用于结直肠癌靶向治疗的壳聚糖表面修饰聚合物纳米粒的制备与表征
Preparation and characterization of polymeric nanoparticles surface modified with chitosan for target treatment of colorectal cancer.
作者信息
Badran Mohamed M, Mady Mohsen M, Ghannam Magdy M, Shakeel Faiyaz
机构信息
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
Department of Physics and Astronomy, College of Science, King Saud University, Riyadh 11451, Saudi Arabia; Biophysics Department, Faculty of Science, Cairo University, Giza, Egypt.
出版信息
Int J Biol Macromol. 2017 Feb;95:643-649. doi: 10.1016/j.ijbiomac.2016.11.098. Epub 2016 Nov 28.
5-Fluorouracil (5-FU) loaded chitosan (C) coated polylactic-co-glycolic acid (PLGA) nanoparticles [NPs] (C-5-FU PLGA NPs) and polycaprolactone [PCL] (C-5-FU PCL NPs) were employed as the carriers for cancer treatment. The prepared NPs showed the spherical shape of NPs with the particle size in the range of 188.1-302.2nm with polydispersity index (PDI) of <0.30. C-coated NPs converted zeta potential from negative to positive value with small modification in particle size distribution. The entrapment efficiency of 5-FU was recorded in the range of 32-51%. The in vitro release studies showed an initial rapid 5-FU release followed by a sustained release profile. The in vitro cytotoxicity of C-5-FU PLGA NPs showed significant inhibition of colon cancer cells (HT-29) compared to the other NPs and drug solution. These results showed that C-5-FU PLGA NPs can be considered as a promising carrier for cancer therapy.
负载5-氟尿嘧啶（5-FU）的壳聚糖（C）包被的聚乳酸-乙醇酸共聚物（PLGA）纳米颗粒[NPs]（C-5-FU PLGA NPs）和聚己内酯[PCL]（C-5-FU PCL NPs）被用作癌症治疗的载体。制备的纳米颗粒呈现出球形，粒径范围为188.1-302.2nm，多分散指数（PDI）<0.30。壳聚糖包被的纳米颗粒使zeta电位从负值转变为正值，粒径分布略有变化。5-氟尿嘧啶的包封率记录在32%-51%的范围内。体外释放研究表明，最初5-氟尿嘧啶快速释放，随后是持续释放曲线。与其他纳米颗粒和药物溶液相比，C-5-FU PLGA NPs的体外细胞毒性对结肠癌细胞（HT-29）表现出显著抑制作用。这些结果表明，C-5-FU PLGA NPs可被视为一种有前景的癌症治疗载体。
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