Lung carcinoma therapy using epidermal growth factor receptor‑targeted lipid polymeric nanoparticles co‑loaded with...

The rate of lung cancer in tuberculosis (TB) patients is 7 to 30% higher than that in healthy individuals. Conventional chemotherapy of lung cancer shows limited efficiency due to poor tumor tissue drug accumulation and nonspecific cytotoxicity. Epidermal growth factor receptor (EGFR) is a promising target, which is overexpressed in lung carcinomas. In the present study, EGFR‑targeted nanoparticles were constructed and co‑delivered cisplatin (CDDP) and doxorubicin (DOX) for lung cancer therapy. In the present research, EGF‑PEG‑DSPE was synthesized. Then, EGFR‑targeted lipid polymeric nanoparticles (LPNs) were fabricated, which consisted of a CDDP‑loaded hybrophobic polymeric core, a DOX‑loaded phospholipid layer, and an outer layer of EGF‑PEG‑DSPE ligand. The particle size, ζ potential, stability, release behavior of LPNs were characterized. The antitumor ability of LPNs were assessed in vitro and in vivo. EGFR‑targeted LPNs loaded with CDDP and DOX (EGF C/D LPNs) had a size of 141.6 nm, and could encapsulate over 80% of feed drugs. Dual drug‑loaded LPNs showed synergistic effects with a combination index (CI) of 0.57. EGF C/D LPNs showed the smallest tumor volume (253 mm3), with a tumor inhibition ratio of 74.5%. In summary, EGF C/D LPNs were stable and released the drugs in a sustained manner. In vitro and in vivo studies revealed that EGF C/D LPNs exhibited improved anticancer activity along with lower toxicity. These results indicated the best efficiency of EGF C/D LPNs for lung carcinoma therapy.