Biomimetic synthesis and evaluation of histidine-derivative templated chiral mesoporous silica for improved oral delivery of the poorly water-soluble drug, nimodipine
Research output: Contribution to journal › Journal article › Research › peer-review
Standard
Biomimetic synthesis and evaluation of histidine-derivative templated chiral mesoporous silica for improved oral delivery of the poorly water-soluble drug, nimodipine. / Li, Heran; Li, Haiting; Wei, Chen; Ke, Jia; Li, Jing; Xu, Lu; Liu, Hongzhuo; YangYang; Li, Sanming; Yang, Mingshi.
In: European Journal of Pharmaceutical Sciences, Vol. 117, 2018, p. 321-330.Research output: Contribution to journal › Journal article › Research › peer-review
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Biomimetic synthesis and evaluation of histidine-derivative templated chiral mesoporous silica for improved oral delivery of the poorly water-soluble drug, nimodipine
AU - Li, Heran
AU - Li, Haiting
AU - Wei, Chen
AU - Ke, Jia
AU - Li, Jing
AU - Xu, Lu
AU - Liu, Hongzhuo
AU - YangYang, null
AU - Li, Sanming
AU - Yang, Mingshi
PY - 2018
Y1 - 2018
N2 - In this study, spherical shaped chiral mesoporous silica nanoparticles (CMS) was biomimetic synthesized using histidine derivatives (C 16 -L-histidine) as template via the sol–gel reaction and employed as poorly water-soluble drug nimodipine (NMP) carrier. Characteristics of CMS and its application as drug carrier were intensively investigated and compared with MCM41. Then NMP was respectively loaded into CMS and MCM41 with the drug: carrier weight ratio of 2:1. Structural features of NMP before and after drug loading were systemically characterized. The results demonstrated that hydrogen bonds were formed between NMP and carriers during the drug loading process. After drug loading, crystalline state of NMP effectively converted into modification L and amorphous state, and the first form turned out to be easily removed by washing. On the other hand, drug dissolution rate was significantly improved after drug loading, and the best result came from NMP-C3 sample. It was able to release 17.83% of drug within 60 min, which was 6.8-fold higher than the release amount of pure NMP. Undoubtedly, NMP-C3 presented the highest relative bioavailability (386.22%), and the best therapeutic effect. Meanwhile, CMS improved the brain distribution of NMP in vivo.
AB - In this study, spherical shaped chiral mesoporous silica nanoparticles (CMS) was biomimetic synthesized using histidine derivatives (C 16 -L-histidine) as template via the sol–gel reaction and employed as poorly water-soluble drug nimodipine (NMP) carrier. Characteristics of CMS and its application as drug carrier were intensively investigated and compared with MCM41. Then NMP was respectively loaded into CMS and MCM41 with the drug: carrier weight ratio of 2:1. Structural features of NMP before and after drug loading were systemically characterized. The results demonstrated that hydrogen bonds were formed between NMP and carriers during the drug loading process. After drug loading, crystalline state of NMP effectively converted into modification L and amorphous state, and the first form turned out to be easily removed by washing. On the other hand, drug dissolution rate was significantly improved after drug loading, and the best result came from NMP-C3 sample. It was able to release 17.83% of drug within 60 min, which was 6.8-fold higher than the release amount of pure NMP. Undoubtedly, NMP-C3 presented the highest relative bioavailability (386.22%), and the best therapeutic effect. Meanwhile, CMS improved the brain distribution of NMP in vivo.
KW - Biomimetic synthesis
KW - Brain distribution
KW - Chiral mesoporous silica
KW - Nimodipine
KW - Oral bioavailability
U2 - 10.1016/j.ejps.2018.03.013
DO - 10.1016/j.ejps.2018.03.013
M3 - Journal article
C2 - 29530545
AN - SCOPUS:85043467317
VL - 117
SP - 321
EP - 330
JO - Norvegica Pharmaceutica Acta
JF - Norvegica Pharmaceutica Acta
SN - 0928-0987
ER -
ID: 220847100