Encapsulation of Andrographolide in poly(lactide-co-glycolide) Nanoparticles: Formulation Optimization and in vitro Efficacy Studies.
Encapsulation of Andrographolide in poly(lactide-co-glycolide) Nanoparticles: Formulation Optimization and in vitro Efficacy Studies.
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DOI：
10.3389/fbioe.2021.639409
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发表时间：
2021
影响因子：
5.7
通讯作者：
Panyam J
中科院分区：
文献类型：
--
作者：
Oseni BA;Azubuike CP;Okubanjo OO;Igwilo CI;Panyam J
穿心莲内酯是一种潜在的化学预防和化学治疗剂，但水溶性差。封装在聚（丙交酯-共-乙交酯）（PLGA）纳米颗粒中可以克服溶解度问题，并使药物能够持续释放，从而提高治疗效果。本研究采用乳化溶剂挥发法将穿心莲内酯包裹在PLGA纳米粒中。研究了各种制剂参数，包括聚合物组成、聚合物分子量、聚合物与药物的比例、表面活性剂浓度和所用有机溶剂对纳米颗粒性质的影响。使用选定的制剂来确定纳米颗粒中的包封对穿心莲内酯的体外抗癌功效的影响。基于平均流体动力学粒度（135 ± 4 nm）和载药量（2.6 ± 0.6%w/w），发现使用丙交酯与乙交酯比例为85：15的聚合物和乙酸乙酯作为有机溶剂配制的纳米颗粒是最佳的。该制剂在48小时内表现出穿心莲内酯的持续释放，并且在转移性乳腺癌细胞系中表现出与游离药物相比显著更大的体外抗癌功效。这些结果表明，额外的，更深入的疗效研究是必要的纳米制剂穿心莲。
Andrographolide is a potential chemopreventive and chemotherapeutic agent that suffers from poor aqueous solubility. Encapsulation in poly(lactide-co-glycolide) (PLGA) nanoparticles can overcome solubility issues and enable sustained release of the drug, resulting in improved therapeutic efficacy. In this study, andrographolide was encapsulated in PLGA nanoparticles via emulsion solvent evaporation technique. Effect of various formulation parameters including polymer composition, polymer molecular weight, polymer to drug ratio, surfactant concentration and the organic solvent used on nanoparticle properties were investigated. A selected formulation was used to determine the effect of encapsulation in nanoparticles on andrographolide’s in vitro anticancer efficacy. Nanoparticles formulated using a polymer with 85:15 lactide to glycolide ratio and ethyl acetate as the organic solvent were found to be optimal based on average hydrodynamic particle size (135 ± 4 nm) and drug loading (2.6 ± 0.6%w/w). This formulation demonstrated sustained release of andrographolide over 48 h and demonstrated significantly greater in vitro anticancer efficacy compared to free drug in a metastatic breast cancer cell line. These results suggest that additional, more in-depth efficacy studies are warranted for the nanoparticle formulation of andrographolide.
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DOI：
10.1016/j.jconrel.2015.10.006
发表时间：
2015-12-10
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Hickey JW;Santos JL;Williford JM;Mao HQ
通讯作者：
Mao HQ
DOI：
10.1155/2013/846740
发表时间：
2013
期刊：
Evidence-based complementary and alternative medicine : eCAM
影响因子：
--
作者：
Jayakumar T;Hsieh CY;Lee JJ;Sheu JR
通讯作者：
Sheu JR
穿心莲内酯诱导的细胞毒性和细胞周期停滞导致 MDA-MB-231 乳腺癌细胞系的程序性细胞死亡。
影响因子：
11
作者：
Banerjee M;Chattopadhyay S;Choudhuri T;Bera R;Kumar S;Chakraborty B;Mukherjee SK
通讯作者：
Mukherjee SK
影响因子：
5.8
作者：
Grabowski, Nadege;Hillaireau, Herve;Fattal, Elias
通讯作者：
Fattal, Elias
影响因子：
14
作者：
Kim, Hyunjoon;Niu, Lin;Panyam, Jayanth
通讯作者：
Panyam, Jayanth