Abstract
Mesoporous silica nanomaterials show great potential to deliver chemotherapeutics for cancer treatment. The key challenges in the development of injectable mesoporous silica formulations are colloidal instability, hemolysis and inefficient drug loading and release. In this study, we evaluated the effect of PEGylation of mesoporous silica nanorods (MSNR) on hemolysis, colloidal stability, mitoxantrone (MTX) loading, in vitro MTX release, and cellular MTX delivery under hypoxic conditions. We found that PEGylation prevented dose-dependent hemolysis in the concentrations studied (0–10 mg/ml) and improved colloidal stability of MSNR. A negative effect of PEGylation on MTX loading was observed but PEGylated MSNR (PMSNR) demonstrated increased MTX release compared to non-PEGylated particles. Under hypoxic conditions, a decrease in the IC50 of MTX and MTX-loaded MSNR was observed when compared to normoxic conditions. These results showed that MSNR could deliver the chemotherapeutic agent, MTX to tumor cells and induce effective cell killing. However, the effect of PEGylation needs to be carefully studied due to the observed adverse effect on drug loading.
Highlights
The application of nanoparticles in anticancer drug delivery has attracted much attention in recent decades[1, 2]
We described the effect of surface functionalization of Mesoporous silica nanoparticles (MSN) on MTX loading and in vitro drug release, and demonstrated that thiol-functionalized MSN were suitable for MTX formulation, demonstrating a crystalline-to-amorphous transformation, high drug loading and pH-sensitive MTX release[25]
We report the application of PEGylated mesoporous silica nanorods (PMSNR) for delivery of anti-cancer drugs under hypoxic conditions
Summary
The application of nanoparticles in anticancer drug delivery has attracted much attention in recent decades[1, 2]. Various nanoparticle-based drug delivery systems have been developed to deliver chemotherapeutic agents to overcome drug resistance[3], to improve drug bioavailability[4], and to achieve selective cellular targeting while diminishing side effects of chemotherapy[5]. Inorganic materials such as mesoporous silicas offer a great potential as drug delivery systems due to their high drug loading, tunable pore size and pore volume, control over shape of the particles, easy surface modifications, and excellent biocompatibility. As hypoxia and subsequent acidosis are unifying factors for tumor cells to acquire resistance to chemotherapy and radiation, such targeted technologies may be helpful to sensitize tumor cells and decrease resistance[27, 28]
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