Amphiphilic poly-N-vinylpyrrolidone nanoparticles as carriers for non-steroidal, anti-inflammatory drugs: In vitro cytotoxicity and in vivo acute toxicity study

作者：Kuskov Andrey N; Kulikov Pavel P; Goryachaya Anastasia V; Tzatzarakis Manolis N; Docea Anca O; Velonia Kelly; Shtilman Mikhail I; Tsatsakis Aristidis M^*

来源：Nanomedicine: Nanotechnology, Biology and Medicine , 2017, 13(3): 1021-1030.

DOI：10.1016/j.nano.2016.11.006

• Poly-N-vinylpyrrolidone
• Indomethacin
• Amphiphilic
• Nanoparticle
• Toxicity
• Drug delivery system

Polymeric nanoparticles were prepared from self-assembled amphiphilic N-vinylpyrrolidone polymers in aqueous media and evaluated as novel carriers of indomethacin, a non-steroidal, anti-inflammatory drug. It was determined that these nanoparticles could be created in spherical morphologies with sizes less than 100 nm, narrow size distributions and high indomethacin contents(up to 35%) combined with high drug loading efficiencies(up to 95%). In cytotoxicity tests using the human embryonic stem cell derived fibroblasts (EBF-H9) and hepatocellular carcinoma cells (HepG2), the indomethacin-loaded polymeric nanoparticles showed higher cell viability compared to that of free indomethacin at the same concentration. The median LD50 values, determined by the Litchfield-Wilcoxon method, were 55-70 mg/kg body weight depending on the polymer molecular design in both mice and rats. Based on the acquired results, these novel amphiphilic polyN-vinylpyrrolidone nanoparticles can be considered as potential carriers for new, highly efficient, injectable drug delivery systems for hydrophobic drugs such as indomethacin.

• 出版日期2017-4
• 单位北京化工大学