Our aim is to study the effects of varying the two acyl moieties in synthesized N,N-diacyl spermines on siRNA formulations and their delivery efficiency in cell lines. Six novel asymmetrical lipopolyamines: [N-cholesteryloxy-3-carbonyl-N-oleoyl-, N-decanoyl-N-oleoyl-, N-decanoyl-N-stearoyl-, N-lithocholoyl-N-oleoyl-, N-myristoleoyl-N-myristoyl-, and N­ oleoyl-N-stearoyl]-1,12-diamino-4,9-diazad...

Our aim is to study the effects of varying the two acyl moieties in synthesized N,N-diacyl spermines on siRNA formulations and their delivery efficiency in cell lines. Six novel asymmetrical lipopolyamines: [N-cholesteryloxy-3-carbonyl-N-oleoyl-, N-decanoyl-N-oleoyl-, N-decanoyl-N-stearoyl-, N-lithocholoyl-N-oleoyl-, N-myristoleoyl-N-myristoyl-, and N­ oleoyl-N-stearoyl]-1,12-diamino-4,9-diazad...

Biodegradable poly(ester amine) (PEA)-based and poly(amido amine) (PAA)-based nanoparticles were developed for efficient in vitro siRNA delivery to human umbilical vein endothelial cells (HUVECs). They were screened, characterized, and compared with traditionally studied DNA-containing particles. Several of the polymeric nanoparticles tested were found to be effective for delivering functional ...

Efficient systemic siRNA delivery to cells in the target tissue is a current critical challenge in the drug delivery field. Several studies have demonstrated that nanoparticles such as polyethylene glycol (PEG)-coated siRNA-lipoplexes may enhance the systemic delivery of siRNA to tumor. However, the disordered tumor microenvironment still poses a potential impediment with respect to the efficie...

Nonspecific association of serum molecules with short-interfering RNA (siRNA) nanoparticles can change their physiochemical characteristics, and results in reduced cellular uptake in the target tissue during the systemic siRNA delivery process. Serum albumin is the most abundant protein in the body and has been used to modify the surface of nanoparticles, to inhibit association of other serum m...

Introduction A safe and effective in vivo siRNA delivery system is a prerequisite for liver tumor treatment based on siRNA cancer therapeutics. Nanoparticles based on superparamagnetic iron oxide (SPIO) provide a promising delivery system. In this study, we aimed to explore a novel nanoparticle, which is composed of SPIO. Materials and methods The particles have a core of iron oxide that is m...

The discovery of RNA interference (RNAi) in mammalian cells has created a new class of therapeutics based on the reversible silencing of specific disease-causing genes. This therapeutic potential depends on the ability to deliver inducers of RNAi, such as short-interfering RNA (siRNA) and micro-RNA (miRNA), to cells of target tissues. This chapter reviews various challenges and delivery strateg...

RNA interference technology has recently been highlighted as a powerful research method as well as a potential therapeutic treatment for several diseases. However, the delivery of small interfering RNA (siRNA) into T cell lines and primary blood cells is exceedingly challenging, as they are resistant to transfection by conventional reagents. As a result, there is an unmet need for nonviral, eff...

For therapeutic applications of siRNA, there are technical challenges with respect to targeted and systemic delivery. We here report a new siRNA carrier, RNAtr NPs, in a way that multiple tandem copies of RNA hairpins as a result of rolling circle transcription (RCT) can be readily adapted in tumour-targeted and systemic siRNA delivery. RNAtr NPs provide a means of condensing large amounts of m...

Macrophages play a key role in the development of many diseases, like tissue injury, cancer and autoimmune diseases. So far, single-drug loaded nanoparticles have been developed to target macrophages. Nevertheless, macrophage dysregulation can induce multiple conditions, i.e., inflammation fibrosis. Therefore, simultaneous co-delivery small molecule drug interfering RNA (siRNA) for gene silenci...