期刊
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
卷 78, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jddst.2022.103977
关键词
Mesoporous silica nanoparticle; Lidocaine derivatives; pH-responsive release; Local anesthesia
资金
- Japan Society for the Promotion of Science
- [21K18064]
In this study, QX-OH was loaded onto carboxyl-functionalized mesoporous silica nanoparticles (MSN) using an ester-based drug loading method to achieve pH-responsive release. The introduction of an ester bond efficiently provided a local anesthetic via pH-responsive release.
The quaternary lidocaine derivative QX-OH is a promising candidate for efficient local anesthesia, but sufficient membrane permeability and pharmacokinetic controllability are still required for clinical usage. In this study, we demonstrated ester-based pH-cleavable loading of QX-OH onto carboxyl-functionalized mesoporous silica nanoparticles (MSN) to control pH-responsive release. MSN was prepared by a sol-gel method, and the surface was functionalized with an amine group and then with a carboxyl group. The properties of the MSNs were characterized by scanning electron microscopy, Fourier-transformed infrared spectroscopy (FT-IR), thermogra-vimetry-differential thermal analysis, Brunauer-Emmett-Teller method, and zeta potential measurement. A sufficient amount of QX-OH, 24.5 wt%, was loaded into the carboxyl-functionalized MSN (MSN_QX-OH) by ester binding. The FT-IR spectrum of MSN_QX-OH showed that the peak of the carboxyl group shifted to a higher wavenumber, that is, QX-OH was bound to the surface via ester bond. MSN_QX-OH released 26% QX-OH at physiological pH for 8 h. Furthermore, when the pH of the solvent was lowered to 5.5, mimicking the endosomal condition, acid hydrolysis of the ester bond released 66% QX-OH within 1 h. In conclusion, the introduction of an ester bond between QX-OH and MSN would efficiently provide a local anesthetic via pH-responsive release.
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