Abstract
Small-interfering RNA (siRNA)-mediated gene silencing with the aid of chitosan (CS)-based carriers has shown efficient and reliable outcome in vitro, but the gene silencing efficiency in vivo is still limited. It is of great importance to balance the protection and release of siRNA from nanoparticles (NPs) so as to achieve high efficiency. However, siRNA release profile from CS/siRNA NPs has been rarely concerned. Here, Förster resonance energy transfer technique was adopted for in vitro investigation of siRNA release from CS NPs in lysozyme-contained buffer. The results clearly showed that siRNA molecules experienced a fast and short release phase under lysozyme competition to both CS and siRNA, and then a slow and long release under lysozyme degradation on CS. Moreover, lysozyme competition played more important role than enzymolysis on trigging siRNA release. This preliminary study of siRNA release is the first step to get insight of in vivo siRNA release mechanism from CS/siRNA NPs, which will be helpful to adjust the design of CS/siRNA NPs for balancing the protection and release of siRNA molecules.
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