Development and Characterization of 5-Fluorouracil Solid Lipid Nanoparticles for Treatment of Colorectal Cancer,Journal of Pharmaceutical Innovation

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Development and Characterization of 5-Fluorouracil Solid Lipid Nanoparticles for Treatment of Colorectal Cancer
Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2022-01-09 , DOI: 10.1007/s12247-021-09605-x
Poournima Patil _{1,

2} , Harinath More ₂ , Suresh Killedar ₃ , Ganesh Vambhurkar ₄

Affiliation

Purpose

In this study, the oral nanotherapeutic approach of 5-fluorouracil solid lipid nanoparticles (5-FU SLNs) for the synergistic treatment of colorectal cancer in preclinical DMH rat model is studied.

Method

5-Fluorouracil solid lipid nanoparticles with solvent evaporation emulsification method by using different ratios of polymer and surfactant.

Result

5-FU SLNs with chitosan and poloxamer 407 ratio of 2.4:0.1 has shown better particle size (147.9 ± 1.48 nm) with entrapment efficiency 90.60 ± 0.01% and loading content 3.40 ± 0.03%. In vitro, drug release studies were done by using simulated fluids at various pHs (1.2, 4.5, 7.5, and 7.0) to mimic the GIT tract and achieve 85.16 ± 0.26% at 24 h in a sustained manner. In the current investigation, treatment with 5-FU SLNs increased levels of SOD, CAT, and GSH in the colonic tissue which were considerably DMH-treated rats having lower level. It should be highlighted that the 5-FU SLNs anticancer activity on colorectal was superior over the course of the study, utilizing an in vivo model. Colonic tumour incidence, speed, size, and multiplicity, as well as the number of ACFs, have all decreased.

Conclusion

Collectively, based on the chitosan-TPP platform, these results suggest that both 5-fluorouracil solid lipid nanoparticles confirmed in vitro and in vivo has shown to provide a promising oral delivery for colorectal cancer.

Graphic Abstract

中文翻译：

用于治疗结直肠癌的 5-氟尿嘧啶固体脂质纳米颗粒的开发和表征

目的

在这项研究中，研究了 5-氟尿嘧啶固体脂质纳米粒 (5-FU SLNs) 在临床前 DMH 大鼠模型中协同治疗结直肠癌的口服纳米治疗方法。

方法

5-氟尿嘧啶固体脂质纳米粒采用溶剂蒸发乳化法，采用不同比例的聚合物和表面活性剂。

结果

壳聚糖和泊洛沙姆 407 比例为 2.4:0.1 的 5-FU SLN 显示出更好的粒径 (147.9 ± 1.48 nm)，包埋效率为 90.60 ± 0.01%，负载量为 3.40 ± 0.03%。在体外，通过使用各种 pH 值（1.2、4.5、7.5 和 7.0）的模拟流体来模拟 GIT 道并在 24 小时内以持续的方式实现 85.16 ± 0.26% 的药物释放研究。在目前的调查中，用 5-FU SLNs 治疗增加了结肠组织中 SOD、CAT 和 GSH 的水平，而 DMH 治疗大鼠的水平显着降低。应该强调的是，在研究过程中，5-FU SLNs 对结肠直肠癌的抗癌活性优于体内模型。结肠肿瘤的发病率、速度、大小和多样性，以及 ACF 的数量均有所下降。