scholarly journals Chitosan-capped enzyme-responsive hollow mesoporous silica nanoplatforms for colon-specific drug delivery

2020 ◽  
Author(s):  
Defu Cai ◽  
Cuiyan Han ◽  
Chang Liu ◽  
Xiaoxing Ma ◽  
Jiayi Qian ◽  
...  

Abstract An enzyme-responsive colon-specific delivery system was developed based on hollow mesoporous silica spheres (HMSS) to which biodegradable chitosan (CS) was attached via cleavable azo bonds (HMSS-N=N-CS). Doxorubicin (DOX) was encapsulated in a noncrystalline state in the hollow cavity and mesopores of HMSS with the high loading amount of 35.2%. In vitro drug release proved that HMSS-N=N-CS/DOX performed enzyme-responsive drug release. The grafted CS could increase the biocompatibility and stability, and reduce the protein adsorption on HMSS. Gastrointestinal mucosa irritation and cell cytotoxicity results indicated the good biocompatibility of HMSS and HMSS-N=N-CS. Cellular uptake results indicated that the uptake of DOX was obviously increased after HMSS-N=N-CS/DOX was preincubated with a colonic enzyme mixture. HMSS-N=N-CS/DOX incubated with colon enzymes showed increased cytotoxicity, and its IC 50 value was three times lower than that of HMSS-N=N-CS/DOX group without colon enzymes. The present work lays the foundation for subsequent research on mesoporous carriers for oral colon-specific drug delivery.

2020 ◽  
Author(s):  
Defu Cai ◽  
Cuiyan Han ◽  
Chang Liu ◽  
Xiaoxing Ma ◽  
Jiayi Qian ◽  
...  

Abstract An enzyme-responsive colon-specific delivery system was developed based on hollow mesoporous silica spheres (HMSS) to which biodegradable chitosan (CS) was attached via cleavable azo bonds (HMSS-N=N-CS). Doxorubicin (DOX) was encapsulated in a noncrystalline state in the hollow cavity and mesopores of HMSS with the high loading amount of 35.2%. In vitro drug release proved that HMSS-N=N-CS/DOX performed enzyme-responsive drug release. The grafted CS could increase the biocompatibility and stability, and reduce the protein adsorption on HMSS. Gastrointestinal mucosa irritation and cell cytotoxicity results indicated the good biocompatibility of HMSS and HMSS-N=N-CS. Cellular uptake results indicated that the uptake of DOX was obviously increased after HMSS-N=N-CS/DOX was preincubated with a colonic enzyme mixture. HMSS-N=N-CS/DOX incubated with colon enzymes showed increased cytotoxicity, and its IC50 value was three times lower than that of HMSS-N=N-CS/DOX group without colon enzymes. The present work lays the foundation for subsequent research on mesoporous carriers for oral colon-specific drug delivery.


2020 ◽  
Author(s):  
Defu Cai ◽  
Cuiyan Han ◽  
Chang Liu ◽  
Xiaoxing Ma ◽  
Jiayi Qian ◽  
...  

Abstract In summary, an enzyme-responsive colon specific drug delivery system was developed based on hollow mesoporous silica sphere (HMSS), in which the biodegradable chitosan (CS) was gated on the openings of HMSS through cleavable azo bonds (HMSS-N=N-CS). Doxorubicin (DOX) was encapsulated into the hollow cavity and mesopores of HMSS, and HMSS-N=N-CS/DOX showed a high loading amount of 35.2%. X-ray diffraction (XRD) experiment proved that the DOX loaded in the HMSS-N=N-CS was in a non–crystalline state. In vitro drug release experiments proved that HMSS-N=N-CS/DOX showed an enzyme-responsive drug release property. The grafted CS could increase the biocompatibility and stability of HMSS, and reduce the protein adsorption on the surface of HMSS. The gastrointestinal mucosa irritation and cell cytotoxicity results indicated the good biocompatibility of HMSS and HMSS-N=N-CS. The confocal laser scanning microscope (CLSM) and flow cytometry technique (FCM) results indicated that the cellular uptake of DOX was obviously increased after the HMSS-N=N-CS/DOX was preincubated with colonic enzyme mixture. Cell viability result indicated that HMSS-N=N-CS/DOX incubated with colon enzyme showed an increased cytotoxicity and the IC50 value was three time less than that of HMSS-N=N-CS/DOX group. The present work will lay the foundation for subsequent research on mesoporous carriers for oral colon-specific drug delivery.


2019 ◽  
Vol 9 (2) ◽  
pp. 316-320
Author(s):  
P Soni ◽  
K Soni ◽  
GP Choudhary

The aim of the study was to prepare site specific drug delivery of flurbiprofen using polysaccharides by the formation of glycosidic linkage which is hydrolysed by the microflora present in colon. This approach prevents drug release in the upper gastrointestinal environment. Due to the minimal degradation of conjugates in upper Git, the in vitro drug release in SGF, SIF and SCF was found upto 4.26±0.03%, 12.41±0.08% and 92.72±3.33% respectively. Keywords: Colon specific drug delivery, Conjugates, Flurbiprofen, Microbial system.


2009 ◽  
Vol 007 (1) ◽  
pp. 8-14
Author(s):  
Junying LAI ◽  
Wenjing LI ◽  
Hongjun WANG ◽  
Kehua TU ◽  
Liqun WANG

2017 ◽  
Vol 150 ◽  
pp. 352-361 ◽  
Author(s):  
Balmiki Kumar ◽  
Senthilguru Kulanthaivel ◽  
Animesh Mondal ◽  
Smruti Mishra ◽  
Biplab Banerjee ◽  
...  

2011 ◽  
Vol 21 (14) ◽  
pp. 5299 ◽  
Author(s):  
Tingting Wang ◽  
Fang Chai ◽  
Qin Fu ◽  
Lingyu Zhang ◽  
Haiyan Liu ◽  
...  

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