In vitro evaluation of nanoparticle drug-coated balloons: a pectin-RGDS-OC8H17-paclitaxel solution

Abstract

AbstractDrug-coated balloons have proved to be an effective technology in percutaneous transluminal angioplasty in treating peripheral artery disease. Paclitaxel-based coating is mainly used. Solutions to such problems as drug loss and inefficient drug release during operations, however, have not been found yet. This study aims to explore the activity of a newly designed paclitaxel-coated balloon in vitro using pectin as the excipient (pectin-paclitaxel) compared with the commercially available shellac excipient balloon, and to characterize the novel nanoparticle paclitaxel-coated balloon with peptide (Arg-Gly-Asp-Ser, RGDS) derivative RGDS-OC8H17 (pectin-RGDS-OC8H17-paclitaxel). Two coating solutions, pectin-paclitaxel and pectin-RGDS-OC8H17-paclitaxel, were successively designed and prepared. The morphology of both coating solutions was first characterized compared with the control group, the commercially available paclitaxel-coated balloon. Then the in vitro experiments were conducted to determine the drug-releasing profiles of both pectin-paclitaxel and pectin-RGDS-OC8H17-paclitaxel coatings. The pectin-RGDS-OC8H17-paclitaxel-coated balloon was smoother and more homogeneous compared with the commercially available paclitaxel-coated balloon and the pectin-paclitaxel-coated balloon. This difference was more obvious when paclitaxel was at low concentration. During the in vitro trial, the drug-releasing curve of the pectin-RGDS-OC8H17-paclitaxel model showed an adjustable paclitaxel-releasing: more than 90% of the paclitaxel released in 2 h at 300 rpm and more than 99% released in 10 min at 1200 rpm. Compared to the performance of the current commercially available shellac excipient products and the pectin-paclitaxel coating, pectin-RGDS-OC8H17-paclitaxel coating provided higher drug-releasing speed. However, the clinical outcomes of this finding need to be further demonstrated. Paclitaxel-coated balloons as an effective therapeutic strategy currently in treating peripheral arterial disease need to be further improved in terms of its efficiency in anti-proliferative drug delivery and release. The pectin-RGDS-OC8H17-paclitaxel coating solution developed in this study exhibited excellent drug-releasing properties. Further experiments are still needed to demonstrate the performance of this novel drug-coated balloon in vivo and its clinical importance.