Development and evaluation of PLGA nanoparticles with cyclosporine and the inclusion of HPβCD for ocular use

Ocular delivery of peptides requires new concepts in order to optimize the bioavailability and its therapeutic effect. The first peptide selected in present research project is Cyclosporine A (CyA) used in the treatment of the dry eye syndrome and against corneal graft rejection. The aim of the project is the development of nanoparticles with physicochemical properties for a suitable and prolonged release of CyA, using a factorial design. These drug delivery systems will be produced employing PLGA using the emulsification solvent evaporation method. Positively charged polymers as chitosan or Eudragit® will be incorporated to obtain nanoparticles with a positive particle charge. Electrostatic interactions with the negatively charged mucins lead to a prolonged residence time at the precorneal area. Nanoparticles will be evaluated on zeta potential, particle size and their in vitro drug release properties. CyA and CyA complexed with HPβCD will be compared. The most suitable preparations will be selected in a next phase of the project for an in vivo study using an animal model.