Chettupalli Ananda Kumar, Kar Nihar Ranjan, Iswariya V T, Panigrahy Uttam Prasad, Singh Laliteshwar Pratap, Roy Harekrishna, Urs Deepadarshan, V Muralidharan, Mandadi Sandhya Rani, Haque M Akiful, Rana Ritesh, Emran Talha Bin
Department of Pharmaceutical Siences, School of Pharmacy, Galgotias University, Greater Noida, Uttar Pradesh 203201, India.
Centurion University of Technology and Management, Odisha, India.
Nanotheranostics. 2025 Jan 1;9(1):1-19. doi: 10.7150/ntno.99271. eCollection 2025.
In treating type 2 diabetes, avoiding glucose reabsorption (glucotoxicity) and managing hyperglycemia are also important. A metabolic condition known as diabetes (type-2) is characterized by high blood sugar levels in comparison to normal Bilosomes (BLs) containing Dapagliflozin (Dapa) were formulated, optimized, and tested for oral therapeutic efficacy in the current investigation. Used the Box Behnken design to optimize the Dapa-BLs, formulated via a thin-film hydration technique. Bile salts (X1) concentration, edge activator (X2) in mg, and non-ionic surfactant (X3) were the independent variables. The Entrapment Efficiency (Y1), Particle size (PS), polydispersity index (PDI), and zeta potential (ZP), were selected as dependent variables. To get the optimal formula, use Design-Expert® software for numerical optimization. The optimal bilosomal formula was selected by boosting %EE, ZP (absolute value), and drug release while also considering decreasing PS and PDI. skin permeation, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM) were evaluate the optimized formulation. The pharmacodynamics activities of the optimized formula were examined on rats and compared to that of the oral Dapa solution. The optimized Dapa-BLs were shown a particle size of 155.36±2.48 nm and an entrapment efficiency of 86.37±2.6%. The SEM image showed a spherical particle with sharp boundaries. The drug release study revealed a significant enhancement in Dapa release (75.31 ± 2.68%) from Dapa -BLs as compared to drug solution (30.46 ± 3.64%). The results of the exvivo permeation and pharmacokinetic studies revealed a 4.49 times higher flux and 3.41 folds higher AUC than drug solution. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than drug solution. The results also showed marked improvement in biochemical parameters. Our findings suggested, the prepared Dapa loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.
在治疗2型糖尿病时，避免葡萄糖重吸收（糖毒性）和控制高血糖也很重要。一种称为2型糖尿病的代谢性疾病，其特征是与正常情况相比血糖水平较高。在当前研究中，制备、优化并测试了含有达格列净（Dapa）的双分子层脂质体（BLs）的口服治疗效果。采用Box Behnken设计优化通过薄膜水化技术制备的Dapa-BLs。胆盐（X1）浓度、边缘活化剂（X2，单位为mg）和非离子表面活性剂（X3）为自变量。包封率（Y1）、粒径（PS）、多分散指数（PDI）和zeta电位（ZP）被选为因变量。使用Design-Expert®软件进行数值优化以获得最佳配方。通过提高包封率百分比、ZP（绝对值）和药物释放，同时考虑降低粒径和多分散指数，来选择最佳双分子层脂质体配方。通过皮肤渗透、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和扫描电子显微镜（SEM）对优化后的制剂进行评估。在大鼠身上检测了优化配方的药效学活性，并与口服达格列净溶液进行比较。优化后的Dapa-BLs粒径为155.36±2.48 nm，包封率为86.37±2.6%。扫描电子显微镜图像显示为边界清晰的球形颗粒。药物释放研究表明，与药物溶液（30.46±3.64%）相比，Dapa从Dapa-BLs中的释放显著增强（75.31±2.68%）。体外渗透和药代动力学研究结果显示，通量比药物溶液高4.49倍，AUC比药物溶液高3.41倍。抗糖尿病活性结果表明，治疗效果比药物溶液有显著（P<0.05）提高。结果还显示生化参数有明显改善。我们的研究结果表明，所制备的载有达格列净的双分子层脂质体在糖尿病治疗效果方面是一种有效的给药方式。
Zotero 插件
