Preparation of core-shell targeted tracer recombinant human interleukin II microspheres via coaxial electrostatic spraying

doi:10.5246/jcps.2024.06.037

Abstract

Abstract:

The potential application of recombinant human interleukin-2 (rhIL-2) in promoting immune cell proliferation and differentiation for the treatment of lung cancer is acknowledged. However, the inherent challenges associated with the short half-life and instability of rhIL-2 necessitate its encapsulation into microspheres for sustained release administration. In this study, the coaxial electrostatic spray technique was employed to fabricate rhIL-2-loaded core-shell microspheres. Quantum dots served as tracer materials, and the core-shell composite microspheres were fashioned with chitosan coating the rhIL-2 and quantum dots conjugates in the core layer and hyaluronic acid in the shell layer. A systematic exploration of factors such as carrier concentration, positive voltage, pinhole diameter, and spray flow rate was conducted using a single-factor method. The coaxial electrostatic spray process parameters for core-shell microsphere preparation were also meticulously optimized. The results indicated that the developed core-shell microspheres exhibited a favorable particle size ranging from 1.2 to 2.0 μm, accompanied by encapsulation efficiency and drug loading values of 78.39% ± 1.96% and 19.58 ± 2.76 μg/mg, respectively. In vitro release studies demonstrated a sustained release effect without any discernible burst release phenomenon. Biological activity assessments revealed that rhIL-2 within the core-shell microspheres mirrored the efficacy of the free protein drug. Additionally, in vivo imaging analysis attested to the active targeting properties of the microspheres. These findings robustly supported the successful development of sustained-release targeted rhIL-2-loaded microspheres, providing a theoretical foundation for protein-microsphere formulations.

Key words: Coaxial spray, Quantum dots, Hyaluronic acid, Microspheres

Supporting:

Yuan Zhu, Jiaqi Xu, Xiaoyan Chen, Yingshu Feng, Caleb Kesse Firempong, Haibing He, Hongfei Liu. Preparation of core-shell targeted tracer recombinant human interleukin II microspheres via coaxial electrostatic spraying[J]. Journal of Chinese Pharmaceutical Sciences, 2024, 33(6): 495-510.

Figures/Tables 16

Table 1. In vitro release curve fitting of microspheres.

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