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Effect of Drug Carrier Melting Points on Drug Release of Dexamethasone-Loaded Microspheres

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Tissue Engineering and Regenerative Medicine Aims and scope

Abstract

Here, we examined the effect of melting point of drug carriers on drug release of dexamethasone (Dex)-loaded microspheres. We prepared poly(L-lactide-ran-ε-caprolactone) (PLC) copolymers with varying compositions of poly(ε-caprolactone) (PCL) and poly(L-lactide) (PLLA). As the PLLA content increased, the melting points of PLC copolymers decreased from 61 to 43 °C. PLC copolymers in vials solubilized at 40–50 °C according to the incorporation of PLLA into the PCL segment. Dexamethasone (Dex)-loaded PLC (MCxLy) microspheres were prepared by the oil-in-water (O/W) solvent evaporation/extraction method. The preparation yields were above 70%, and the mean particle size ranged from 30 to 90 μm. The MCxLy microspheres also showed controllable melting points in the range of 40–60 °C. Dex-loaded MCxLy microspheres showed similar in vitro and in vivo sustained release patterns after the initial burst of Dex. The in vitro and in vivo order of the Dex release was MC80L20 > MC90L10 > MC95L5, which agreed well with the melting point order of the drug carrier. Using in vivo fluorescence imaging of fluorescein (FI)-loaded microspheres implanted in animals, we confirmed the sustained release of FI over an extended period. In vivo inflammation associated with the PLC microsphere implants was less pronounced than that associated with Poly(lactide-co-glycolide) (PLGA). In conclusion, we successfully demonstrated that it is possible to control Dex release using Dex-loaded MCxLy microspheres with different melting points.

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Acknowledgements

This study was supported by a grant from a Basic Science Research Program (2016R1A2B3007448) through the National Research Foundation of Korea (NRF) funded by the Ministry of Education.

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  1. Ji Hoon Park and Doo Yeon Kwon are equal first authors.

Authors and Affiliations

  1. Department of Molecular Science and Technology, Ajou University, 206 Worldcup-ro, Yeongtong-gu, Suwon, 16499, Korea

    Ji Hoon Park, Doo Yeon Kwon, Ji Yeon Heo, Seung Hun Park, Joon Yeong Park, Jae Ho Kim & Moon Suk Kim

  2. Department of Polymer Engineering, Pukyong National University, 365 Sinseon-ro, Nam-gu, Busan, 48547, Korea

    Bong Lee

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  1. Ji Hoon Park
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Correspondence to Moon Suk Kim.

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The authors declare that they have no conflict of interest.

Ethical statement

This study was conducted under the approval of the Institutional Animal Experiment Committee at Ajou University School of Medicine (Approval No. 2016-0048).

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Park, J.H., Kwon, D.Y., Heo, J.Y. et al. Effect of Drug Carrier Melting Points on Drug Release of Dexamethasone-Loaded Microspheres. Tissue Eng Regen Med 14, 743–753 (2017). https://doi.org/10.1007/s13770-017-0077-7

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  • DOI: https://doi.org/10.1007/s13770-017-0077-7

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