In vitro and in vivo evaluation of a water‐in‐oil microemulsion of platycodin D
| Autor: | Jinyang Shen, Bingxue Zhou, Cao Zhiling, Ji Jing, Di Zhang, Yuexia Zhu, Li Jiaojiao, Li Kong, Ye Jin |
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| Rok vydání: | 2021 |
| Předmět: |
Male
Platycodon Pharmaceutical Science 01 natural sciences Rats Sprague-Dawley chemistry.chemical_compound In vivo Drug Discovery Animals Microemulsion Particle Size Phospholipids Chromatography Aqueous solution Ethanol Viscosity 010405 organic chemistry Chemistry Platycodin D Water Hydrogen-Ion Concentration Saponins Triterpenes Rats 0104 chemical sciences Bioavailability 010404 medicinal & biomolecular chemistry Oleic acid Intestinal Absorption Permeability (electromagnetism) Area Under Curve Emulsions Titration Soybeans Half-Life Oleic Acid |
| Zdroj: | Archiv der Pharmazie. |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.202000497 |
| Popis: | Platycodin D (PD) is the active metabolite of Platycodon grandiflorum. The main purpose of this study was to develop and evaluate a water-in-oil (W/O) microemulsion formulation of PD (PD-ME). The PD-ME was successfully prepared by the water titration method at K m = 2, to draw the pseudoternary phase diagrams. Physical characterization including the particle size, pH, refractive index, average viscosity, and polydispersity index (PDI) was performed. The in vivo characteristics were evaluated by intestinal permeability and pharmacokinetic studies. The optimized microemulsion formulation consisted of 100 mg/ml PD aqueous solution, soybean phospholipids, ethanol, and oleic acid (27:39:19:15, w/w). The average viscosity, pH, droplet size, PDI, and zeta potential of the PD-ME were 78.65 ± 0.13 cPa•s, 5.70 ± 0.05, 30.46 ± 0.20 nm, 0.33 ± 0.00, and -3.13 mV, respectively. The drug concentration of the PD-ME was 26.3 ± 0.6 mg/ml. The PD-ME showed significantly higher apparent permeability coefficients than PD (p |
| Databáze: | OpenAIRE |
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