Journal of Chinese Pharmaceutical Sciences ›› 2020, Vol. 29 ›› Issue (8): 554-563.DOI: 10.5246/jcps.2020.08.052

• Original articles • Previous Articles     Next Articles

Preparation and in vitro evaluation of APT011-loaded sustained-release microspheres

Chengqun Li1,2, Xia Niu2, Jiahui Mu2, Xiaomei Wang2, Jin Su1*, Guiling Li2*   

  1. 1. Department of Pharmacy, Jiamusi University, Jiamusi 154007, China
    2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Science & Peking Union Medical College, Beijing 100050, China
  • Received:2020-03-12 Revised:2020-04-19 Online:2020-08-31 Published:2020-05-18
  • Contact: Tel.: +86-13803659063; +86-10-67022156, E-mail:;
  • Supported by:
    National Science & Technology Major Project “Key New Drug Creation and Manufacturing” (Grant No. 2019ZX09201001-003-007).


In the present study, we aimed to prepare sustained-release microspheres for injection of neurokinin-1 (NK-1) receptor antagonist APT011, and to evaluate their physicochemical properties, in vitro sustained-release effect and preliminary stability. APT011-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique. The L9 (34) orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation. Microscope photographs showed that APT011-loaded microspheres were spherical, and the particle size was ~90 μm with uniform size distribution. XRD results indicated that APT011 existed in the microspheres in an amorphous form. DSC results showed that there was no significant interaction between APT011 and blank microspheres. APT011-loaded microspheres had a significant sustained-release effect, which maintained release for at least 2 months. Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40 °C and under high lighting condition. APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability, demonstrating real potential for the clinical practice.

Key words: PLGA, Microsphere, Prescription technology, In vitro evaluation, Preliminary stability

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