文献类型：期刊文献

英文题名：Charge-Reversal APTES-Modified Mesoporous Silica Nanoparticles with High Drug Loading and Release Controllability

作者：Wang, Yifeng[1];Sun, Yi[1];Wang, Jine[1];Yang, Yang[1];Li, Yulin[1,2];Yuan, Yuan[1];Liu, Changsheng[1]

机构：[1]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Key Lab Ultrafine Mat, Minist Educ, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Shanghai Collaborat Innovat Ctr Biomfg, Shanghai 200237, Peoples R China

年份：2016

卷号：8

期号：27

起止页码：17166

外文期刊名：ACS APPLIED MATERIALS & INTERFACES

收录：;EI(收录号：20162902622249);WOS:【SCI-EXPANDED(收录号:WOS:000379794100018)】；

基金：We are grateful for the financial support from the Shanghai Municipal Natural Science Foundation (15ZR1408500). The Key Program of the National Natural Science Foundation of China (31330028) and 111 Project (Grant B14018) are also acknowledged for their financial support.

语种：英文

外文关键词：mesoporous silica nanocarriers; charge reversal; doxorubicin; drug delivery; pH responsive

摘要：In this study, we demonstrate a facile strategy (DL-SF) for developing MSN-based nanosystems through drug loading (DL, using doxorubicin as a model drug) followed by surface functionalization (SF) of mesoporous silica nanoparticles (MSNs) via aqueous (3-aminopropyl)triethoxysilane (APTES) silylation. For comparison, a reverse functionalization process (i.e., SF DL) was also studied. The pre-DL process allows for an efficient encapsulation (encapsulation efficiency of similar to 75%) of an anticancer drug [doxorubicin (DOX)] inside MSNs, and post-SF allows in situ formation of an APTES outer layer to restrict DOX leakage under physiological conditions. This method makes it possible to tune the DOX release rate by increasing the APTES decoration density through variation of the APTES concentration. However, the SF-DL approach results in a rapid decrease in drug loading capacity with an increase in APTES concentration because of the formation of the APTES outer layer hampers the inner permeability of the DOX drug, resulting in a burst release similar to that of undecorated MSNs. The resulting DOX-loaded DL-SF MSNs present a slightly negatively charged surface under physiological conditions and become positively charged in and extracellular microenvironment of solid tumor due to the protonation effect under acidic conditions. These merits aid their maintenance of long-term stability in blood circulation, high cellular uptake by a kind of skin carcinoma cells, and an enhanced intracellular drug release behavior, showing their potential in the delivery of many drugs beyond anticancer chemotherapeutics.