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Development and Evaluation of Letrozole-Loaded Hyaluronic Acid/Chitosan-Coated Poly( d , l -lactide- co -glycolide) Nanoparticles
Journal of Pharmaceutical Innovation ( IF 2.6 ) Pub Date : 2021-02-05 , DOI: 10.1007/s12247-021-09538-5
Radwa Radwan , Ayat Abdelkader , Heba A. Fathi , Mahmoud Elsabahy , Gihan Fetih , Mahmoud El-Badry

Purpose

Letrozole (LTZ), an aromatase inhibitor with poor aqueous solubility, is used as the first line treatment for hormonal sensitive breast cancer in postmenopausal women. The purpose of the current study is to develop hyaluronic acid (HA)/chitosan (Cs)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles for the delivery of LTZ to improve therapeutic efficacy, control release and minimize side effects of LTZ.

Methods

PLGA nanoparticles were prepared, and the effect of various parameters on particle size, surface charge, and encapsulation efficiency was extensively studied. The morphology of nanoparticles was visualized using transmission electron microscopy (TEM), and drug-polymer interactions were studied using differential scanning calorimetry (DSC) and Fourier transform-infrared spectroscopy (FT-IR). The in vitro release kinetics and effect of freeze-drying process on the physicochemical characteristics of nanoparticles were also evaluated. Moreover, the in vivo acute toxicities of blank and drug-loaded nanoparticles were assessed.

Results

PLGA nanoparticles exhibited nanosized (464.3 ± 2.1 nm) spherical particles, negative surface charge (zeta-potential of − 10.5 ± 0.4 mV), and high drug encapsulation efficiency of 63.9 ± 3.7% and sustained drug release pattern over 48 h. The in vivo acute toxicity study revealed that the nanoparticles were well tolerated at a dose of 300 mg/kg.

Conclusion

HA/Cs-coated PLGA nanoparticles might provide a promising system for LTZ delivery and further investigations could confirm their potential efficacy in breast cancer therapy.



中文翻译:

来曲唑负载透明质酸/壳聚糖包衣的聚(d,l-丙交酯-乙交酯)纳米粒子的开发与评价

目的

来曲唑(LTZ)是一种水溶性差的芳香酶抑制剂,被用作绝经后妇女激素敏感型乳腺癌的一线治疗方法。目前研究的目的是开发透明质酸(HA)/脱乙酰壳多糖(CS)包被的聚(d-lactide--glycolide)(PLGA)的纳米颗粒为LTZ的输送,以提高治疗功效,控制释放和最小化LTZ的副作用。

方法

制备了PLGA纳米颗粒,并广泛研究了各种参数对粒径,表面电荷和包封效率的影响。使用透射电子显微镜(TEM)观察纳米颗粒的形貌,并使用差示扫描量热法(DSC)和傅立叶变换红外光谱(FT-IR)研究药物-聚合物的相互作用。还评估了体外释放动力学和冷冻干燥过程对纳米颗粒理化特性的影响。此外,评估了空白和载药纳米粒子的体内急性毒性。

结果

PLGA纳米颗粒表现出纳米级(464.3±2.1 nm)球形颗粒,负表面电荷(ζ电位-10.5±0.4 mV),高药物包封效率63.9±3.7%和48小时持续释药模式。体内急性毒性研究表明,纳米颗粒在300 mg / kg的剂量下具有良好的耐受性。

结论

HA / Cs涂层的PLGA纳米颗粒可能为LTZ的输送提供有希望的系统,进一步的研究可以证实其在乳腺癌治疗中的潜在功效。

更新日期:2021-02-05
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