Colon-targeted oral delivery is crucial for the treatment of colon-related diseases, as this delivery strategy enables precise drug administration to the diseased site, enhances drug bioavailability, and improves pati...Colon-targeted oral delivery is crucial for the treatment of colon-related diseases, as this delivery strategy enables precise drug administration to the diseased site, enhances drug bioavailability, and improves patient com- pliance. In particular, nanoparticle-based oral formulations shield drugs from the harsh gastrointestinal environment, and selectively increase drug colon cells, thus elevating concentration inside diseased therapeutic efficacy while reducing systemic toxicity. In this review, we elaborate recent progress in this area, with emphasis on the patho- physiological characteristics of colon site and design strategies to take advantage of these characteristics for colon targeting.展开更多
Anti-inflammatory drugs targeting inflammatory bowel disease(IBD)have attracted considerable attention but still face low therapeutic outcomes and frequent side effects.Astaxanthin(ATX),a natural ketone,possesses pote...Anti-inflammatory drugs targeting inflammatory bowel disease(IBD)have attracted considerable attention but still face low therapeutic outcomes and frequent side effects.Astaxanthin(ATX),a natural ketone,possesses potent antioxidant and anti-inflammatory properties.However,it faces problems such as poor water solubility,photothermal instability,and low bioavailability.Here,we employed a supramolecular encapsulation strategy to create a nanoscale oral delivery system for ATX(referred to as FC-ATX NPs)by coupling fucoidan(FUC)with chitosan oligosaccharides(COS).The obtained FC-ATX NPs exhibited a particular“bean pod”structure with uniform size,good encapsulation efficiency,excellent physical and chemical stability,pH-triggered intestinal targeted slow-release properties,and potent antioxidant capacity.In vitro cell culture experiments showed that FC-ATX NPs promoted cellular uptake and scavenged excessive intracellular reactive oxygen species(ROS).In mouse models of colitis,FC-ATX NPs enhanced the drug absorption of intestinal epithelial cells and effectively accumulated at the site of inflammation.This work provides an efficient approach to enhance the bioavailability of ATX and has excellent application potential as an oral targeted delivery system for colitis therapy.展开更多
Objective:To develop a pectin and chitosan-based colon-targeted mi-crocapsule for paclitaxel(PTX)and evaluate its stability and drug release characteristics in an artificial simulated gastrointestinal environment.Meth...Objective:To develop a pectin and chitosan-based colon-targeted mi-crocapsule for paclitaxel(PTX)and evaluate its stability and drug release characteristics in an artificial simulated gastrointestinal environment.Methods:Pectin/chitosan dou-ble-polymer microcapsules(PCPM)were prepared using an ionic gelation method com-bined with spray-drying technology,with PTX as the model drug.The morphology and mechanical strength of the microcapsules were observed using a stereomicroscope,and the encapsulation efficiency and drug loading were determined.The drug release behav-ior and tolerance of the microcapsules were analyzed by simulating artificial gastric juice(pH1.2)and intestinal fluid(pH6.8)environments.Results:The average particle sizes of PPS(Note:Likely a typo in the original text;presumably a control sample such as pure pectin microcapsules)and PCPM microcapsules were(38±4)μm and(50±5)μm,respec-tively.The encapsulation efficiencies were 95.7%±1.0%and 86.2%±7.6%,and the drug loadings were 47.8%±0.5%and 43.1%±3.8%,respectively.The protection rate of PTX in PCPM microcapsules was significantly higher than that of the PTX standard in artifi-cial gastrointestinal fluid,reaching 67.0%±0.8%at 2 h.The total release rate in colonic fluid reached 91.0%±0.8%within 8 h,indicating that PCPM microcapsules achieve colon-specific drug release through enzymatic hydrolysis in the gastrointestinal tract.Conclusion:PCPM has good gastrointestinal tolerance and colon-targeted drug release performance,which is a new strategy for colon-targeted delivery of oral formulations of PTX.展开更多
Oral colonic nano-drug delivery system has attracted growing attention in treating colon cancer for their excellent characteristics.However,the unique and complex structure of the gastrointestinal tract is still an ob...Oral colonic nano-drug delivery system has attracted growing attention in treating colon cancer for their excellent characteristics.However,the unique and complex structure of the gastrointestinal tract is still an obstacle to the safe delivery of drugs targeting sites in colon tumors.Here,we designed magnetically driven dual-targeted oral colonic nanoparticles loaded with chlorogenic acid using pectin and oleic acid-modified iron oxide(Fe3O4@OA).Specific degradation of pectin by pectinase produced by colonic flora and magnetic fields applied to the colon confers specific targeting of nanoparticles to the colon.In order to overcome the challenge of preparing magnetically driven nanoparticles with small and homogeneous particle sizes by a single conventional method,we developed the combined ultrasound-emulsification technique.The average particle size of the prepared nanoparticles was 81.04±1.02 nm,which showed good drug release in the simulated colonic environment.In vitro anticancer studies,the drug-loaded nanoparticles possess an obvious toxicity and apoptosis-inducing ability against cancer cells.Meanwhile,the hemolysis results demonstrated the safety of the nanoplatform(PET/CGA/Fe_(3)O_(4)@OA).This work holds broad prospects as a new treatment modality for colon cancer.展开更多
Intervening in the microbial environment holds promise for enhancing antitumor efficacy by reshaping the tumor microenvironment,yet few strategies have been reported.In a study led by Zou and coworkers,oral hydrogels ...Intervening in the microbial environment holds promise for enhancing antitumor efficacy by reshaping the tumor microenvironment,yet few strategies have been reported.In a study led by Zou and coworkers,oral hydrogels are introduced to regulate the microbiota balance in the intestines and tumors,triggering an antitumor immune response.This work presents a microbiota-targeted drug delivery system that demonstrates notable efficacy in colon targeting and colon retention for the treatment of colorectal cancer.This represents a significant clinical advancement in treating colorectal cancer,which is particularly vulnerable to microbial infitration.展开更多
基金supported by the National Natural Science Foundation of China(81471779)the National Thousand Young Talents Programthe Program for Professor of Special Appointment(Eastern Scholar)at Shanghai Institutions of Higher Learning
文摘Colon-targeted oral delivery is crucial for the treatment of colon-related diseases, as this delivery strategy enables precise drug administration to the diseased site, enhances drug bioavailability, and improves patient com- pliance. In particular, nanoparticle-based oral formulations shield drugs from the harsh gastrointestinal environment, and selectively increase drug colon cells, thus elevating concentration inside diseased therapeutic efficacy while reducing systemic toxicity. In this review, we elaborate recent progress in this area, with emphasis on the patho- physiological characteristics of colon site and design strategies to take advantage of these characteristics for colon targeting.
基金financially supported by the Chongqing Graduate Program of Research and Innovation(No.CYS22207)the National Natural Science Foundation of China(No.51703187)Chongqing Talents of Exceptional Young Talents Project,China(Nos.CQYC202005029 and cstc2021ycjh-bgzxm0061)。
文摘Anti-inflammatory drugs targeting inflammatory bowel disease(IBD)have attracted considerable attention but still face low therapeutic outcomes and frequent side effects.Astaxanthin(ATX),a natural ketone,possesses potent antioxidant and anti-inflammatory properties.However,it faces problems such as poor water solubility,photothermal instability,and low bioavailability.Here,we employed a supramolecular encapsulation strategy to create a nanoscale oral delivery system for ATX(referred to as FC-ATX NPs)by coupling fucoidan(FUC)with chitosan oligosaccharides(COS).The obtained FC-ATX NPs exhibited a particular“bean pod”structure with uniform size,good encapsulation efficiency,excellent physical and chemical stability,pH-triggered intestinal targeted slow-release properties,and potent antioxidant capacity.In vitro cell culture experiments showed that FC-ATX NPs promoted cellular uptake and scavenged excessive intracellular reactive oxygen species(ROS).In mouse models of colitis,FC-ATX NPs enhanced the drug absorption of intestinal epithelial cells and effectively accumulated at the site of inflammation.This work provides an efficient approach to enhance the bioavailability of ATX and has excellent application potential as an oral targeted delivery system for colitis therapy.
文摘Objective:To develop a pectin and chitosan-based colon-targeted mi-crocapsule for paclitaxel(PTX)and evaluate its stability and drug release characteristics in an artificial simulated gastrointestinal environment.Methods:Pectin/chitosan dou-ble-polymer microcapsules(PCPM)were prepared using an ionic gelation method com-bined with spray-drying technology,with PTX as the model drug.The morphology and mechanical strength of the microcapsules were observed using a stereomicroscope,and the encapsulation efficiency and drug loading were determined.The drug release behav-ior and tolerance of the microcapsules were analyzed by simulating artificial gastric juice(pH1.2)and intestinal fluid(pH6.8)environments.Results:The average particle sizes of PPS(Note:Likely a typo in the original text;presumably a control sample such as pure pectin microcapsules)and PCPM microcapsules were(38±4)μm and(50±5)μm,respec-tively.The encapsulation efficiencies were 95.7%±1.0%and 86.2%±7.6%,and the drug loadings were 47.8%±0.5%and 43.1%±3.8%,respectively.The protection rate of PTX in PCPM microcapsules was significantly higher than that of the PTX standard in artifi-cial gastrointestinal fluid,reaching 67.0%±0.8%at 2 h.The total release rate in colonic fluid reached 91.0%±0.8%within 8 h,indicating that PCPM microcapsules achieve colon-specific drug release through enzymatic hydrolysis in the gastrointestinal tract.Conclusion:PCPM has good gastrointestinal tolerance and colon-targeted drug release performance,which is a new strategy for colon-targeted delivery of oral formulations of PTX.
基金supported by the National Key R&D Program of China(grant No.2019YFB1309703).
文摘Oral colonic nano-drug delivery system has attracted growing attention in treating colon cancer for their excellent characteristics.However,the unique and complex structure of the gastrointestinal tract is still an obstacle to the safe delivery of drugs targeting sites in colon tumors.Here,we designed magnetically driven dual-targeted oral colonic nanoparticles loaded with chlorogenic acid using pectin and oleic acid-modified iron oxide(Fe3O4@OA).Specific degradation of pectin by pectinase produced by colonic flora and magnetic fields applied to the colon confers specific targeting of nanoparticles to the colon.In order to overcome the challenge of preparing magnetically driven nanoparticles with small and homogeneous particle sizes by a single conventional method,we developed the combined ultrasound-emulsification technique.The average particle size of the prepared nanoparticles was 81.04±1.02 nm,which showed good drug release in the simulated colonic environment.In vitro anticancer studies,the drug-loaded nanoparticles possess an obvious toxicity and apoptosis-inducing ability against cancer cells.Meanwhile,the hemolysis results demonstrated the safety of the nanoplatform(PET/CGA/Fe_(3)O_(4)@OA).This work holds broad prospects as a new treatment modality for colon cancer.
基金support from School of Chemical Science and Engineering,Tongji University.
文摘Intervening in the microbial environment holds promise for enhancing antitumor efficacy by reshaping the tumor microenvironment,yet few strategies have been reported.In a study led by Zou and coworkers,oral hydrogels are introduced to regulate the microbiota balance in the intestines and tumors,triggering an antitumor immune response.This work presents a microbiota-targeted drug delivery system that demonstrates notable efficacy in colon targeting and colon retention for the treatment of colorectal cancer.This represents a significant clinical advancement in treating colorectal cancer,which is particularly vulnerable to microbial infitration.
