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Engineering of Layered Nanocarriers of Quercetin for the Treatment of Diabetes Using Box-Behnken Design
Particle & Particle Systems Characterization ( IF 2.7 ) Pub Date : 2023-10-23 , DOI: 10.1002/ppsc.202300037
Priyank Shah 1 , Pravin Shende 1
Affiliation  

Layered nanocarriers are polymeric systems integrated with layers of glucose-responsive polymers and polyethylene glycol monomethyl ether 2000 PEG2000 to enhance the targeting effect and release kinetics. The prime purpose of this research study is to demonstrate a controlled release of Quercetin from formulation of quercetin (Qu)-based layered nanocarriers (LNCs) with higher stability and anti-diabetic activity. The QuLNCs are synthesized using the nanoprecipitation method and optimized by Box-Behnken design of the Design of Experiment (DoE) method. The Quercetin Nanoparticles (QuNPs) are prepared using Polyvinyl alcohol (PVA) and Poly (D,L- lactic-co-glycolic acid) (PLGA) polymers where the two layers of Phenylboronic acid (PBA) are conjugated using 3-amino propyl-triethoxysilane (APTES) as a functionalizing agent followed by PEGylation of the entire system using PEG2000. The optimized QuLNCs are characterized by various parameters like Particle size (PS), Zeta potential (ZP), % Entrapment efficiency (%EE), Attenuated total reflectance- Fourier Transform Infrared Spectroscopy (ATR-FTIR), Differential scanning Calorimetry (DSC), Transmission electron microscopy (TEM), in vitro as well as in vivo studies. The QuLNCs showed a % entrapment efficiency of 82.846 ± 0.957% and release of 85.04 ± 3.21% of Qu for 24 h from the layered nanocarriers. The in vivo studies of QuLNCs exhibited a significant controlled release of quercetin for modulating blood glucose levels. Hence, these results proved QuLNCs system acts as a favorable approach for the treatment of type 1 diabetes to offer a longer duration of action.

中文翻译:

使用 Box-Behnken 设计进行槲皮素层状纳米载体工程治疗糖尿病

层状纳米载体是与葡萄糖响应聚合物层和聚乙二醇单甲醚 2000 PEG 2000集成的聚合物系统,可增强靶向效果和释放动力学。本研究的主要目的是证明基于槲皮素 (Qu) 的层状纳米载体 (LNC) 制剂中槲皮素的受控释放,具有更高的稳定性和抗糖尿病活性。 QuLNC 使用纳米沉淀法合成,并通过实验设计 (DoE) 方法的 Box-Behnken 设计进行优化。槲皮素纳米颗粒 (QuNP) 使用聚乙烯醇 (PVA) 和聚 (D,L-乳酸-乙醇酸) (PLGA) 聚合物制备,其中两层苯硼酸 (PBA) 使用 3-氨基丙基- 缀合。三乙氧基硅烷 (APTES) 作为功能化剂,然后使用 PEG 2000对整个系统进行聚乙二醇化。优化的 QuLNC 具有各种参数,如粒径 (PS)、Zeta 电位 (ZP)、% 捕获效率 (%EE)、衰减全反射率 - 傅里叶变换红外光谱 (ATR-FTIR)、差示扫描量热法 (DSC)、透射电子显微镜 (TEM)、体外和体内研究。 QuLNC 的包封率为 82.846 ± 0.957%,24 小时内从层状纳米载体中释放出 85.04 ± 3.21% 的 Qu。 QuLNC 的体内研究表明,槲皮素具有显着的受控释放作用,可调节血糖水平。因此,这些结果证明 QuLNCs 系统是治疗 1 型糖尿病的有利方法,具有更长的作用持续时间。
更新日期:2023-10-23
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