Increased cellular uptake of lauryl gallate loaded in superparamagnetic poly(methyl methacrylate) nanoparticles due to surface modification with folic acid

Abstract

Lauryl gallate loaded in superparamagnetic poly(methyl methacrylate) nanoparticles surface modified with folic acid were synthesized by miniemulsion polymerization in just one step. In vitro biocompatibility and cytotoxicity assays on L929 (murine fibroblast), human red blood, and HeLa (uterine colon cancer) cells were performed. The effect of folic acid at the nanoparticles surface was evaluated through cellular uptake assays in HeLa cells. Results showed that the presence of folic acid did not affect substantially the polymer particle size (~120 nm), the superparamagnetic behavior, the encapsulation efficiency of lauryl gallate (~87 %), the Zeta potential (~38 mV) of the polymeric nanoparticles or the release profile of lauryl gallate. The release profile of lauryl gallate from superparamagnetic poly(methyl methacrylate) nanoparticles presented an initial burst effect (0-1 h) followed by a slow and sustained release, indicating a biphasic release system. Lauryl gallate loaded in superparamagnetic poly(methyl methacrylate) nanoparticles with folic acid did not present cytotoxicity effects on L929 and human red blood cells. However, free lauryl gallate presented significant cytotoxic effects on L929 and human red blood cells at all tested concentrations. The presence of folic acid increased the cytotoxicity of lauryl gallate loaded in nanoparticles on HeLa cells due to a higher cellular uptake when HeLa cells were incubated at 37 °C. On the other hand, when the nanoparticles were incubated at low temperature (4 °C) cellular uptake was not observed, suggesting that the uptake occurred by folate receptor mediated energy-dependent endocytosis. Based on presented results our work suggests that this carrier system can be an excellent alternative in targeted drug delivery by folate receptor.

Targeted delivery of poly (methyl methacrylate) particles in colon cancer cells selectively attenuates cancer cell proliferation

“…Polymeric nanocarriers are found to be effective in safe drug delivery because its hydrophobic core which helps in the dissolution of hydrophobic drugs [14]. Among the different types of hydrophobic polymers, PMMA is widely used in drug delivery applications [15][16][17][18]. PMMA is basically biocompatible polyester with high resistance to chemical hydrolysis, and high drug permeability and most important is that it does not cause toxicity [19].…”

Cannabis Extracts and Their Cytotoxic Effects on Human Erythrocytes, Fibroblasts, and Murine Melanoma

“…Hemolytic activity was evaluated by hemolysis assay according to the methodology described by Feuser et al (2016).…”

“…4A. According to the criteria of the Standard Test Method for Analysis of Hemolytic Properties (E2524-08), hemolysis of greater than 5% indicates that the tested compound is harmful (Feuser et al 2016). Fig.…”

Biopolymers in Drug Delivery and Regenerative Medicine

“…Polyacrylates are anionic polymers that present maximum swelling at pH neutral to alkaline, and minimum under acidic conditions, making them ideal for colon-specific drug delivery systems [151]. Feuser et al (2016) modified with folic acid polymethyl meta acrylate and ferrous sulfate to produce superparamagnetic nanoparticles with excellent colloidal stability and high efficacy in encapsulating lauryl gallate (antioxidant). The release profile of lauryl gallate showed an initial burst effect followed by a slow and sustained release, indicating a biphasic release system.…”