The effect of cyclodextrin on both the agglomeration and the in vitro characteristics of drug loaded and targeted silica nanoparticles

Abstract

One of the problems in the use of nanoparticles (NPs) as carriers in drug delivery systems is their agglomeration which mainly appears due to their high surface energy. This results in formation of NPs with different sizes leading to differences in their distribution and bioavailability. The surface coating of NPs with certain compounds can be used to prevent or minimize this problem. In this study, the effect of cyclodextrin (CD) on the agglomeration state and hence on the in vitro characteristics of drug loaded and targeted silica NPs was investigated. A sample of NPs was loaded with anticancer agents, then modified with a long polymer, carboxymethyl-β-cyclodextrin (CM-β-CD) and folic acid (FA), respectively. Another sample was modified similarly but without CD. The surface modification was characterized using fourier transform infrared spectroscopy (FT-IR). The polydispersity (PD) was measured using dynamic light scattering (DLS) and was found to be smaller for CD modified NPs. The results of the in vitro drug release showed that the release rate from both samples exhibited similar pattern for the first 5 hours, however the rate was faster from CD modified NPs after 24 hours. The in vitro cell viability assay confirmed that CD modified NPs were about 30% more toxic to HeLa cells. These findings suggest that CD has a clear effect in minimizing the agglomeration of such modified silica NPs, accelerating their drug release rate and enhancing their targeting effect.