Abstract
Large-pore coralline mesoporous silica microparticles (CMS) were synthesized using the triblock polymer PEG-b-PEO-b-PEG and a hydrothermal method. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed the coralline morphology of the fabricated materials. The Brunauer–Emmett–Teller (BET) method and the Barrett–Joyner–Halenda (BJH) model confirmed the existence of large pores (20 nm) and of a tremendous specific surface area (663.865 m2·g−1) and pore volume (0.365 cm3·g−1). A novel pH-sensitive multiamine-chain carboxyl-functionalized coralline mesoporous silica material (CMS–(NH)3–COOH) was obtained via a facile “grafting-to” approach. X-ray photoelectron spectroscopy (XPS) and Fourier-transform infrared spectroscopy (FT-IR) validated the effective interfacial functionalization of CMS with carboxyl and multiamine chains. The encapsulation and release behavior of the dual drug (gefitinib (GB) and doxorubicin (DOX)) was also investigated. It was found that CMS–(NH)3–COOH allows rapid encapsulation with a high loading capacity of 47.36% for GB and 26.74% for DOX. Furthermore, the release profiles reveal that CMS–(NH)3–COOH can preferably control the release of DOX and GB. The accumulative release rates of DOX and GB were 32.03% and 13.66%, respectively, at a low pH (pH 5.0), while they reduced to 8.45% and 4.83% at pH 7.4. Moreover, all of the modified silica nanoparticles exhibited a high biocompatibility with a low cytotoxicity. In particular, the cytotoxicity of both of these two drugs was remarkably reduced after being encapsulated. CMS–(NH)3–COOH@GB@DOX showed tremendously synergistic effects of the dual drug in the antiproliferation and apoptosis of A549 human cancer cells in vitro.
Highlights
Cancer is the leading cause of death in the world
Two drugs were conjugated to coralline mesoporous silica microparticles (CMS)–(NH)3 –COOH and showed an enhanced uptake in A549 human cancer cells compared with the microparticles obtained with only gefitinib
After cooling to room temperature, the carboxyl-functionalized materials were obtained by filtering, were washed three times with ethanol and deionized water, were dried at 35 ◦ C for 24 h, and were named CMS–(NH)3 –COOH
Summary
Cancer is the leading cause of death in the world. In 2016, there were 17.2 million cancer cases worldwide and 8.9 million deaths [1]. Based on previous methods [29], we designed a facile synthetic route to produce carboxyl-functionalized large-pore mesoporous silica materials that are able to effectively encapsulate and release gefitinib and doxorubicin. Transmission electron microscopy (TEM) images of the obtained materials (large-pore coralline mesoporous silica microparticles; CMS) show that the material possesses an unambiguous open-framework structure This structure favors efficient mass transfer, as the high-density entrances enable rapid and efficient drug encapsulation. 12, 766 anhydride with the amino to obtain carboxylic-functionalized materials 3with of 19 multiamine chains (CMS–(NH)3–COOH) (see Scheme 1) We applied this novel pH-sensitive multiamine-chain carboxyl-functionalized coralline mesoporous silica carrier for A549 human cancer cells in vitro. Two drugs were conjugated to CMS–(NH)3 –COOH and showed an enhanced uptake in A549 human cancer cells compared with the microparticles obtained with only gefitinib. CMS–(NH)3 –COOH could be a potential drug carrier for active therapeutic aspects in cancer therapy
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