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      Preparation and physicochemical characterization of T-OA PLGA microspheres

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          As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3 β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin- 2-methyl ester (T-OA). Early-stage preparation discovery concept (EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water (O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and high performance liquid chromatography (HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 μm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r 2 = 0.994 7. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.

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          Author and article information

          Chinese Journal of Natural Medicines
          20 December 2017
          : 15
          : 12
          : 912-916
          1Beijing Institute of Traditional Chinese Medicine, Beijing Hospital of Traditional Chinese Medicine, Beijing100010, China
          2School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China
          Author notes
          *Corresponding author: NI Jian, Tel: +86-010-84738607, E-mail: njtcm@

          These authors have no conflict of interest to declare.

          Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
          Funded by: Innovation Team of Beijing University of Chinese Medicine
          Award ID: 2011-CXTD-13
          Funded by: Collaborative Innovation Construction Plan of Beijing University of Chinese Medicine
          Award ID: 2013-XTCX-03
          This work was supported by the Innovation Team of Beijing University of Chinese Medicine (No. 2011-CXTD-13) and the Collaborative Innovation Construction Plan of Beijing University of Chinese Medicine (No. 2013-XTCX-03).


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