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载 5-氟尿嘧啶壳聚糖纳米粒治疗皮肤癌的研究。

Study of 5-Fluorouracil Loaded Chitosan Nanoparticles for Treatment of Skin Cancer.

机构信息

Department of Pharmaceutics & Pharmaceutical Technology, Charotar University of Science and Technology, Ramanbhai Patel College of Pharmacy, CHARUSAT Campus Changa, Gujarat, India.

出版信息

Recent Pat Nanotechnol. 2020;14(3):210-224. doi: 10.2174/1872210513666190702165556.

Abstract

BACKGROUND

The purpose of this study was to formulate, characterize and in-vitro cytotoxicity of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection polymers and method for the preparation of nanoparticles.

METHODS

In the present study nanoparticles were prepared by simple ionic gelation method using various concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and drug release study.

RESULTS

The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1 nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy and dynamic light scattering technique revealed spherical particles with uniform size. The invitro release profile showed controlled release up to 24 hr. Further study was carried using A375 basal cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay.

CONCLUSION

These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell carcinoma type of skin cancer.

摘要

背景

本研究的目的是制备、表征和体外细胞毒性研究 5-氟尿嘧啶负载的控释纳米粒用于皮肤癌的治疗。专利(US8414926B1)、(US61654404A)、(WO2007150075A3)等在选择聚合物和纳米粒的制备方法方面提供了帮助。

方法

在本研究中,通过使用不同浓度的壳聚糖和三聚磷酸钠(TPP)的简单离子凝胶化方法制备纳米粒。使用 25-2 部分因子设计筛选和优化了几个工艺和配方参数。对制备的纳米粒进行了粒径、形态、电荷、包封效率、交联机制和药物释放研究。

结果

优化的负载 5-氟尿嘧啶的纳米粒的粒径为 320±2.1nm,包封效率为 85.12%±1.1%,Zeta 电位为 29mv±1mv。扫描电子显微镜和动态光散射技术显示出具有均匀粒径的球形颗粒。体外释放曲线显示可控制释放达 24 小时。进一步使用 A375 基底细胞癌细胞系进行研究,通过 MTT 测定法阐明其细胞毒性的机制。

结论

这些结果表明,将 5-氟尿嘧啶递送到皮肤中具有增强的包封效率的可能性,表明该制剂在治疗基底细胞癌型皮肤癌方面的有效性。

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