在药物研发领域,如何有效提高难溶性药物的溶解与吸收是一个极具挑战的难题。目前,过饱和药物递送系统(Supersaturating drug delivery systems,SDDS)利用药物溶液处于过饱和态的优势,可同时提高难溶性药物的表观溶解度与渗透性。本文...在药物研发领域,如何有效提高难溶性药物的溶解与吸收是一个极具挑战的难题。目前,过饱和药物递送系统(Supersaturating drug delivery systems,SDDS)利用药物溶液处于过饱和态的优势,可同时提高难溶性药物的表观溶解度与渗透性。本文对过饱和度的理论及其在药物研发领域中的实际应用进行了系统的综述,介绍了过饱和度的产生与维持、及其与药物吸收的关系,归纳了常用的SDDS技术,并对无定形固体分散体、共晶、无定形/共无定形产生过饱和进行重点阐述。展开更多
Image-guided thermal ablation(TA),which is less invasive,has been widely applied for treating various kinds of tumors.However,TA still poses the potential risk of thermal damage to sensitive tissue nearby.Therefore,an...Image-guided thermal ablation(TA),which is less invasive,has been widely applied for treating various kinds of tumors.However,TA still poses the potential risk of thermal damage to sensitive tissue nearby.Therefore,an adjunctive thermoprotective hydrodissection technique with constant injection of 5%glucose(5%Glu)has currently been adopted for clinical application,but this may be hazardous to humans.In this study,a multifunctional hyaluronic acid-based hydrogel(HA-Dc)was developed for hydrodissection.Compared with 5%Glu(the most clinically used solution)and the previously reported F127 hydrogel,the HA-Dc hydrogel was studied in vitro in a porcine liver model and in vivo in a rabbit model and showed good injectability and better tissue retention,stability,and thermoprotective properties throughout the TA procedure.Furthermore,in the preclinical evaluation in a Macaca fascicularis(M.fascicularis)model,HA-Dc showed excellent performance in terms of stricter neuroprotection compared with 5%Glu.In addition,the HA-Dc hydrogel with good biocompatibility and controllable degradation behavior in vivo could be a promising platform for thermal protection during clinical TA procedures.展开更多
文摘在药物研发领域,如何有效提高难溶性药物的溶解与吸收是一个极具挑战的难题。目前,过饱和药物递送系统(Supersaturating drug delivery systems,SDDS)利用药物溶液处于过饱和态的优势,可同时提高难溶性药物的表观溶解度与渗透性。本文对过饱和度的理论及其在药物研发领域中的实际应用进行了系统的综述,介绍了过饱和度的产生与维持、及其与药物吸收的关系,归纳了常用的SDDS技术,并对无定形固体分散体、共晶、无定形/共无定形产生过饱和进行重点阐述。
基金financially supported by the National Natural Science Foundation of China(81971632,51773231)the Natural Science Foundation of Guangdong Province(2020A1515010425,2022A1515010024)+1 种基金Key Scientific and Technological Program of Guangzhou City(201802020023)Shenzhen Science and Technology Project(JCYJ20190807160801664,JCYJ20220818103207016).
文摘Image-guided thermal ablation(TA),which is less invasive,has been widely applied for treating various kinds of tumors.However,TA still poses the potential risk of thermal damage to sensitive tissue nearby.Therefore,an adjunctive thermoprotective hydrodissection technique with constant injection of 5%glucose(5%Glu)has currently been adopted for clinical application,but this may be hazardous to humans.In this study,a multifunctional hyaluronic acid-based hydrogel(HA-Dc)was developed for hydrodissection.Compared with 5%Glu(the most clinically used solution)and the previously reported F127 hydrogel,the HA-Dc hydrogel was studied in vitro in a porcine liver model and in vivo in a rabbit model and showed good injectability and better tissue retention,stability,and thermoprotective properties throughout the TA procedure.Furthermore,in the preclinical evaluation in a Macaca fascicularis(M.fascicularis)model,HA-Dc showed excellent performance in terms of stricter neuroprotection compared with 5%Glu.In addition,the HA-Dc hydrogel with good biocompatibility and controllable degradation behavior in vivo could be a promising platform for thermal protection during clinical TA procedures.