Characterization and evaluation of metformin-loaded solid lipid nanoparticles for celluar and mitochondrial uptake.
Considered a popular drug for diabetes in recent years, metformin was determined to have a moderate anti-tumor effect, particularly in breast cancer. In this study, the anticancer mechanism of metformin was verified by preparing solid lipid nanoparticles (SLNs) and chitosan-modified solid lipid nanoparticles (CSLNs) containing metformin and then estimating the potential of these SLNs for uptake in cells and mitochondria. Metformin-SLNs were prepared using an emulsification and low-temperature solidification method. The mean particle size, zeta potential, entrapment efficiency, and loading efficiency of metformin-SLNs and metformin chitosan-modified SLNs were 102.3 ± 4.16 and 200.1 ± 17.69 nm, -21.25 ± 4.89 and 50.6 ± 4.09 mv, 26.25 ± 2.59% and 33.6 ± 2.21%, and 1.74 ± 0.16% and 1.46 ± 0.10%, respectively. TEM images showed that both the nanoparticles had spherical morphologies with no aggregation. Results of cellular and mitochondrial uptake showed that the metformin-SLNs were easier to uptake in cells and mitochondria than the pure drug group (that was the control group without SLN structure modification). The findings of this research provide a basis for conducting further studies on the anticancer mechanism of metformin.
a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
Qiang
Q
Xu
a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
Tao
T
Zhu
a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
Chaoli
C
Yi
a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
Qi
Q
Shen
D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D061986:MCF-7 Cells; D008687:Metformin / Q000737:chemistry* / Q000378:metabolism; D008928:Mitochondria / Q000378:metabolism*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility
D004337:Drug Carriers; D008055:Lipids; D048271:Chitosan; D008687:Metformin
Celluar uptake; SLNs; chitosan; metformin; mitochondrial uptake