Abstract
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.
Highlights
Since nab paclitaxel is composed of paclitaxel and human serum albumin (HSA), the content of paclitaxel in nanoparticles is crucial
The particle size increased as a function of paclitaxel content. This result may have been due to the fact that the viscosity of paclitaxel-polyethylene glycol (PEG) complexes raises with increasing paclitaxel content, which makes it difficult to disperse mixtures of HSA and paclitaxel-PEG into aqueous solutions and result in large paclitaxel-HSA particles
The highest inhibitory effect above 95% was observed in mice administered Abraxane or self-made nanoparticles at the dose of 15mg/kg. All of these results indicate that the anti-tumor activity of paclitaxel was significantly improved through the introduction of albumin nanoparticles, which is likely related to enhanced drug distribution in tumor tissues caused by albumin
Summary
A novel preparative method for nanoparticle albumin-bound paclitaxel with high drug loading treatment of a wide variety of cancers, such as breast, lung, and advanced ovarian cancers [1,2,3]. A novel preparative method for nanoparticle albumin-bound paclitaxel with high drug loading for albumin-based nanoparticle formation [23] In spite of these current loading trends, low entrapment efficiency and introduced toxicity are predominant issues in solvent media preparation for these HSA nanoparticles [23]. A novel preparative method for nanoparticle albumin-bound paclitaxel with high drug loading methods This new preparative method has been applied for patent in China and Patent Coorperation System, and has been authorized to obtain the invention patent from China National Intellectual Property Administration and Japan Patent Office [24, 25]
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