Preparation and in vitro Evaluation of Cationic Mesoporous Silica Nanoparticles Loaded with Puerarin for Oral Administration

ZHANG Kuankuan1, CHEN Danfei2, ZHANG Rongrong2, XIAO Shigeng3, XU Junjun3?

主办：上海医药工业研究院
　　　中国药学会
　　　中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
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Chinese Journal of Pharmaceuticals
Chinese Journal of Pharmaceuticals ›› 2016, Vol. 47 ›› Issue (05) : 558. DOI: 10.16522/j.cnki.cjph.2016.05.009

Preparation and in vitro Evaluation of Cationic Mesoporous Silica Nanoparticles Loaded with Puerarin for Oral Administration

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Abstract

The cationic mesoporous silica nanoparticles (CMSN) were synthesized by Stober method. The average particle size and z potential of the prepared CMSN with spherical appearance and obvious mesoporous structure were (98.4±2.8)nm and (13.2±1.8)mV. There was no obvious cytotoxicity in vitro of CMSN in the range of 0—20 μg/ml against Caco-2 cells. By using saturated solution adsorbing method, puerarin (1) was highly encapsulated into CMSN. After repeated adsorption for 7 times, the drug loading of CMSN reached a full load of about 18％. In pH 7.4 phosphate buffer containing 2％ sodium dodecylsulfate, the release data of 1 from the 1-CMSN was well-fitted to the Weibull equation with the correlation coefficient of 0.923 6. In Caco-2 cell monolayers, the apparent permeability coefficients, Papp(A→B) and Papp(B→A), were (23.89±1.22)×10-6 cm/s and (17.03±1.21)×10-6 cm/s. The efflux ratio (ER) of 1-CMSN was 1.403, which was significantly higher than that of the bulk drug (P<0.05).

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cationic mesoporous silica nanoparticle / puerarin / oral administration / in vitro release / cytotoxicity / transmembrane transport

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ZHANG Kuankuan1, CHEN Danfei2, ZHANG Rongrong2, XIAO Shigeng3, XU Junjun3?. Preparation and in vitro Evaluation of Cationic Mesoporous Silica Nanoparticles Loaded with Puerarin for Oral Administration. Chinese Journal of Pharmaceuticals. 2016, 47(05): 558 https://doi.org/10.16522/j.cnki.cjph.2016.05.009

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