Rawat Aruna, Chauhan Samrat, Singh Rahul Pratap, Gupta Sumeet, Jhawat Vikas
Department of Pharmaceutical Science, School of Healthcare and Allied Science, GD Goenka University, Gurugram, Haryana, India.
Chitkara College of Pharmacy, Chitkara University, Patiala, Punjab, India.
Drug Dev Ind Pharm. 2025 Jul 2:1-18. doi: 10.1080/03639045.2025.2525952.
This study aimed to develop and optimize Telmisartan-Curcumin Solid Dispersion Nanoparticles (SDNs) to improve the management of diabetic nephropathy by enhancing Telmisartan's solubility and release rate.
A Box-Behnken design was used to optimize the formulation with critical excipients PVP VA S630 and Poloxamer 407. Pre-formulation studies assessed Telmisartan's solubility and lipophilic nature. The optimized formulation (TLS-15) was evaluated for solubility, drug release, particle size, zeta potential, and in vitro release. A comparison was made with a formulation without Curcumin (TLS-15 WC). TEM imaging and release kinetics analysis were conducted.
The optimized formulation (TLS-15) demonstrated significantly improved solubility (4.801 μg/ml) and drug release (99.68%) with an appropriate particle size (303.5 nm) and zeta potential (-12.17 mV). TLS-15 WC exhibited lower values for solubility (4.74 μg/ml), drug release (98.3%), particle size (291.2 nm), and zeta potential (-25.4 mV). TEM revealed uniformly distributed spherical nanoparticles. TLS-15 showed a 99.54% release after 6 hours, compared to 98.3% for TLS-15 WC, following first-order release kinetics (R = 0.9934).
The study successfully developed and optimized Telmisartan-Curcumin SDNs, enhancing Telmisartan's solubility and release. Curcumin played a critical role in boosting the therapeutic potential of the formulation. While challenges remain with stability and manufacturing, the formulation shows promise for improving bioavailability and efficacy in diabetic nephropathy treatment. However, additional studies are needed to validate its effectiveness.
本研究旨在开发并优化替米沙坦 - 姜黄素固体分散纳米粒（SDNs），通过提高替米沙坦的溶解度和释放速率来改善糖尿病肾病的治疗。
采用Box - Behnken设计，以关键辅料聚乙烯吡咯烷酮VA S630和泊洛沙姆407优化制剂配方。处方前研究评估了替米沙坦的溶解度和亲脂性。对优化后的制剂（TLS - 15）进行溶解度、药物释放、粒径、zeta电位及体外释放评估。与不含姜黄素的制剂（TLS - 15 WC）进行比较。进行了透射电子显微镜（TEM）成像和释放动力学分析。
优化后的制剂（TLS - 15）表现出显著提高的溶解度（4.801μg/ml）和药物释放率（99.68%），粒径适宜（303.5nm），zeta电位为（ - 12.17mV）。TLS - 15 WC的溶解度（4.74μg/ml）、药物释放率（98.3%）、粒径（291.2nm）和zeta电位（ - 25.4mV）较低。TEM显示纳米粒呈均匀分布的球形。TLS - 15在6小时后释放率为99.54%，而TLS - 15 WC为98.3%，符合一级释放动力学（R = 0.9934）。
本研究成功开发并优化了替米沙坦 - 姜黄素SDNs，提高了替米沙坦的溶解度和释放率。姜黄素在增强制剂的治疗潜力方面发挥了关键作用。尽管在稳定性和生产方面仍存在挑战，但该制剂在改善糖尿病肾病治疗的生物利用度和疗效方面显示出前景。然而，需要进一步研究来验证其有效性。
