title: Characterization and evaluation of metformin-loaded solid lipid nanoparticles for celluar and mitochondrial uptake.
abstract: 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.
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Xu
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Tao
authors.initials: T
authors.lastname: Zhu
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Chaoli
authors.initials: C
authors.lastname: Yi
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Shen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001943:Breast Neoplasms / Q000188:drug therapy; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D006801:Humans; D008055:Lipids / Q000737:chemistry; D061986:MCF-7 Cells; D008297:Male; D008687:Metformin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008928:Mitochondria / Q000378:metabolism*; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008055:Lipids; D048271:Chitosan; D008687:Metformin
keywords: Celluar uptake; SLNs; chitosan; metformin; mitochondrial uptake