Abstract
We aimed to design and manufacture a transporter capable of delivering small interfering RNAs (siRNAs) into the skin without causing any damage. β-glucans are unique chiral polysaccharides with well-defined immunological properties and supramolecular wrapping ability. However, the chiral properties of these polymers have hardly been applied in drug delivery systems. In this study, β-glucan nanoparticles were designed and manufactured to deliver genetic material to the target cells. The β-glucan molecules were self-assembled with an siRNA into nanoparticles of 300–400 nm in diameter via a conformational transition process, in order to construct a gene delivery system. The assembled gene nanocarriers were associated with high gene-loading ability. The expression and efficiency of siRNA were verified after its delivery via β-glucan. Our results provide evidence that β-glucan nanoparticles can be effectively used to deliver siRNA into the cells.
Highlights
Small interfering RNAs suppress the expression of the target gene and regulate it, suggesting a new possibility of their exploitation in gene therapy [1,2,3]
It was confirmed that a ratio of 1:4 was ideal, which was applied to subsequent experiments. siRNAs can be loaded into the low-molecular-weight glucan nanoparticles (GluNPs) by forming hydrogen bonds between them
Summary siRNAs have considerable value in the treatment of diseases; it is challenging to deliver them to the target tissues, because of their large sizes
Summary
Small interfering RNAs (siRNAs) suppress the expression of the target gene and regulate it, suggesting a new possibility of their exploitation in gene therapy [1,2,3]. The development of siRNAs for practical application requires a technique for stably and effectively delivering the siRNAs to the target tissue. There are problems associated with siRNA delivery at various stages, depending on the route of delivery and the effect of the physical and biochemical environment of the disease [7,8,9]. The development of β-glucan nanocarriers has garnered increasing attention owing to its particular chiral interaction with bioactive molecules. The supramolecular interactions between β-glucans and pharmaceutical molecules are based on chiral interactions instead of excessive electrostatic/hydrophobic interactions, which are frequently adopted in conventional polymer drug delivery systems that may lead to denaturing of tissue proteins and damage to cell membranes [10,11,12,13,14]. Β-glucan itself has a well-established immunopotentiation ability with low toxicity, as has been demonstrated in Biomedicines 2020, 8, 497; doi:10.3390/biomedicines8110497 www.mdpi.com/journal/biomedicines
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