Mahmoud Tamer Mohamed, Abdelfatah Mohamed Mahmoud, Omar Mahmoud Mohamed, Hasan Omiya Ali, Wali Saad M, El-Mofty Mohamed S, Ewees Mohamed G, Salem Amel E, Abd-El-Galil Tarek I, Mahmoud Dina Mohamed
Pharmaceutics and Industrial Pharmacy Department, Al-Manara College for Medical Sciences, Maysan 62010, Iraq.
Department of Pharmaceutics, Faculty of Pharmacy, Nahda University, Beni Suef 62764, Egypt.
Pharmaceutics. 2025 Jan 7;17(1):72. doi: 10.3390/pharmaceutics17010072.
Liver cancer is a prevalent form of carcinoma worldwide. A novel chitosan-coated optimized formulation capped with irradiated silver nanoparticles (INops) was fabricated to boost the anti-malignant impact of rosuvastatin calcium (RC). Using a 2-factorial design, eight formulations were produced using the solvent evaporation process. The formulations were characterized in vitro to identify the optimal formulation (Nop). The FTIR spectra showed that the fingerprint region is not superimposed with that of the drug; DSC thermal analysis depicted a negligible peak shift; and XRPD diffractograms revealed the disappearance of the typical drug peaks. Nop had an entrapment efficiency percent (EE%) of 86.2%, a polydispersity index (PDI) of 0.254, a zeta potential (ZP) of -35.3 mV, and a drug release after 12 h (Q12) of 55.6%. The chitosan-coated optimized formulation (CS.Nop) showed significant mucoadhesive strength that was 1.7-fold greater than Nop. Physical stability analysis of CS.Nop revealed negligible alterations in VS, ZP, PDI, and drug retention (DR) at 4 °C. The irradiated chitosan-coated optimized formulation capped with silver nanoparticles (INops) revealed the highest inhibition effect on carcinoma cells (97.12%) compared to the chitosan-coated optimized formulation (CS.Nop; 81.64) and chitosan-coated optimized formulation capped with silver nanoparticles (CS.Nop.AgNPs; 92.41). The bioavailability of CS-Nop was 4.95-fold greater than RC, with a residence time of about twice the free drug. CS.Nop has displayed a strong in vitro-in vivo correlation with R 0.9887. The authors could propose that novel INop could serve as an advanced platform to improve oral bioavailability and enhance hepatic carcinoma recovery.
肝癌是全球范围内一种常见的癌症形式。制备了一种新型的壳聚糖包衣优化制剂，其表面覆盖有辐照银纳米颗粒（INops），以增强瑞舒伐他汀钙（RC）的抗恶性作用。采用二因素设计，通过溶剂蒸发法制备了八种制剂。对这些制剂进行体外表征以确定最佳制剂（Nop）。傅里叶变换红外光谱（FTIR）显示指纹区与药物的指纹区不重叠；差示扫描量热（DSC）热分析显示峰位移可忽略不计；X射线粉末衍射（XRPD）图谱显示典型的药物峰消失。Nop的包封率（EE%）为86.2%，多分散指数（PDI）为0.254，zeta电位（ZP）为 -35.3 mV，12小时后的药物释放率（Q12）为55.6%。壳聚糖包衣优化制剂（CS.Nop）显示出显著的粘膜粘附强度，比Nop高1.7倍。CS.Nop的物理稳定性分析表明，在4°C下，其体积收缩（VS）、ZP、PDI和药物保留率（DR）的变化可忽略不计。与壳聚糖包衣优化制剂（CS.Nop；81.64）和壳聚糖包衣银纳米颗粒优化制剂（CS.Nop.AgNPs；92.41）相比，辐照壳聚糖包衣银纳米颗粒优化制剂（INops）对癌细胞的抑制作用最高（97.12%）。CS-Nop的生物利用度比RC高4.95倍，驻留时间约为游离药物的两倍。CS.Nop显示出与R 0.9887的强体外-体内相关性。作者认为新型INop可作为一个先进的平台，以提高口服生物利用度并促进肝癌的恢复。
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