022-9760; 1572-8935
• DOI: 10.1007/s10965-022-03359-x

Designing and developing efficient and non-toxic drug delivery systems is an exciting subject in pharmacology and cancer therapy. In this study, we have developed a nano-carrier based on the third generation of polyamidoamine (PAMAM-G3) dendrimer, grafted with polyethylene glycol (PEG 4000) and folic acid (FA) for oral delivery of Imatinib (IM) with sustained release. The synthesized drug carrier and the manufactured nano-complexes (two different amounts of IM encapsulated by the drug carrier) were characterized using FTIR and 1 HNMR spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), dynamic light scattering (DLS), and zeta potential analysis. The SEM images showed a typical smooth brittle structure for nano-complexes and, DSC thermograms confirmed the purity and integrity of both formulations. The average size of nano-complexes using DLS analysis was estimated to be around 100 nm with a zeta potential of + 0.2 mV. The drug loading efficiency and the drug release of nano-complexes were also studied in-vitro at pH 7.4 using UV–Vis spectroscopy. The manufactured nano carrier showed efficient entrapment of IM drug, and a sustained release was observed for nano-complexes in physiological conditions. Both formulations were effective against the human colorectal cancer cell line (SW480) and the human lung cancer cell line (A549) in the in-vitro cellular growth inhibition method. The best result was acquired against the cell line SW480 with the IC 50 value of 38.88 ± 0.13 (μg.mL −1 ).