Open AccessA novel preparative method for nanoparticle albumin-bound paclitaxel with high drug loading and its evaluation both in vitro and in vivo
Author(s) -
Yue Gao,
Jingxue Nai,
Zhongzhen Yang,
Jinbang Zhang,
Siyu Ma,
Yumei Zhao,
Hui Li,
Jiaxin Li,
Yang Yang,
Meiyan Yang,
Yuli Wang,
Wenbin Gong,
Fanglin Yu,
Chunsheng Gao,
Zhiping Li,
Xingguo Mei
Publication year - 2021
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0250670
Subject(s) - paclitaxel , chemistry , in vivo , polyethylene glycol , peg ratio , human serum albumin , differential scanning calorimetry , nanoparticle , chromatography , albumin , in vitro , drug , pharmacology , materials science , nanotechnology , medicine , biochemistry , surgery , chemotherapy , physics , microbiology and biotechnology , finance , economics , biology , thermodynamics
We developed a novel preparative method for nanoparticle albumin-bound (nab) paclitaxel with high drug loading, which was based on improved paclitaxel solubility in polyethylene glycol (PEG) and self-assembly of paclitaxel in PEG with albumin powders into nanoparticles. That is, paclitaxel and PEG were firstly dissolved in ethanol, which was subsequently evaporated under vacuum. The obtained liquid was then mixed with human serum albumin powders. Thereafter, the mixtures were added into phosphate-buffered saline and nab paclitaxel suspensions emerged after ultrasound. Nab paclitaxel was finally acquired after dialysis and freeze drying. The drug loading of about 15% (W/V) were realized in self-made nab paclitaxel, which was increased by approximately 50% compared to 10% (W/V) in Abraxane. Now this new preparative method has been authorized to obtain patent from China and Japan. The similar characteristics of self-made nab paclitaxel compared to Abraxane were observed in morphology, encapsulation efficiency, in vitro release, X-ray diffraction analysis, differential scanning calorimetry analysis, and circular dichroism spectra analysis. Consistent concentration-time curves in rats, biodistributions in mice, anti-tumor activities in mice, and histological transmutation in mice were also found between Abraxane and self-made nanoparticles. In a word, our novel preparative method for nab paclitaxel can significantly improve drug loading, obviously decrease product cost, and is considered to have potent practical value.