目的制备白头翁总皂苷结肠定位固体分散体。方法采用溶剂法制备白头翁总皂苷固体分散体,以体外累计释放度为评价指标,采用单因素方法筛选制备工艺及处方,并采用电子扫描显微镜(SEM)、红外光谱(IR)对制备的固体分散体进行分析。结果 SEM...目的制备白头翁总皂苷结肠定位固体分散体。方法采用溶剂法制备白头翁总皂苷固体分散体,以体外累计释放度为评价指标,采用单因素方法筛选制备工艺及处方,并采用电子扫描显微镜(SEM)、红外光谱(IR)对制备的固体分散体进行分析。结果 SEM和IR分析结果显示白头翁总皂苷和Eudragit S100形成了固体分散体。体外释放度结果显示载药量在20%时指标成分在p H 1.0溶液中2 h基本不释放,在p H 6.8溶液中4 h累积释放度小于16%,在p H 7.8溶液中2 h累积释放大于86%。结论所制备的固体分散体达到了结肠定位的效果。展开更多
Ulcerative colitis(UC)is a common progressive inflammatory disease whose incidence has increased rapidly in recent years,and can develop into colorectal cancer in severe cases.There are currently no adequate or effect...Ulcerative colitis(UC)is a common progressive inflammatory disease whose incidence has increased rapidly in recent years,and can develop into colorectal cancer in severe cases.There are currently no adequate or effective treatments for UC due to the fact that some patients have found suboptimal results after repeated administration,while others have experienced adverse effects.With the rapid development of nanotechnology,developing innovative colon-targeting platforms is essential to improving efficacy,reducing side effects,and improving patient compliance.In this review,we summarize the pathophysiological characteristics of UC and the most recent status of numerous nanodrug delivery systems based on different targeting mechanisms in treating UC.Oral,intravenous,and rectal drug delivery nanoparticles targeting the colon are discussed,which can provide ideas for the design of colon-targeting nanoparticles for the treatment of colon diseases,especially for the treatment of UC.Last but not least,we provide a glimpse into the future of colon-targeted delivery systems,as well as future advancements in the field.展开更多
Objective To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alop...Objective To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides （TASA） was prepared. Methods The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results The pellet core consisted of 40% TASA, 1：2 in ratio of Bletilla striata polysaccharide （BSP）, an enzyme-degradable material, to microcrystalline cellu{ose （MCC）, filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit $100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h, And the similarity factor f2 of sophoridine and matrine of release curve for investigated formulation was internal in （50-100） and 〉 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion The coated pellets achieve a certain colon-specific release and synchronous release.展开更多
A series of cross-linked gels of Poly（N-isopropylacrylamide） [P（NIPAAm）] and Poly（methacr-ylic acid）[P（MAA）] homopolymers and P（NIPAAm-co-MAA） random copolymers were synthesized based on NIPAAm and MAA using...A series of cross-linked gels of Poly（N-isopropylacrylamide） [P（NIPAAm）] and Poly（methacr-ylic acid）[P（MAA）] homopolymers and P（NIPAAm-co-MAA） random copolymers were synthesized based on NIPAAm and MAA using 4,4-Bis-（methacryloylamino） azobenzene （BMAAB） as a cross-linker. The swelling behavior of these hydrogels in different pH buffer solutions was studied. The influential factors of the gels including composition of NIPAAm and MAA, pH and temperature upon swelling behavior were investigated. The obtained gels not only hold pH and thermometrical sensitivity, but also take on enzymatic sensitivity due to the cross-linker could be degraded by enzymes of colon. Swelling equilibrium degree of copolymers was very low in acidic medium, which could avoid drug releasing due to biggish swelling of carder in stomach. Hydrogels would partly swell owing to higher pH value in small intestine. When arrived in colon, hydrogels completely swelled, meanwhile, azoenzymes located would degrade azo-bonds of polymeric network and then drug released in colon.展开更多
文摘目的制备白头翁总皂苷结肠定位固体分散体。方法采用溶剂法制备白头翁总皂苷固体分散体,以体外累计释放度为评价指标,采用单因素方法筛选制备工艺及处方,并采用电子扫描显微镜(SEM)、红外光谱(IR)对制备的固体分散体进行分析。结果 SEM和IR分析结果显示白头翁总皂苷和Eudragit S100形成了固体分散体。体外释放度结果显示载药量在20%时指标成分在p H 1.0溶液中2 h基本不释放,在p H 6.8溶液中4 h累积释放度小于16%,在p H 7.8溶液中2 h累积释放大于86%。结论所制备的固体分散体达到了结肠定位的效果。
基金financially supported by Beijing Nova Program(Nos.Z211100002121127 and 20220484219)Beijing Natural Science Foundation(No.L212059)+1 种基金Fundamental Research Funds for the Central Universities(No.3332021101)CAMS Innovation Fund for Medical Sciences(CIFMS,Nos.2021-I2M-1-026 and 2021-I2M-1-028).
文摘Ulcerative colitis(UC)is a common progressive inflammatory disease whose incidence has increased rapidly in recent years,and can develop into colorectal cancer in severe cases.There are currently no adequate or effective treatments for UC due to the fact that some patients have found suboptimal results after repeated administration,while others have experienced adverse effects.With the rapid development of nanotechnology,developing innovative colon-targeting platforms is essential to improving efficacy,reducing side effects,and improving patient compliance.In this review,we summarize the pathophysiological characteristics of UC and the most recent status of numerous nanodrug delivery systems based on different targeting mechanisms in treating UC.Oral,intravenous,and rectal drug delivery nanoparticles targeting the colon are discussed,which can provide ideas for the design of colon-targeting nanoparticles for the treatment of colon diseases,especially for the treatment of UC.Last but not least,we provide a glimpse into the future of colon-targeted delivery systems,as well as future advancements in the field.
基金Major science and technology projects of Guangdong province,China(2013A022100039)Science innovation projects of higher school(2012KJCX0060)+3 种基金Technology Bureau of ZhanjiangGuangdong province,China(2011C3108015)Guangdong province sail plan project of high level talents in 2014the National Natural Science Foundation of China(81473401)
文摘Objective To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides （TASA） was prepared. Methods The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results The pellet core consisted of 40% TASA, 1：2 in ratio of Bletilla striata polysaccharide （BSP）, an enzyme-degradable material, to microcrystalline cellu{ose （MCC）, filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit $100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h, And the similarity factor f2 of sophoridine and matrine of release curve for investigated formulation was internal in （50-100） and 〉 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion The coated pellets achieve a certain colon-specific release and synchronous release.
文摘A series of cross-linked gels of Poly（N-isopropylacrylamide） [P（NIPAAm）] and Poly（methacr-ylic acid）[P（MAA）] homopolymers and P（NIPAAm-co-MAA） random copolymers were synthesized based on NIPAAm and MAA using 4,4-Bis-（methacryloylamino） azobenzene （BMAAB） as a cross-linker. The swelling behavior of these hydrogels in different pH buffer solutions was studied. The influential factors of the gels including composition of NIPAAm and MAA, pH and temperature upon swelling behavior were investigated. The obtained gels not only hold pH and thermometrical sensitivity, but also take on enzymatic sensitivity due to the cross-linker could be degraded by enzymes of colon. Swelling equilibrium degree of copolymers was very low in acidic medium, which could avoid drug releasing due to biggish swelling of carder in stomach. Hydrogels would partly swell owing to higher pH value in small intestine. When arrived in colon, hydrogels completely swelled, meanwhile, azoenzymes located would degrade azo-bonds of polymeric network and then drug released in colon.
