Alhakamy Nabil A, Abdullah Samaa, Md Shadab, Ansari Akhalakur Rahman, Bhattamisra Subrat Kumar, Ibrahim Ibrahim M, Alahdal Hadil, Altamimi Abeer A, Shaik Rasheed A
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.
Center of Excellence for Drug Research Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia.
Heliyon. 2024 Jul 4;10(13):e34074. doi: 10.1016/j.heliyon.2024.e34074. eCollection 2024 Jul 15.
Empagliflozin (EMP) is known for its poor safety and efficacy profile due to its fast body distribution and poor solubility. Accordingly, an oral long-acting and floating/raft-forming nano gel was optimized to release coated EMP nanoparticles, and the released EMP nanoparticles showed enhanced dissolution compared to raw EMP particles. To repurpose EMP for cancer treatment, EMP shows anti-cancer and anti-inflammatory effects against cancer cells. EMP nanoparticles were characterized using FT-IR, PXRD, SEM, EMP encapsulation assay, and release studies. The raft-forming gel encapsulating the EMP was optimized and characterized. The EMP co-polymeric nanoparticles were studied to investigate EMP anti-cancer and anti-inflammatory activities against stomach cancer cells. The solubility of EMP nanoparticles was enhanced in 0.1 N HCl and pH 6.8 by 5 and 12 folds, respectively, compared to raw EMP powder. The particle size and zeta-potential values of improved EMP nanoparticles were 135.40 ± 18.60 nm, and -19.30 ± 0.80 mV, respectively. FT-IR, PXRD, SEM and TEM characterizations revealed polymeric coating of EMP particles. The study suggested that this optimized controlled-release raft-forming gel is a promising local oral approach against stomach cancer. The repurposing of EMP co-polymeric nanoparticles for stomach cancer and associated gastritis treatment was justified.
恩格列净（EMP）因其在体内分布迅速且溶解度差，安全性和有效性不佳而闻名。因此，优化了一种口服长效且具有漂浮/筏状形成的纳米凝胶，以释放包衣的恩格列净纳米颗粒，与未加工的恩格列净颗粒相比，释放出的恩格列净纳米颗粒的溶出度有所提高。为将恩格列净用于癌症治疗，恩格列净对癌细胞具有抗癌和抗炎作用。通过傅里叶变换红外光谱（FT-IR）、粉末X射线衍射（PXRD）、扫描电子显微镜（SEM）、恩格列净包封率测定和释放研究对恩格列净纳米颗粒进行了表征。对包封恩格列净的筏状形成凝胶进行了优化和表征。研究了恩格列净共聚物纳米颗粒对胃癌细胞的抗癌和抗炎活性。与未加工的恩格列净粉末相比，恩格列净纳米颗粒在0.1 N盐酸和pH 6.8中的溶解度分别提高了5倍和12倍。改进后的恩格列净纳米颗粒的粒径和zeta电位值分别为135.40±18.60 nm和-19.30±0.80 mV。FT-IR、PXRD、SEM和透射电子显微镜（TEM）表征显示恩格列净颗粒有聚合物包衣。该研究表明，这种优化的控释筏状形成凝胶是一种有前景的局部口服抗胃癌方法。将恩格列净共聚物纳米颗粒用于胃癌及相关胃炎治疗是合理的。
