Tan Mei-E, He Cheng-Hui, Jiang Wen, Zeng Cheng, Yu Ning, Huang Wei, Gao Zhong-Gao, Xing Jian-Guo
Key Laboratory of Xinjiang Endemic Phytomedicine Resources of Ministry of Education, School of Pharmacy, Shihezi University, Shihezi.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Department of Pharmaceutics, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing.
Int J Nanomedicine. 2017 Apr 19;12:3253-3265. doi: 10.2147/IJN.S131893. eCollection 2017.
Total flavonoid extract from L. (TFDM) contains effective components of L. that have myocardial protective function. However, the cardioprotection function of TFDM is undesirable due to its poor solubility. In order to improve the solubility and efficacy of TFDM, we developed TFDM-loaded solid lipid nanoparticles (TFDM-SLNs) and optimized the formulation of TFDM-SLNs using central composite design and response surface methodology. The physicochemical properties of TFDM-SLNs were characterized, and the pharmacodynamics was investigated using the myocardial ischemia-reperfusion injury model in rats. The nanoparticles of optimal formulation for TFDM-SLNs were spherical in shape with the average particle size of 104.83 nm and had a uniform size distribution with the polydispersity index value of 0.201. TFDM-SLNs also had a negative zeta potential of -28.7 mV to ensure the stability of the TFDM-SLNs emulsion system. The results of pharmacodynamics demonstrated that both TFDM and TFDM-SLN groups afforded myocardial protection, and the protective effect of TFDM-SLNs was significantly superior to that of TFDM alone, based on the infarct area, histopathological examination, cardiac enzyme levels and inflammatory factors in serum. Due to the optimal quality and the better myocardial protective effect, TFDM-SLNs are expected to become a safe and effective nanocarrier for the oral delivery of TFDM.
光果甘草总黄酮提取物(TFDM)含有光果甘草具有心肌保护作用的有效成分。然而,TFDM的心脏保护功能因其溶解度差而不理想。为了提高TFDM的溶解度和疗效,我们制备了载TFDM的固体脂质纳米粒(TFDM-SLNs),并采用中心复合设计和响应面法优化了TFDM-SLNs的处方。对TFDM-SLNs的理化性质进行了表征,并使用大鼠心肌缺血-再灌注损伤模型研究了其药效学。TFDM-SLNs最佳处方的纳米粒呈球形,平均粒径为104.83 nm,粒径分布均匀,多分散指数值为0.201。TFDM-SLNs的ζ电位为-28.7 mV,呈负电性,以确保TFDM-SLNs乳液体系的稳定性。药效学结果表明,基于梗死面积、组织病理学检查、心肌酶水平和血清炎症因子,TFDM组和TFDM-SLNs组均具有心肌保护作用,且TFDM-SLNs的保护作用明显优于单独使用TFDM。由于质量最佳且具有更好的心肌保护作用,TFDM-SLNs有望成为一种安全有效的用于口服TFDM的纳米载体。