含利培酮原位形成缓释液晶凝胶:体外评价及兔体内药代动力学

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摘要

本研究旨在扩展利培酮持续递送的新载体,以改善精神分裂症治疗。利培酮是一种抗精神病药物,用于治疗各种心理疾病。脂质液晶(LLC)凝胶含有各种脂质、溶剂和稳定剂,在与水介质接触时变成缓释凝胶。方法:对单油酸甘油(GMO)、二油酸甘油(GDO)和三油酸甘油(GTO)以及磷脂酰胆碱(PC)与油和n-甲基-2吡咯烷酮(NMP)溶剂百分比(w/w %)的初始爆发释放(IBR)进行了评估。进行了一些体外评估、药代动力学评估和组织病理学研究,以获得最佳配方。结果:与其他甘油基制剂相比,gdo基LLC显示出较低的IBR。药动学数据显示,GDO在PC:油= 2.2:1和NMP = 30%时缓释2个月。利培酮CONSTA®可在2-3周后达到所需的治疗水平;然而,在滞后期,联合口服利培酮是必不可少的。组织病理学结果显示在家兔中几乎没有副作用。结论:本研究证实了GDO-based LLC与利培酮CONSTA®相比的巨大潜力。此外,结果表明,单次注射gdo基制剂可在治疗范围内保持2个月的体外和体内药物释放。
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Sustained Release In-situ Forming Liquid Crystal Gel Containing Risperidone: In-vitro Evaluation and Pharmacokinetics in Rabbits
Introduction: The present study aimed to extend a novel vehicle for sustained delivery of risperidone to improve schizophrenia therapy. Risperidone is used as an anti-psychotic drug to treat various psychological conditions. Lipid liquid crystal (LLC) gel containing various lipids, solvents, and stabilizers turns into a sustain-release gel in contact with the aqueous medium. Method: Glycerol monooleate (GMO), glycerol dioleate (GDO), and glycerol trioleate (GTO) alongside several ratios of phosphatidylcholine (PC) to oil and N-methyl-2-pyrrolidone (NMP) solvent percent (w/w %) were assessed for initial burst release (IBR) for LLC. Some In-vitro evaluations, pharmacokinetics assessments, and histopathological studies were done to gain optimal formulation. Results: the GDO-based LLC showed lower IBR in comparison to other glycerol-based formulations. Pharmacokinetic data revealed that GDO at PC:oil = 2.2:1 and NMP = 30% made a sustained release for two months. Risperdal CONSTA® can reach the required therapeutic levels after 2–3 weeks; however, over the lag period, co-administration of oral risperidone is essential. The histopathology results indicated approximately no side effects in rabbits. Conclusion: This study confirms the great potential of GDO-based LLC in comparison to Risperdal CONSTA®. Furthermore, the results showed that a single injection of GDO-based formulations could maintain drug release in both in-vitro and in-vivo for two months in the therapeutic range.
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