A pH-sensitive poly(methyl methacrylate) copolymer for efficient drug and gene delivery across the cell membrane

Abstract

A versatile drug delivery system based on calcium phosphate/Eudragit®-E100 nanoparticles with a diameter below 200 nm was realized by a water-in-oil-in-water (W 1 /O/W 2) emulsion solvent evaporation technique. Hydrophilic drugs (siRNA for gene silencing and bovine serum albumin as model protein) and hydrophobic drugs (5,10,15,20-tetrakis(4-hydroxyphenyl)-21H,23H-porphine, THPP, a photosensitizer for photodynamic therapy) were encapsulated as model drugs. Eudragit®-E100 is a poly(methyl methacrylate) copolymer with a low solubility at neutral pH and a high solubility at low pH. Thus, the particles are stable in cell culture media and rapidly dissolved in the lysosome after cellular uptake and delivery of their cargo into the cell. The particles had a positive charge (zeta potential +49 mV) and were taken up very well by epithelial cells (HeLa) as shown by fluorescence microscopy and confocal laser scanning microscopy. Gene-silencing experiments on HeLa-eGFP cells gave knockdown efficiencies of 39% with no toxic effects. The particles can be freeze-dried without cryoprotectant and easily redispersed in water, thus making their transport and storage convenient.

Electrophoretically Deposited Chitosan/Eudragit E 100/AgNPs Composite Coatings on Titanium Substrate as a Silver Release System

“…Under the influence of environmental changes, it is also possible to self-organize the biopolymer into micelles, gel formation, or swelling [ 14 ]. Among the pH-sensitive biopolymers chitosan [ 15 ], Eudragit E 100 [ 16 ], poly(4-vinylpyridine) [ 17 ], and poly(L-histidine) are prominent [ 18 ]. They may form a matrix in which metallic nanoparticles with antibacterial properties can be dispersed.…”

pH Tunable Thin Film Gradients of Magnetic Polymer Colloids for MRI Diagnostics

“…There is a loose and loopy polymer adsorption takes place at the pH of the PAA deposition solution near to the pKa value of 4.5 [16]. Magnetic polymer colloids having Eudragit E100, which is a cationic pH-responsive coating polymer with dimethylaminoethyl ammonium functional groups having low solubility at pH neutral and a high solubility at pH below 5 [30]. Eudragit E100 is prepared by the polymerization of acrylic and methacrylic acid or their esters, both of these polymers are biodegradable, non-toxic and synthetic displayed in Figure 5b.…”

Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

“…E100 is extensively utilized in oral and topical preparations and mostly considered non-irritant, nontoxic and effectively safe for human beings [21]. In addition, the positive charge of particles of amino groups present in E100 enhances the cellular uptake of biomolecules and protects them from enzymatic attack by proton sponge effect, providing storable nanoparticulate without cryoprotectant after freeze-drying [22]. Methotrexate nanoparticles (MTX-NPs) once prepared were embedded into chitosan hydrogel.…”