Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 172, Issue -, Pages 372-379Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2018.08.016
Keywords
Amphotericin B; Nanosuspensions; High pressure homogenization; Antisolvent precipitation; Solubility; Bioavailability
Funding
- National Natural Science Foundation of China [81773660]
- Natural Science Fund Project of Guangdong Province [2016A030312013]
- Science and Technology Foundation of Nansha District [2016KF012]
- 111 project [B16047]
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Amphotericin B (AmB) is a widely used polyene antifungal agent; however, its poor solubility limits its clinical application. In this study, AmB nanosuspensions were prepared by a high pressure homogenization method (AmB-HPH) and an antisolvent precipitation method (AmB-AP) to improve the drug solubility. To reveal the distinct influences of these two different preparation methods, systematic comparisons of particle size, crystalline state, wettability, in vitro dissolution and in vivo pharmacokinetics on the properties of AmB-HPH and AmB-AP were performed. The results indicated that AmB-AP was in an amorphous state, exhibiting higher saturation solubility and dissolution rate than those of AmB-HPH in the crystalline state. However, the relative bioavailability of AmB-HPH was higher than that of AmB-AP in vivo, which was likely attributed to its better stability. In conclusion, both AmB-HPH and AmB-AP can enhance the solubility and bioavailability of AmB, but the stability of the nanosuspension prepared by the anti-solvent precipitation method should be carefully considered.
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