We encapsulated vincristine into folic acid-conjugated PEGylated liposomes to improve the anti-tumor efficacy on multidrug resistant cancers.It was observed that the drug delivery system we constructed exhibited maxim...We encapsulated vincristine into folic acid-conjugated PEGylated liposomes to improve the anti-tumor efficacy on multidrug resistant cancers.It was observed that the drug delivery system we constructed exhibited maximum cytotoxicity on KBv200 cells(multidrug resistant variant)compared with any other formulations.The semi-quantitative analysis of region of interest revealed that there was a great increase in area under curve(AUC)of a near-infrared fluorescein in solid tumors due to folic acid-mediated accumulation.Folic acid-conjugated PEGylated liposomes showed a significant tumor growth inhibiting effect in vitro and in vivo.TUNEL assay revealed that folic acid-conjugated PEGylated liposomes could induce cell apoptosis much more greatly than others.This study demonstrated that it had potential application prospective for the treatment of multidrug resistant cancer.展开更多
In the original version of this article on p 122, two inappropriate images were placed in B and C of Fig. 1, which didn’t represent the group of FA-PEG-LS and PEG-LS/VCR. In the revised graphic provided below, the ap...In the original version of this article on p 122, two inappropriate images were placed in B and C of Fig. 1, which didn’t represent the group of FA-PEG-LS and PEG-LS/VCR. In the revised graphic provided below, the appropriate images are used.These corrections do not change the results and conclusions of this work.展开更多
The purpose of this study is to evaluate the in vivo retention capabilities of poloxamer-based in situ hydrogels for vaginal application with nonoxinol-9 as the model drug. Two in situ hydrogel formulations, which con...The purpose of this study is to evaluate the in vivo retention capabilities of poloxamer-based in situ hydrogels for vaginal application with nonoxinol-9 as the model drug. Two in situ hydrogel formulations, which contained 18% poloxamer 407 plus 1% poloxamer 188(GEL1, relative hydrophobic)or 6% poloxamer 188(GEL2, relative hydrophilic), were compared with respect to the rheological properties, in vitro hydrogel erosion and drug release. The vaginal retention capabilities of these hydrogel formulations were further determined in two small animal models, including drug quantitation of vaginal rinsing fluid in mice and isotope tracing with99 m Tc in rats. The two formulations exhibited similar phase transition temperatures ranging from 27 to 32 1C. Increasing the content of poloxamer 188 resulted in higher rheological moduli under body temperature, but slightly accelerated hydrogel erosion and drug release. When compared in vivo, GEL1 was eliminated significantly slower in rat vagina than GEL2,while the vaginal retention of these two hydrogel formulations behaved similarly in mice. In conclusion,increases in the hydrophilic content of formulations led to faster hydrogel erosion, drug release andintravaginal elimination. Rats appear to be a better animal model than mice to evaluate the in situ hydrogel for vaginal application.展开更多
基金This work was supported by National Science and Technology Major Project(2012ZX09304004)National Basic Research Program of China(973 Program,2010CB934000)+1 种基金National Natural Science Foundation of China(81072593,81102402)Specialized Research Fund for the Doctoral Program of Higher Education(20110071130011).
文摘We encapsulated vincristine into folic acid-conjugated PEGylated liposomes to improve the anti-tumor efficacy on multidrug resistant cancers.It was observed that the drug delivery system we constructed exhibited maximum cytotoxicity on KBv200 cells(multidrug resistant variant)compared with any other formulations.The semi-quantitative analysis of region of interest revealed that there was a great increase in area under curve(AUC)of a near-infrared fluorescein in solid tumors due to folic acid-mediated accumulation.Folic acid-conjugated PEGylated liposomes showed a significant tumor growth inhibiting effect in vitro and in vivo.TUNEL assay revealed that folic acid-conjugated PEGylated liposomes could induce cell apoptosis much more greatly than others.This study demonstrated that it had potential application prospective for the treatment of multidrug resistant cancer.
文摘In the original version of this article on p 122, two inappropriate images were placed in B and C of Fig. 1, which didn’t represent the group of FA-PEG-LS and PEG-LS/VCR. In the revised graphic provided below, the appropriate images are used.These corrections do not change the results and conclusions of this work.
基金supported by the National Key Technology R&D Program(2012BAI31B04)the Open Project Program of National Population+1 种基金Family Planning Key Laboratory of Contraceptives Drugs and Devices(2016KF08)the National Natural Science Foundation of China(81102385)
文摘The purpose of this study is to evaluate the in vivo retention capabilities of poloxamer-based in situ hydrogels for vaginal application with nonoxinol-9 as the model drug. Two in situ hydrogel formulations, which contained 18% poloxamer 407 plus 1% poloxamer 188(GEL1, relative hydrophobic)or 6% poloxamer 188(GEL2, relative hydrophilic), were compared with respect to the rheological properties, in vitro hydrogel erosion and drug release. The vaginal retention capabilities of these hydrogel formulations were further determined in two small animal models, including drug quantitation of vaginal rinsing fluid in mice and isotope tracing with99 m Tc in rats. The two formulations exhibited similar phase transition temperatures ranging from 27 to 32 1C. Increasing the content of poloxamer 188 resulted in higher rheological moduli under body temperature, but slightly accelerated hydrogel erosion and drug release. When compared in vivo, GEL1 was eliminated significantly slower in rat vagina than GEL2,while the vaginal retention of these two hydrogel formulations behaved similarly in mice. In conclusion,increases in the hydrophilic content of formulations led to faster hydrogel erosion, drug release andintravaginal elimination. Rats appear to be a better animal model than mice to evaluate the in situ hydrogel for vaginal application.