Inflammatory bowel diseases(IBD)significantly contribute to high mortality globally and negatively affect patients’qualifications of life.The gastrointestinal tract has unique anatomical characteristics and physiolog...Inflammatory bowel diseases(IBD)significantly contribute to high mortality globally and negatively affect patients’qualifications of life.The gastrointestinal tract has unique anatomical characteristics and physiological environment limitations.Moreover,certain natural or synthetic anti-inflammatory drugs are associated with poor targeting,low drug accumulation at the lesion site,and other side effects,hindering them from exerting their therapeutic effects.Colon-targeted drug delivery systems represent attractive alternatives as novel carriers for IBD treatment.This review mainly discusses the treatment status of IBD,obstacles to drug delivery,design strategies of colon-targeted delivery systems,and perspectives on the existing complementary therapies.Moreover,based on recent reports,we summarized the therapeutic mechanism of colon-targeted drug delivery.Finally,we addressed the challenges and future directions to facilitate the exploitation of advanced nanomedicine for IBD therapy.展开更多
Baicalin(BA)is a flavonoid extracted from the dried root of Scutellaria baicalensis Georgi with excellent antioxidant and anti-inflammatory biological activities.In this study,Eudragit S100 was used as the colonic tar...Baicalin(BA)is a flavonoid extracted from the dried root of Scutellaria baicalensis Georgi with excellent antioxidant and anti-inflammatory biological activities.In this study,Eudragit S100 was used as the colonic target material to prepare BA colonic targeting granules(EBCGs)based on plasticizer dry powder coating technology to improve the targeting transportation performance of BA.In vitro studies showed that EBCGs with pH-sensitive properties were successfully prepared by plasticizer dry powder coating,and in vivo animal imaging studies showed that EBCGs could deliver BA to the colon and inhibit the release of BA in the upper gastrointestinal tract(GIT).In vivo studies showed that EBCGs had good therapeutic effects in colitis,which reduced expression levels of tumor necrosis factor alpha(TNF-α)and interleukin-1β(IL-1β)and increased superoxide dismutase(SOD)activities in the colonic tissues of rats with colitis.In conclusion,Eudragit S100 could be used for the preparation of multi-unit oral colon-targeted formulations by plasticizer dry powder coating technology,and our prepared EBCGs had good colon-targeting properties,which could improve the therapeutic effect and provide a potential application for ulcerative colitis(UC).展开更多
Both electrospinning apparatus and their commercial products are extending their applications in a wide variety of fields.However,very limited reports can be found about how to implement an energy-saving process and i...Both electrospinning apparatus and their commercial products are extending their applications in a wide variety of fields.However,very limited reports can be found about how to implement an energy-saving process and in turn to reduce the production cost.In this paper,a brand-new type of coaxial spinneret with a solid core and its electrospinning methods are developed.A novel sort of medicated Eudragit/lipid hybrid nanofibers are generated for providing a colon-targeted sustained release of aspirin.A series of characterizations demonstrates that the as-prepared hybrid nanofibers have a fine linear morphology with the aspirin/lipid separated from the matrix Eudragit to form many tiny islands.In vitro dissolution tests exhibit that the hybrid nanofibers are able to effectively prevent the release of aspirin under an acid condition(8.7%±3.4%for the first two hours),whereas prolong the drug release time period under a neutral condition(99.7±4.2%at the seventh hour).The energy-saving mechanism is discussed in detail.The prepared aspirin-loaded hybrid nanofibers can be further transferred into an oral dosage form for potential application in countering COVID-19 in the future.展开更多
基金supported by CACMS Innovation Fund(CI2021B016,CI2021A04801)National Natural Science Foundation of China(82192913,82174073)+2 种基金Qihuang Scholar ProgramCACMS Foundation(ZZ13-035-10)China Postdoctoral Science Foundation(2023M733913).
文摘Inflammatory bowel diseases(IBD)significantly contribute to high mortality globally and negatively affect patients’qualifications of life.The gastrointestinal tract has unique anatomical characteristics and physiological environment limitations.Moreover,certain natural or synthetic anti-inflammatory drugs are associated with poor targeting,low drug accumulation at the lesion site,and other side effects,hindering them from exerting their therapeutic effects.Colon-targeted drug delivery systems represent attractive alternatives as novel carriers for IBD treatment.This review mainly discusses the treatment status of IBD,obstacles to drug delivery,design strategies of colon-targeted delivery systems,and perspectives on the existing complementary therapies.Moreover,based on recent reports,we summarized the therapeutic mechanism of colon-targeted drug delivery.Finally,we addressed the challenges and future directions to facilitate the exploitation of advanced nanomedicine for IBD therapy.
基金supported by Outstanding Youth Foundation of Jiangxi Province(grant No.20224ACB216019)Natural Science Foundation of Jiangxi Province(grant Nos.20202BABL206151 and 20202BABL216026)+2 种基金Doctoral startup fund of Jiangxi Science and Technology Normal University(grant No.2019BSQD015)Department Education Science and Technology Research Project of Jiangxi(grant No.GJ201134)the Open Project of Jiangxi Provincial Key Laboratory of Drug Design and Evaluation(grant No.JKD-KF-2104).
文摘Baicalin(BA)is a flavonoid extracted from the dried root of Scutellaria baicalensis Georgi with excellent antioxidant and anti-inflammatory biological activities.In this study,Eudragit S100 was used as the colonic target material to prepare BA colonic targeting granules(EBCGs)based on plasticizer dry powder coating technology to improve the targeting transportation performance of BA.In vitro studies showed that EBCGs with pH-sensitive properties were successfully prepared by plasticizer dry powder coating,and in vivo animal imaging studies showed that EBCGs could deliver BA to the colon and inhibit the release of BA in the upper gastrointestinal tract(GIT).In vivo studies showed that EBCGs had good therapeutic effects in colitis,which reduced expression levels of tumor necrosis factor alpha(TNF-α)and interleukin-1β(IL-1β)and increased superoxide dismutase(SOD)activities in the colonic tissues of rats with colitis.In conclusion,Eudragit S100 could be used for the preparation of multi-unit oral colon-targeted formulations by plasticizer dry powder coating technology,and our prepared EBCGs had good colon-targeting properties,which could improve the therapeutic effect and provide a potential application for ulcerative colitis(UC).
基金This study was supported by the Natural Science Foundation of Shanghai,China(No.20ZR1439000)the USST college student innovation projects,China(Nos.SH2020227&XJ2020376-2020378).
文摘Both electrospinning apparatus and their commercial products are extending their applications in a wide variety of fields.However,very limited reports can be found about how to implement an energy-saving process and in turn to reduce the production cost.In this paper,a brand-new type of coaxial spinneret with a solid core and its electrospinning methods are developed.A novel sort of medicated Eudragit/lipid hybrid nanofibers are generated for providing a colon-targeted sustained release of aspirin.A series of characterizations demonstrates that the as-prepared hybrid nanofibers have a fine linear morphology with the aspirin/lipid separated from the matrix Eudragit to form many tiny islands.In vitro dissolution tests exhibit that the hybrid nanofibers are able to effectively prevent the release of aspirin under an acid condition(8.7%±3.4%for the first two hours),whereas prolong the drug release time period under a neutral condition(99.7±4.2%at the seventh hour).The energy-saving mechanism is discussed in detail.The prepared aspirin-loaded hybrid nanofibers can be further transferred into an oral dosage form for potential application in countering COVID-19 in the future.
