Supercritical CO2 foamed polycaprolactone scaffolds for controlled delivery of 5-fluorouracil, nicotinamide and triflusal

• Published in: International journal of pharmaceutics Vol. 496; no. 2; pp. 654 - 663
• Main Authors: Salerno, Aurelio, Saurina, Javier, Domingo, Concepción
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 30.12.2015
• Subjects: Carbon Dioxide - chemistry; Drug Delivery Systems - instrumentation; Drug Delivery Systems - methods; Drug release; Fluorouracil - administration & dosage; Fluorouracil - pharmacokinetics; HeLa Cells; Humans; Niacinamide - administration & dosage; Niacinamide - pharmacokinetics; Polycaprolactone; Polyesters - administration & dosage; Polyesters - pharmacokinetics; Pore structure; Salicylates - administration & dosage; Salicylates - pharmacokinetics; Scaffolds; scCO2 foaming; Tissue Scaffolds - chemistry; Drug release; Pore structure; scCO2 foaming; Polycaprolactone; Scaffolds; scCO foaming
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2015.11.012

[Display omitted] •Supercritical CO2 is used for the preparation of porous drug delivery scaffolds.•Three different drugs, namely 5-fluorouracil, nicotinamide and triflusal are used.•Drug loading depend on scaffold composition and drug solubility in supercritical CO2.•Drug delivery depend mainly upon scaffolds composition and pore structure features. The manufacture of porous polycaprolactone (PCL) scaffolds containing three different drugs, namely 5-fluorouracil, nicotinamide and triflusal, was investigated in this work with the aim of obtaining bioactive systems with controlled drug delivery capabilities. The scaffolds were prepared by means of a supercritical CO2 (scCO2) foaming technique by optimizing the drug loading process. This was achieved by dissolving the drugs in organic solvents miscible with scCO2 and by mixing these drug/solvent solutions with PCL powder. The as prepared mixtures were further compressed to eliminate air bubbles and finally processed by the scCO2 foaming technique. ScCO2 saturation and foaming conditions were optimized to create the porosity within the samples and to allow for the concomitant removal of the organic solvents. Physical and chemical properties of porous scaffolds, as well as drug content and delivery profiles, were studied by HPLC. The results of this study demonstrated that the composition of the starting PCL/drug/solvent mixtures affected polymer crystallization, scaffold morphology and pore structure features. Furthermore, it was found that drug loading efficiency depended on both initial solution composition and drug solubility in scCO2. Nevertheless, in the case of highly scCO2-soluble drugs, such as triflusal, loading efficiency was improved by adding a proper amount of free drug inside of the pressure vessel. The drug delivery study indicated that release profiles depended mainly upon scaffolds composition and pore structure features.