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Fabrication of Nanosuspensions to Improve the Oral Bioavailability of Total Flavones from Hippophae rhamnoides L. and their Comparison with an Inclusion Complex
- Source :
- AAPS PharmSciTech. 21
- Publication Year :
- 2020
- Publisher :
- Springer Science and Business Media LLC, 2020.
-
Abstract
- The aim of this work was to increase the solubility and oral bioavailability of isorhamnetin, kaempferol, and quercetin in the total flavones of Hippophae rhamnoides L. (TFH) by preparing their nanosuspensions (NSs) and an inclusion complex. Based on the particle size and zeta potential, P407, Soluplus, SDS, PEG-6000, and HP-β-CD were selected as stabilizers. TFH NSs and a TFH/HP-β-CD inclusion complex were prepared, and their morphology, crystallinity, molecular interactions, and cytotoxicity were investigated. Furthermore, the saturation solubility, dissolution, and pharmacokinetics of the three flavonoids in the TFH, TFH NSs, and TFH/HP-β-CD inclusion complex were compared. The five obtained TFH NSs were physically stable, and their particle sizes were all below 200 nm. The solubility and dissolution of the three active components were obviously enhanced by the formation of the TFH NSs and TFH/HP-β-CD inclusion complex. Correspondingly, the oral bioavailability of isorhamnetin, kaempferol, and quercetin increased up to 4.11-, 3.85-, and 6.73-fold, respectively, in the TFH NSs and 2.89-, 3.71-, and 9.51-fold, respectively, in the TFH/HP-β-CD inclusion complexes compared to those in the raw TFH. In brief, both NSs and inclusion complexes can improve the oral bioavailability of the three flavonoids in TFH. Taking the drug loading and the stable ratio of the multiple components into consideration, the NSs is a more promising strategy than the inclusion complex for increasing the oral bioavailability of multiple water-insoluble components in herbal extracts. Graphical abstract.
- Subjects :
- Male
Administration, Oral
Biological Availability
Pharmaceutical Science
02 engineering and technology
Aquatic Science
030226 pharmacology & pharmacy
Flavones
Rats, Sprague-Dawley
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Pharmacokinetics
Hippophae
Drug Discovery
Animals
Solubility
Ecology, Evolution, Behavior and Systematics
Isorhamnetin
chemistry.chemical_classification
Ecology
biology
Hippophae rhamnoides
General Medicine
021001 nanoscience & nanotechnology
biology.organism_classification
2-Hydroxypropyl-beta-cyclodextrin
Rats
Bioavailability
chemistry
Nanoparticles
0210 nano-technology
Quercetin
Kaempferol
Agronomy and Crop Science
Nuclear chemistry
Subjects
Details
- ISSN :
- 15309932
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- AAPS PharmSciTech
- Accession number :
- edsair.doi.dedup.....1681246c7ce678746d49a011ecdaa5a8