PDF(Pubmed)
Abstract：
BACKGROUND: Hydroxy-α-Sanshool (HAS) possesses various pharmacological properties, such as analgesia and regulating gastrointestinal function. However, the low oral bioavailability of HAS has limited its oral delivery in clinical application.
RESULTS: To enhance its oral bioavailability, a nanocomposite delivery system based on chitosan (CH, as the polycation) and sodium alginate (SA, as the polyanion) was prepared using a layer-by-layer coating technique. The morphology, thermal behavior and Fourier transform infrared spectrum (FTIR) showed that the obtained sodium alginate/chitosan-coated HAS-loaded liposomes (SA/CH-HAS-LIP) with core-shell structures have been successfully covered with polymers. When compared with HAS-loaded liposomes (HAS-LIP), SA/CH-HAS-LIP displayed obvious pH sensitivity and a sustained-release behavior in in vitro studies, which fitted well to Weibull model. In vivo, the half-life of HAS from SA/CH-HAS-LIP remarkably extended after oral administration compared to the free drug. Additionally, it allowed a 4.6-fold and 4.2-fold increase in oral bioavailability, respectively, compared with free HAS and HAS-LIP.
CONCLUSIONS: SA/CH-HAS-LIP could be a promising release vehicle for the oral delivery of HAS to increase its oral bioavailability.
RESULTS: To enhance its oral bioavailability, a nanocomposite delivery system based on chitosan (CH, as the polycation) and sodium alginate (SA, as the polyanion) was prepared using a layer-by-layer coating technique. The morphology, thermal behavior and Fourier transform infrared spectrum (FTIR) showed that the obtained sodium alginate/chitosan-coated HAS-loaded liposomes (SA/CH-HAS-LIP) with core-shell structures have been successfully covered with polymers. When compared with HAS-loaded liposomes (HAS-LIP), SA/CH-HAS-LIP displayed obvious pH sensitivity and a sustained-release behavior in in vitro studies, which fitted well to Weibull model. In vivo, the half-life of HAS from SA/CH-HAS-LIP remarkably extended after oral administration compared to the free drug. Additionally, it allowed a 4.6-fold and 4.2-fold increase in oral bioavailability, respectively, compared with free HAS and HAS-LIP.
CONCLUSIONS: SA/CH-HAS-LIP could be a promising release vehicle for the oral delivery of HAS to increase its oral bioavailability.
摘要：
背景：羟基-α-Sanshool（HAS）具有多种药理特性，如镇痛和调节胃肠功能。然而,HAS口服生物利用度低,限制了其口服给药的临床应用。
结果：为了提高其口服生物利用度，一种基于壳聚糖(CH，作为聚阳离子）和海藻酸钠（SA，作为聚阴离子）是使用逐层涂覆技术制备的。形态学,热行为和傅里叶变换红外光谱（FTIR）表明，所获得的海藻酸钠/壳聚糖包覆的具有核壳结构的HAS脂质体（SA/CH-HAS-LIP）已成功地被聚合物覆盖。当与HAS负载脂质体（HAS-LIP）相比时，SA/CH-HAS-LIP在体外研究中表现出明显的pH敏感性和缓释行为,这与威布尔模型非常吻合。在体内,与游离药物相比，口服后SA/CH-HAS-LIP的HAS半衰期显着延长。此外,它使口服生物利用度增加了4.6倍和4.2倍，分别,与免费HAS和HAS-LIP相比。
结论：SA/CH-HAS-LIP可能是一种有希望的HAS口服释放载体，以增加其口服生物利用度。
结果：为了提高其口服生物利用度，一种基于壳聚糖(CH，作为聚阳离子）和海藻酸钠（SA，作为聚阴离子）是使用逐层涂覆技术制备的。形态学,热行为和傅里叶变换红外光谱（FTIR）表明，所获得的海藻酸钠/壳聚糖包覆的具有核壳结构的HAS脂质体（SA/CH-HAS-LIP）已成功地被聚合物覆盖。当与HAS负载脂质体（HAS-LIP）相比时，SA/CH-HAS-LIP在体外研究中表现出明显的pH敏感性和缓释行为,这与威布尔模型非常吻合。在体内,与游离药物相比，口服后SA/CH-HAS-LIP的HAS半衰期显着延长。此外,它使口服生物利用度增加了4.6倍和4.2倍，分别,与免费HAS和HAS-LIP相比。
结论：SA/CH-HAS-LIP可能是一种有希望的HAS口服释放载体，以增加其口服生物利用度。
