Tulbah Alaa S, Gamal Amr
Department of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt.
Saudi Pharm J. 2021 Dec;29(12):1449-1457. doi: 10.1016/j.jsps.2021.11.002. Epub 2021 Nov 11.
Lung cancer is the leading cause of cancer death. Many studies have shown the beneficial effects of Atorvastatin in decreasing the mortality risk and improving survival among patients with lung cancer. This research paper focuses on improving AVT cytotoxic activity and cellular uptake by developing mannitol microcarriers as a promising drug delivery system for lung cancer treatment and, studying the impact of improving inhalation deposition on the delivery and Dry Powder formulations efficiency. The AVT loaded mannitol (AM) microparticles (AVT-AM) formulation was prepared by spray drying and characterized for its physicochemical properties and aerodynamic deposition. The results revealed that the AVT-AM formulation has good flow properties and aerosol deposition with a particle size of 3418 nm ± 26.86. The formulation was also assessed in vitro for cytotoxicity effects (proliferation, apoptosis, and cell cycle progression) on A549 human lung adenocarcinoma. Compared with free AVT, the AVT-AM formulation has significantly higher cellular uptake and anti-cancer properties by disrupting cell cycle progression via either apoptosis or cell cycle arrest in the G2/M phase. This study shows that AVT loaded mannitol microcarriers may provide a potentially effective and sustained pulmonary drug delivery for lung cancer treatment.
肺癌是癌症死亡的主要原因。许多研究表明,阿托伐他汀在降低肺癌患者的死亡风险和提高生存率方面具有有益作用。本研究论文专注于通过开发甘露醇微载体来提高AVT的细胞毒性活性和细胞摄取,甘露醇微载体是一种有前景的用于肺癌治疗的药物递送系统,并研究改善吸入沉积对递送和干粉制剂效率的影响。通过喷雾干燥制备了负载AVT的甘露醇(AM)微粒(AVT-AM)制剂,并对其物理化学性质和空气动力学沉积进行了表征。结果显示,AVT-AM制剂具有良好的流动性质和气溶胶沉积,粒径为3418 nm±26.86。还在体外评估了该制剂对A549人肺腺癌的细胞毒性作用(增殖、凋亡和细胞周期进程)。与游离AVT相比,AVT-AM制剂通过凋亡或细胞周期阻滞在G2/M期破坏细胞周期进程,具有显著更高的细胞摄取和抗癌特性。本研究表明,负载AVT的甘露醇微载体可能为肺癌治疗提供一种潜在有效且持续的肺部药物递送方式。