1. Poloxamer modified florfenicol instant microparticles for improved oral bioavailability.
- Author
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Zhang W, Liu CP, Chen SQ, Liu MJ, Zhang L, Lin SY, Shu G, Yuan ZX, Lin JC, Peng GN, Zhong ZJ, Yin LZ, Zhao L, and Fu HL
- Subjects
- Administration, Oral, Animals, Biological Availability, Particle Size, Poloxamer administration & dosage, Poloxamer chemistry, Rabbits, Solubility, Surface Properties, Thiamphenicol administration & dosage, Thiamphenicol blood, Thiamphenicol pharmacokinetics, Poloxamer pharmacokinetics, Thiamphenicol analogs & derivatives
- Abstract
Surfactants can improve the hydrophobicity of poorly water-soluble drugs and increase the stability of microparticles by reducing surface tension. This study describes that surfactant-engineered florfenicol instant microparticles (FIMs) increase bioavailability through a micellar solubilization mechanism. The FIMs were prepared by a modified emulsification method, and the optimal prescription was obtained by a combination of single factor investigation and response surface methodology. The microparticles prepared in this study reduce the polymer materials while increasing the drug content. FIM has a smaller particle size and modification of poloxamer, resulting in better solubility and higher bioavailability. The in vitro solubility of FIM is 1.43 times higher than that of the bulk drug, and the dissolution equilibrium can be achieved in 10 minutes. Compared with florfenicol, FIM showed a decrease in T
max in the plasma concentration curve, with a peak concentration of 1.43 times and an area of 1.41 times. Considering the advantages of in vitro/in vivo performance and ease of preparation, FIMs may have great application prospects in pharmacy research., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier B.V. All rights reserved.)- Published
- 2020
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