Permeability of Skin-Mimicking Cell Coatings by Polymers of Complex Architecture Based on Polyoxazolines

Abstract

In the scope of drug delivery, the transdermal route is desirable because it provides attainable therapeutic concentrations and has minimal systemic side effects. To make the skin a feasible route for the delivery of therapeutic agents, the biggest challenge is overcoming its natural coating. In this paper, we investigate the effect of the architectures (homopolymer vs. block copolymer vs. hybrid block–graft copolymer) of several amphiphilic polymeric derivatives of poly(2-oxazoline) on skin permeability. The block copolymers are composed of a hydrophobic poly(2-oxazoline) block and a hydrophilic PEG block. The hybrid block–graft copolymers are obtained by grafting hydrophobic side chains of polycaprolactone to a poly(2-oxazoline) backbone. We used the commercially available EpiDerm™ by MatTek, composed of human epidermal cells, as a model of human skin. Two parameters of skin permeation are reported: penetration rate and lag time. We hypothesize that the skin permeation characteristics correlate with the critical micelle concentration and particle size of the studied polymers, while both parameters are a function of the complex architectures of the presented macromolecular constructs. While homopolymer poly(2-oxazolines) show the least permeation, the block copolymers demonstrate partial permeation. The hybrid block–graft copolymers exhibited full penetration through the model skin samples.