In situ forming biodegradable poly(ε-caprolactone) microsphere systems: a challenge for transarterial embolization therapy. In vitro and preliminary ex vivo studies
Autor: | Andrea Salis, Ioannis Nikolakakis, Giulia R. Fois, Marcello Maestri, Antonia Icaro Cornaglia, Elena Piera Porcu, Giovanna Rassu, Paolo Giunchedi, Elisabetta Gavini, Marco Diana |
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Rok vydání: | 2017 |
Předmět: |
In situ
Male Pathology medicine.medical_specialty Materials science medicine.medical_treatment Chemistry Pharmaceutical Polyesters Pharmaceutical Science Ibuprofen 02 engineering and technology 030226 pharmacology & pharmacy Embolic Agent Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine Animals Embolization Particle Size 021001 nanoscience & nanotechnology Microspheres Rats Polyester Drug Liberation chemistry Particle size 0210 nano-technology Caprolactone Ex vivo medicine.drug Biomedical engineering |
DOI: | 10.6084/m9.figshare.4737907 |
Popis: | Background: In situ forming biodegradable poly(ε-caprolactone) (PCL) microspheres (PCL-ISM) system was developed as a novel embolic agent for transarterial embolization (TAE) therapy of hepatocellular carcinoma (HCC). Ibuprofen sodium (Ibu-Na) was loaded on this platform to evaluate its potential for the treatment of post embolization syndrome. Methods: The influence of formulation parameters on the size/shape, encapsulation efficiency and drug release was investigated using mixture experimental design. Regression models were derived and used to optimize the formulation for particle size, encapsulation efficiency and drug release profile for TAE therapy. An ex vivo model using isolated rat livers was established to assess the in situ formation of microspheres. Results: All PCL-ISM components affected the studied properties and fitting indices of the regression models were high (Radj2 = 0.810 for size, 0.964 encapsulation efficiency, and 0.993 or 0.971 for drug release at 30 min or 48 h). The optimized composition was: PCL = 4%, NMP = 43.1%, oil = 48.9%, surfactant = 2% and drug = 2%. Ex vivo studies revealed that PCL-ISM was able to form microspheres in the hepatic arterial bed. Conclusions: PCL-ISM system provides a novel tool for the treatment of HCC and post-embolization syndrome. It is capable of forming microspheres with desirable size and Ibu-Na release profile after injection into blood vessels. |
Databáze: | OpenAIRE |
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