Preparation and evaluation in vitro and in vivo of pristinamycin enteric-coated granules based on albumin nanoparticles

Abstract

Context

The purpose of this study was to prepare enteric-coated particles based on albumin nanoparticles (NPs) using a mixture of PI_A albumin NPs freeze-dried powder (PA-PI_A) and PII_A albumin NPs freeze-dried powder (PA-PII_A) to improve the bioavailability effect of pristinamycin.

Objective

This is the first study on the preparation of pristinamycin into enteric-coated granules based on albumin NPs, and our study has effectively improved the bioavailability of pristinamycin and ensured its safety.

Methods

Pristinamycin albumin enteric-coated granules (PAEGs) were prepared by hybrid wet granulation. The characterizations of albumin NPs were performed by in vitro and in vivo studies of PAEGs. The assays were analyzed using zeta-sizer, transmission electron microscopy, high-performance liquid chromatography, and a fully automated biochemical index analyzer.

Results

The morphology of NPs was close to spherical. PI_A-NPs and PII_A-NPs respectively had a zeta potential of (−24.33 ± 0.75) mV and (+7.30 ± 0.27) mV and mean size of (251.91 ± 19.64) nm and (232.83 ± 22.61) nm. The release of PI_A and PII_A from PAEGs in the artificial gastrointestinal fluid was as high as 58.46% and 87.79%. In the experimental group of oral PAEGs, PI_A and PII_A were AUC_(0-t) (3.68 ± 0.58) mg·L⁻¹·h⁻¹ and (2.81 ± 1.06) mg·L⁻¹·h⁻¹. The results of aspartate aminotransferase and alanine aminotransferase biochemical indices showed that there was no significant difference between the experimental and normal groups of oral PAEGs.

Conclusion

The PAEGs significantly increased the release of PI_A and PII_A in simulated intestinal fluid and improved the bioavailability. The oral administration of PAEGs may not damage the liver of rats. We hope that our study will promote its industrial development or clinical application.

Keywords:

• Pristinamycin
• albumin nanoparticles
• enteric-coated granules
• oral administration
• pharmacokinetics

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The author(s) reported there is no funding associated with the work featured in this article.