Abstract | Background: Methods: CsA-NSs were prepared using a wet bead milling method. Particle size, morphology and crystallinity state of CsA-NSs were characterized. The in vitro dissolution, the intestinal absorption properties and pharmacokinetic study of CsA-NSs were investigated. Results: CsA-NSs with sizes of 280 nm, 522 nm and 2967 nm were prepared. The shape of CsA-NSs with smaller size was similar to that of spheres. The crystallinity of CsA in nanocrystals was reduced. The dissolution rate of CsA-NSs (280 nm) was greater than that of CsA-NSs (522 nm) and CsA-NSs (2967 nm). CsA-NSs (280 nm) showed higher absorption rate constants (Kα ) and effective permeability coefficients (Peff ) of different intestinal segments compared with that of CsA-NSs (522 nm) and CsA-NSs (2967 nm). AUC0-48h of 280 nm CsA-NSs was about 1.12-fold of that of 522 nm CsA-NSs, and about 1.51-fold of that of 2967 nm CsA-NSs. In particular, the particle size of CsA-NSs was nanoscale, and their bioavailability was bioequivalent with marked self-microemulsion ( Sandimmun Neoral®). Conclusion: It is feasible to prepare CsA-NSs. The dissolution rate, gastrointestinal transport properties and the oral absorption of CsA-NSs were promoted by reducing size. Considering the cost, efficiency and energy consumption, there should be an optimal particle size range in industrial production.
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Authors | Wenjun Sun, Jing Gao, Ranran Fan, Ting Zhang, Yang Tian, Zengming Wang, Hui Zhang, Aiping Zheng |
Journal | International journal of nanomedicine
(Int J Nanomedicine)
Vol. 17
Pg. 1741-1755
( 2022)
ISSN: 1178-2013 [Electronic] New Zealand |
PMID | 35469173
(Publication Type: Journal Article)
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Copyright | © 2022 Sun et al. |
Chemical References |
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Topics |
- Administration, Oral
- Biological Availability
- Cyclosporine
(pharmacokinetics)
- Particle Size
- Suspensions
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