Cilostazol-Loaded Poly(ε-Caprolactone) Electrospun Drug Delivery System for Cardiovascular Applications

• Published in: Pharmaceutical research Vol. 35; no. 2; pp. 32 - 20
• Main Authors: Rychter, Marek, Baranowska-Korczyc, Anna, Milanowski, Bartłomiej, Jarek, Marcin, Maciejewska, Barbara M., Coy, Emerson L., Lulek, Janina
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.02.2018; Springer; Springer Nature B.V
• Subjects: Atherosclerosis - surgery; Biochemistry; Biodegradability; Biodegradation; Biomedical and Life Sciences; Biomedical Engineering and Bioengineering; Biomedicine; Blood Vessel Prosthesis; Blood Vessel Prosthesis Implantation - adverse effects; Calorimetry; Cilostazol - administration & dosage; Cilostazol - pharmacokinetics; Differential scanning calorimetry; Diffraction; Drug Compounding - methods; Drug delivery; Drug Delivery Systems; Drug Liberation; Drugs; Electrospinning; Fibers; Formulations; Humans; Infrared spectroscopy; Mechanical properties; Medical Law; Modulus of elasticity; Pharmacology/Toxicology; Pharmacy; Platelet Aggregation Inhibitors - administration & dosage; Platelet Aggregation Inhibitors - pharmacokinetics; Polycaprolactone; Polyesters - chemistry; Polymers; Raman spectra; Raman spectroscopy; Research Paper; Spectroscopy; Spectrum analysis; Thrombosis - etiology; Thrombosis - prevention & control; Vehicles; X-ray diffraction; X-rays; cilostazol; tissue regeneration; drug delivery system; electrospinning; polycaprolactone
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1007/s11095-017-2314-0

Purpose The study discusses the value of electrospun cilostazol-loaded (CIL) polymer structures for potential vascular implant applications. Methods Biodegradable polycaprolactone (PCL) fibers were produced by electrospinning on a rotating drum collector. Three different concentrations of CIL: 6.25%, 12.50% and 18.75% based on the amount of polymer, were incorporated into the fibers. The fibers were characterized by their size, shape and orientation. Materials characterization was carried out by Fourier Transformed Infrared spectroscopy (FTIR), Raman spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD). In vitro drug release study was conducted using flow-through cell apparatus (USP 4). Results Three-dimensional structures characterized by fibers diameter ranging from 0.81 to 2.48 μm were in the range required for cardiovascular application. DSC and XRD confirmed the presence of CIL in the electrospun fibers. FTIR and Raman spectra confirmed CIL polymorphic form. Elastic modulus values for PCL and the CIL-loaded PCL fibers were in the range from 0.6 to 1.1 GPa. The in vitro release studies were conducted and revealed drug dissolution in combination with diffusion and polymer relaxation as mechanisms for CIL release from the polymer matrix. Conclusions The release profile of CIL and nanomechanical properties of all formulations of PCL fibers demonstrate that the cilostazol loaded PCL fibers are an efficient delivery system for vascular implant application.