PLGA nanoparticles optimized by Box-Behnken for efficient encapsulation of therapeutic Cymbopogon citratus essential oil
PLGA nanoparticles optimized by Box-Behnken for efficient encapsulation of therapeutic Cymbopogon citratus essential oil
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DOI：
10.1016/j.colsurfb.2019.06.010
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发表时间：
2019-09-01
影响因子：
5.8
通讯作者：
Falcao, Deborah Q.
中科院分区：
文献类型：
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作者：
Almeida, Kessiane B.;Ramos, Aline S.;Falcao, Deborah Q.
本研究采用Box-Behnken设计，考察超声时间、超声功率、精油/聚合物比等工艺参数对包封效率和颗粒平均水动力直径的影响，以优化香橼精油在plga纳米颗粒中的包封效果。采用乳化/溶剂扩散法制备了纳米颗粒，并用FTIR、DSC和TGA/DTA对其进行了物理化学表征。用WST-1和LDH测定人HaCat角质形成细胞的细胞毒性。优化后的配方水动力平均粒径为277 nm，多分散性指数为0.18，Zeta电位为-16 mV，包封效率为73%。纳米颗粒表征表明，纳米载体中只有柠檬醛被掺入，并有一定数量的柠檬醛吸附在纳米载体表面，这突出了提高油热稳定性的潜力。药物释放谱表现为双相模式，具有依赖于聚合物基质扩散的实质性持续释放。纯精油在低浓度下对细胞活力的毒性作用被包封后明显消除。结果表明，plga纳米颗粒能够通过控制释放和降低毒性来改善精油的理化特性，表明其在药物制剂中的潜在应用前景。
This study aimed to optimize Cymbopogon citratus essential oil loaded into PLGA-nanoparticles by investigating the effect of processing variables (sonication time, ultrasound power, and essential oil/polymer ratio) on encapsulation efficiency and particle mean hydrodynamic diameter using Box-Behnken design. Nanoparticles were prepared by an emulsification/solvent diffusion method and physicochemically characterized by FTIR, DSC and TGA/DTA. Cytotoxicity was evaluated in human HaCat keratinocytes by WST-1 and LDH assays. The optimized formulation had a hydrodynamic mean diameter of 277 nm, a polydispersity index of 0.18, a Zeta potential of -16 mV and an encapsulation efficiency of 73%. Nanoparticle characterization showed that only citral was incorporated in nanocarriers, with some amount adsorbed on their surface, and highlighted the potential in increasing the oil thermal stability. The drug release profile demonstrated a biphasic pattern with a substantial sustained release depending on diffusion from the polymeric matrix. Toxicity effects on cell viability of pure essential oil at low concentrations were significantly eliminated when encapsulated. Results revealed the ability of PLGA-nanoparticles to improve essential oil physicochemical characteristics, by controlling release and reducing toxicity, suggesting their potential use in pharmaceutical preparations.