Self-Microemulsifying Drug Delivery System of Phillygenin: Formulation Development, Characterization and Pharmacokinetic Evaluation
Autor: | Yurun Tian, Huanhuan Xue, Lingzhi Wang, Jiankai Tang, Liwei Zhang, Wenrui Yan |
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Jazyk: | angličtina |
Rok vydání: | 2020 |
Předmět: |
phillygenin
lcsh:RS1-441 Pharmaceutical Science 02 engineering and technology Polyethylene glycol Absorption (skin) 030226 pharmacology & pharmacy Article lcsh:Pharmacy and materia medica self-microemulsifying drug delivery system 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Distribution (pharmacology) Self-microemulsifying drug delivery system Active ingredient Chromatography 021001 nanoscience & nanotechnology Bioavailability chemistry oral bioavailability Drug delivery in vitro dissolution 0210 nano-technology pharmacokinetics |
Zdroj: | Pharmaceutics Volume 12 Issue 2 Pharmaceutics, Vol 12, Iss 2, p 130 (2020) |
ISSN: | 1999-4923 |
Popis: | Phillygenin, as an active ingredient of Forsythia suspensa, possesses a wide range of biological and pharmacological activity. However, its development and application are restricted due to its poor bioavailability and low solubility. Our work aimed to develop a self-microemulsifying drug delivery system to improve the oral bioavailability of phillygenin. The composition of the self-microemulsifying drug delivery system was preliminary screened by the pseudo-ternary phase diagram. Subsequently, the central composite design method was employed to optimize the prescription of the self-microemulsifying drug delivery system loaded with phillygenin. The prepared self-microemulsifying drug delivery system of phillygenin was characterized in terms of morphology, droplet size distribution, polydispersity index and stability. Then, the in vitro dissolution and the oral bioavailability were analyzed. The optimized self-microemulsifying drug delivery system of phillygenin consisted of 27.8% Labrafil M1944CS, 33.6% Cremophor EL, 38.6% polyethylene glycol 400 (PEG-400) and 10.2 mg/g phillygenin loading. The prepared self-microemulsifying drug delivery system of phillygenin exhibited spherical and uniform droplets with small size (40.11 ± 0.74 nm) and satisfactory stability. The in vitro dissolution experiment indicated that the cumulative dissolution rate of the self-microemulsifying drug delivery system of phillygenin was significantly better than that of free phillygenin. Furthermore, after oral administration in rats, the bioavailability of phillygenin was significantly enhanced by the self-microemulsifying drug delivery system. The relative bioavailability of the self-microemulsifying drug delivery system of phillygenin was 588.7% compared to the phillygenin suspension. These findings suggest that the self-microemulsifying drug delivery system of phillygenin can be a promising oral drug delivery system to improve the absorption of phillygenin. |
Databáze: | OpenAIRE |
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