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Article

Amphiphilic Block Copolymer Microspheres Derived from Castor Oil, Poly(ε-carpolactone), and Poly(ethylene glycol): Preparation, Characterization and Application in Naltrexone Drug Delivery

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Physicochemistry Laboratory of Electrolytes and Interfacial Nanosystems (PHENIX), UMR CNRS 8234, Faculty of Science and Engineering, Sorbonne University, 75252 Paris CEDEX 05, France
2
Laboratory of Chemistry and Technology of Polymers and Dyes, Chemistry Department, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
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Laboratory of Polymeric Materials, Department of Materials Science and Engineering, University of Ioannina, Administration Building, University Campus Dourouti, 45110 Ioannina, Greece
4
Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
*
Authors to whom correspondence should be addressed.
Materials 2018, 11(10), 1996; https://doi.org/10.3390/ma11101996
Received: 28 September 2018 / Revised: 12 October 2018 / Accepted: 12 October 2018 / Published: 16 October 2018
(This article belongs to the Special Issue Synthesis, Characterization and Applications of Block Copolymers)
In the present study, the newly synthesized castor oil-derived thioether-containing ω-hydroxyacid (TEHA) block copolymers with polycaprolactone (TEHA-b-PCL), with methoxypoly(ethylene glycol) (mPEG), (TEHA-b-mPEG) and with poly(ethylene glycol) (PEG) (TEHA-b-PEG-b-TEHA), were investigated as polymeric carriers for fabrication of naltrexone (NLX)-loaded microspheres by the single emulsion solvent evaporation technique. These microspheres are appropriate for the long-term treatment of opioid/alcohol dependence. Physical properties of the obtained microspheres were characterized in terms of size, morphology, drug loading capacity, and drug release. A scanning electron microscopy study revealed that the desired NLX-loaded uniform microspheres with a mean particle size of 5–10 µm were obtained in all cases. The maximum percentage encapsulation efficiency was found to be about 25.9% for the microspheres obtained from the TEHA-b-PEG-b-TEHA copolymer. Differential scanning calorimetry and X-ray diffractometry analysis confirmed the drug entrapment within microspheres in the amorphous state. In vitro dissolution studies revealed that all NLX-loaded formulations had a similar drug release profile: An initial burst release after 24 h, followed by a sustained and slower drug release for up to 50 days. The analysis of the release kinetic data, which were fitted into the Korsmeyer–Peppas release model, indicated that diffusion is the main release mechanism of NLX from TEHA-b-PCL and TEHA-b-mPEG microspheres, while microspheres obtained from TEHA-b-PEG-b-TEHA exhibited a drug release closer to an erosion process. View Full-Text
Keywords: castor oil; poly(ε-caprolactone); poly(ethylene glycol); amphiphilic block copolymers; microspheres; naltrexone; drug release castor oil; poly(ε-caprolactone); poly(ethylene glycol); amphiphilic block copolymers; microspheres; naltrexone; drug release
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MDPI and ACS Style

Nerantzaki, M.; Skoufa, E.; Adam, K.-V.; Nanaki, S.; Avgeropoulos, A.; Kostoglou, M.; Bikiaris, D. Amphiphilic Block Copolymer Microspheres Derived from Castor Oil, Poly(ε-carpolactone), and Poly(ethylene glycol): Preparation, Characterization and Application in Naltrexone Drug Delivery. Materials 2018, 11, 1996. https://doi.org/10.3390/ma11101996

AMA Style

Nerantzaki M, Skoufa E, Adam K-V, Nanaki S, Avgeropoulos A, Kostoglou M, Bikiaris D. Amphiphilic Block Copolymer Microspheres Derived from Castor Oil, Poly(ε-carpolactone), and Poly(ethylene glycol): Preparation, Characterization and Application in Naltrexone Drug Delivery. Materials. 2018; 11(10):1996. https://doi.org/10.3390/ma11101996

Chicago/Turabian Style

Nerantzaki, Maria; Skoufa, Eirini; Adam, Kyriakos-Vasileios; Nanaki, Stavroula; Avgeropoulos, Apostolos; Kostoglou, Margaritis; Bikiaris, Dimitrios. 2018. "Amphiphilic Block Copolymer Microspheres Derived from Castor Oil, Poly(ε-carpolactone), and Poly(ethylene glycol): Preparation, Characterization and Application in Naltrexone Drug Delivery" Materials 11, no. 10: 1996. https://doi.org/10.3390/ma11101996

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