In the fight against cancer, controlled drug delivery systems have emerged to enhance the therapeutic efficacy and safety of anti-cancer drugs. Among these systems, mesoporous silica nanoparticles （MSNs） with a func...In the fight against cancer, controlled drug delivery systems have emerged to enhance the therapeutic efficacy and safety of anti-cancer drugs. Among these systems, mesoporous silica nanoparticles （MSNs） with a functional surface possess obvious advantages and were thus rapidly developed for cancer treatment. Many stimuli-responsive materials, such as nanopartides, polymers, and inorganic materials, have been applied as caps and gatekeepers to control drug release from MSNs. This review presents an overview of the recent progress in the production of pH-responsive MSNs based on the pH gradient between normal tissues and the tumor microenvironment. Four main categories of gatekeepers can respond to acidic conditions. These categories will be described in detail.展开更多
Electrospinning is a very simple and versatile process by which polymer nanofibers with di-ameters ranging from a few nanometers to sev-eral micrometers can be produced using an electrostatically driven jet of polymer...Electrospinning is a very simple and versatile process by which polymer nanofibers with di-ameters ranging from a few nanometers to sev-eral micrometers can be produced using an electrostatically driven jet of polymer solution or polymer melt. Significant progress has been made in this process throughout the past few years and electrospinning has advanced its ap-plications in many fields, including pharmaceu-tics. Electrospun nanofibers show great prom-ise for developing many types of novel drug delivery systems (DDS) due to their special characteristics and the simple but useful and effective top-down fabricating process. The current state of electrospun nanofiber-based DDS is focused on drug-loaded nanofiber preparation from pharmaceutical and biode-gradable polymers and different types of DDS. However, there are more opportunities to be exploited from the electrospinning process and the corresponding drug-loaded nanofibers for drug delivery. Additionally, some other related challenges and the possible resolutions are outlined in this review.展开更多
目的制备利格列汀自乳化释药系统(linagliptin self-nanoemulsifying drug delivery systems,LGP-SNEDDSs),并考察其大鼠体内药动学。方法通过测定利格列汀在不同油相、表面活性剂和助表面活性剂中的溶解度,确定LGP-SNEDDSs的处方组成;...目的制备利格列汀自乳化释药系统(linagliptin self-nanoemulsifying drug delivery systems,LGP-SNEDDSs),并考察其大鼠体内药动学。方法通过测定利格列汀在不同油相、表面活性剂和助表面活性剂中的溶解度,确定LGP-SNEDDSs的处方组成;通过伪三元相图法获得其处方用量;评价了LGP-SNEDDSs的理化性质以及体外药物溶出速率;考察利格列汀混悬液和LGP-SNEDDSs经大鼠灌胃给药后的体内药动学。结果溶解度实验结果显示,分别选择辛酸/癸酸甘油三酯、辛酸癸酸聚乙二醇甘油酯和二乙二醇单乙基醚作为LGP-SNEDDSs的油相、表面活性剂和助表面活性剂,用量配比为6:3:1;LGP-SNEDDSs经水稀释后形成淡蓝色微乳液,在透射电镜下可观察到微乳呈球形或类球形,大小均匀,平均乳滴大小为(63.4±7.8)nm;体外溶出结果显示,LGP-SNEDDSs中的药物在10 min内可完全溶出,显著高于利格列汀片中药物溶出速度;稳定性结果显示LGP-SNEDDSs在加速条件下放置3个月稳定性良好。大鼠药动学结果显示,LGP-SNEDDSs可提高药物达峰浓度和生物利用度。结论将利格列汀制备成自乳化释药系统,可有效提高体内的生物利用度,对利格列汀的二次开发利用具有重要意义。展开更多
基金supported by the Chinese Natural Science Foundation Project (Grant No. 30970784 and 81171455)a National Distinguished Young Scholars Grant (Grant No. 31225009) from the National Natural Science Foundation of China+5 种基金the National Key Basic Research Program of China (Grant No. 2009CB930200)the Chinese Academy of Sciences (CAS) ‘Hundred Talents Program’ (Grant No. 07165111ZX)the CAS Knowledge Innovation Program, and the State HighTech Development Plan (Grant No. 2012AA020804)the ‘Strategic Priority Research Program’ of the Chinese Academy of Sciences (Grant No. XDA09030301)NIH/NIMHD 8 G12 MD007597USAMRMC W81XWH-10-1-0767 grants
文摘In the fight against cancer, controlled drug delivery systems have emerged to enhance the therapeutic efficacy and safety of anti-cancer drugs. Among these systems, mesoporous silica nanoparticles （MSNs） with a functional surface possess obvious advantages and were thus rapidly developed for cancer treatment. Many stimuli-responsive materials, such as nanopartides, polymers, and inorganic materials, have been applied as caps and gatekeepers to control drug release from MSNs. This review presents an overview of the recent progress in the production of pH-responsive MSNs based on the pH gradient between normal tissues and the tumor microenvironment. Four main categories of gatekeepers can respond to acidic conditions. These categories will be described in detail.
文摘Electrospinning is a very simple and versatile process by which polymer nanofibers with di-ameters ranging from a few nanometers to sev-eral micrometers can be produced using an electrostatically driven jet of polymer solution or polymer melt. Significant progress has been made in this process throughout the past few years and electrospinning has advanced its ap-plications in many fields, including pharmaceu-tics. Electrospun nanofibers show great prom-ise for developing many types of novel drug delivery systems (DDS) due to their special characteristics and the simple but useful and effective top-down fabricating process. The current state of electrospun nanofiber-based DDS is focused on drug-loaded nanofiber preparation from pharmaceutical and biode-gradable polymers and different types of DDS. However, there are more opportunities to be exploited from the electrospinning process and the corresponding drug-loaded nanofibers for drug delivery. Additionally, some other related challenges and the possible resolutions are outlined in this review.
