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.

背景：本研究的目的是制定、表征和体外细胞毒性的 5-氟尿嘧啶负载控释纳米粒子用于治疗皮肤癌。纳米颗粒专利（US8414926B1）、（US61654404A）、（WO2007150075A3）等有助于选择聚合物和制备纳米颗粒的方法。

方法：在本研究中，使用不同浓度的壳聚糖和三聚磷酸钠 (TPP) 通过简单的离子凝胶法制备纳米颗粒。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。对制备的纳米粒子的粒径、形状、电荷、包埋效率、交联机制和药物释放研究进行评估。

结果：优化后的5-氟尿嘧啶负载纳米粒子粒径为320±2.1 nm，包封率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球形颗粒大小均匀。体外释放曲线显示控制释放长达 24 小时。进一步研究使用A375基底细胞癌细胞系通过MTT测定阐明其细胞毒性机制。

结论：这些结果表明以增强的包封效率将5-氟尿嘧啶递送至皮肤的可能性表明该制剂治疗基底细胞癌类型皮肤癌的有效性。