Efficient Functional Delivery of siRNA using Mesoporous Silica Nanoparticles with Ultralarge Pores

• Published in: Small (Weinheim an der Bergstrasse, Germany) Germany), 2012-06, Vol.8 (11), p.1752-1761
• Main Authors: Na, Hee-Kyung, Kim, Mi-Hee, Park, Kihyun, Ryoo, Soo-Ryoon, Lee, Kyung Eun, Jeon, Hyesung, Ryoo, Ryong, Hyeon, Changbong, Min, Dal-Hee
• Format: Article
• Language: English
• Subjects: cancer therapy; drug delivery; mesoporous materials; nanoparticles; Nanoparticles - chemistry; Porosity; RNA interference; RNA, Small Interfering - administration & dosage; RNA, Small Interfering - chemistry; Silicon Dioxide - chemistry; Temperature
• ISSN: 1613-6810; 1613-6829
• DOI: 10.1002/smll.201200028

Among various nanoparticles, mesoporous silica nanoparticles (MSNs) have attracted extensive attention for developing efficient drug‐delivery systems, mostly due to their high porosity and biocompatibility. However, due to the small pore size, generally below 5 nm in diameter, potential drugs that are loaded into the pore have been limited to small molecules. Herein, a small interfering RNA (siRNA) delivery strategy based on MSNs possessing pores with an average diameter of 23 nm is presented. The siRNA is regarded as a powerful gene therapeutic agent for treatment of a wide range of diseases by enabling post‐transcriptional gene silencing, so‐called RNA interference. Highly efficient, sequence‐specific, and technically very simple target gene knockdown is demonstrated using MSNs with ultralarge pores of size 23 nm in vitro and in vivo without notable cytotoxicity. A strategy for efficient small interfering RNA (siRNA) delivery is developed using mesoporous silica nanoparticles with pores of diameter 23 nm (MSN23). The siRNA delivery vehicle is designed to load siRNAs inside the pores for high loading capacity and thus effective protection from nucleases, to accomplish highly efficient siRNA‐mediated target gene knockdown.