1. Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China; 2. Jiaxing Key Laboratory of Oncological Photodynamic Therapy and Targeted Drug Research, Jiaxing 314000, China; 3. Shanghai Weier Laboratory, Shanghai 201712, China
Abstract：OBJECTIVE To prepare a lyophilized powder of paclitaxel palmitate albumin nanoparticles (Nab-PTX-PA) was prepared, and its antitumor effect and bone marrow suppression toxicity were evaluated. METHODS Nanoparticle albumin evaluate (NabTM technology) was used to prepare Nab-PTX-PA. The morphology, particle size and potential of Nab-PTX-PA formulation were characterized and compared before and after lyophilization of Nab-PTX-PA Changes in particle size and potential after reconstitution. By constructing a 4T1 tumor-bearing mouse model, the anti-tumor activity of Nab-PTX-PA was investigated. After the administration of tumor-bearing mice, routine blood tests were conducted to investigate the bone marrow suppression toxicity of the preparation. RESULTS In this study, Nab-PTX-PA lyophilized powder with smooth and full appearance and good dispersibility after reconstitution in normal saline was prepared, and the particle size of Nab-PTX-PA lyophilized powder was (87.63±1.15) nm (n=3). The Zeta potential was (-11.7±0.61) mV (n=3), and the particle size and potential of Nab-PTX-PA did not change significantly before lyophilization and after reconstitution. The RESULTS of pharmacodynamic studies showed that the antitumor effect of Nab-PTX-PA (51.16 mg·kg-1) was higher than that of Abraxane® (20 mg·kg-1), and it was statistically significant. Bone marrow suppression toxicity RESULTS show that Nab-PTX-PA (25.58 mg·kg-1) has lower bone marrow suppression toxicity in mice than the equal-dose commercially available drug Abraxane® , while Nab-PTX-PA (51.16 mg·kg-1) of bone marrow suppression toxicity is comparable to the commercially available drug Abraxane® (20 mg·kg-1). CONCLUSION Nab-PTX-PA lyophilized powder prepared by NabTM technology has stable properties. Nab PTX PA (25.58 mg·kg-1) and the same dose of Abraxane® (20 mg·kg-1), nab PTX PA (51.16 mg·kg-1) and Abraxane® (20 mg·kg-1) has the same toxicity, and the antitumor effect is obvious.
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2022, Vol. 57 
