RRC ID 51326
著者 Suzuki Y, Okuda T, Okamoto H.
タイトル Development of New Formulation Dry Powder for Pulmonary Delivery Using Amino Acids to Improve Stability.
ジャーナル Biol Pharm Bull
Abstract Cationic polymers are being studied as non-viral gene delivery vectors. Poly{N-[N-(2-aminoethyl)-2-aminoethyl]aspartamide} (PAsp(DET)) and their block copolymers with poly(ethylene glycol), PEG-PAsp(DET), have been reported as efficient biodegradable non-viral vectors which form a polyplex with plasmid DNA (pDNA). However, the polyplexes are not stable because PAsp(DET) and PEG-PAsp(DET) are easily subjected to hydrolysis; therefore, they need to be prepared on site. In this study, using the biodegradable polycations as non-viral vectors, PAsp(DET) and PEG-PAsp(DET), we investigated the effects of L-leucine (Leu) on the polyplex. We prepared solutions and dry powders with and without Leu. Both dry powders had large and porous particles and Leu acted as a dispersing agent. The transfection activity of the sample solutions decreased within a month. However, the decrease in the transfection activity was partially suppressed by the dry powder with Leu at 5 and 25°C at 3 months. Furthermore, transfection experiments revealed that Leu exhibited a pDNA-stabilizing effect in the solution and dry powder. Similar results were observed for pDNA integrity, where a polyplex was formed in the dry powder. The results suggest that Leu is a candidate stabilizer to protect pDNA from degradation.
巻・号 39(3)
ページ 394-400
公開日 2016-1-1
DOI 10.1248/bpb.b15-00822
PMID 26725531
MeSH Administration, Inhalation Animals Cell Line, Tumor DNA / administration & dosage DNA / chemistry* Drug Compounding Drug Stability Gene Expression Leucine / chemistry* Luciferases, Firefly / genetics Mice Particle Size Peptides / chemistry* Plasmids Polyethylene Glycols / chemistry* Powders
IF 1.863
引用数 6
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