In situ hexagonal liquid crystal for intra-articular delivery of sinomenine hydrochloride - 31/07/19
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Highlights |
• | The ISH was prepared by a liquid precursor mixture containing phytantriol (PT), Vitamin E acetate (VEA), ethanol (ET), and water (PT/VEA/ET/water, 60.8:3.2:16.0:20.0, w/w/w/w). |
• | Effects of VEA on the phase structure of liquid crystals and the in vitro drug release behavior for sustained drug delivery system. |
• | The ISH reduced the leakage of SMH into the systemic circulation. |
• | The SMH loaded ISH has a positive correlation between the concentration of SMH in synovium and the anti-inflammatory effect. |
Abstract |
The aim of this study was to investigate the release behaviors of sinomenine hydrochloride loaded via in situ hexagonal liquid crystal (ISH), and its potential to improve the local bioavailability in knee joints of sinomenine hydrochloride (SMH) after intra-articular administration. The ISH was prepared by a liquid precursor mixture containing phytantriol (PT), Vitamin E acetate (VEA), ethanol (ET), and water. The in vitro release profiles revealed a sustained release of SMH from the optimized ISH formula (PT/VEA/ET/water, 60.8:3.2:16.0:20.0, w/w/w/w), which was selected for the in vivo pharmacokinetics and preliminary pharmacodynamics studies. In both healthy and adjuvant-induced arthritis (AA) rats, the SMH loaded ISH showed significantly smaller SMH AUC0-∞ in plasma (P < 0.01), and higher SMH concentration in synoviums (2˜168 h) than that of SMH solution, indicating that the ISH significantly reduced the leakage of SMH into systemic circulation. The t1/2α of SMH loaded ISH in the knee joints of AA rats, was longer (13.42 h) than that of healthy rats (1.34 h) (P < 0.05), most likely that in vivo drug release behavior of SMH loaded ISH was affected by the physiological environment of the joint. It was found that the SMH loaded ISH could benefit AA-rats by suppressing the level of IL-1β in comparison to SMH solutions. The results of the histopathology of knee joints in AA rats displayed that the SMH loaded ISH might be suitable for the development of treatment strategies for rheumatoid arthritis diseases.
Le texte complet de cet article est disponible en PDF.Keywords : In Situ hexagonal liquid crystal, Sinomenine hydrochloride, Rheumatoid arthritis, Sustained release, Intra-articular administration
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Vol 117
Article 108993- septembre 2019 Retour au numéro
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