PHARMACEUTICAL COMPOSITION OF LIPID NANOPARTICLES FOR DELIVERING NUCLEIC ACID MEDICINES CONTAINING TREHALOSE DERIVATIVE AND NOVEL STRUCTURE-MAINTAINING COMPOUND

The present invention relates to a novel composition of lipid nanoparticles for stabilizing nucleic acid drugs and enhancing in vivo deliverability. The lipid nanoparticles are composed of nucleic acid medicines and lipids, wherein the nucleic acid includes all of mRNA-based vaccines, immunoenhancer RNA, miRNA, siRNA, pDNA, antisense ODN, pDNA, and the like. The lipids of the lipid nanoparticles include trehalose-based lipids, ionization lipids, phospholipids, PEG-lipids, and structural lipids. Among these, the structural lipids provide a composition capable of replacing commonly used cholesterol with a lithocholic acid derivative, a glycyrrhetinic acid derivative, or a diosgenin derivative compound. The lipid nanoparticles according to the present invention may be used as a vaccine or a therapeutic agent according to the type of nucleic acid medicine used. La présente invention concerne une nouvelle composition de nanoparticules lipidiques pour stabiliser des médicaments d'acide nucléique et améliorer la capacité d'administration in vivo. Les nanoparticules lipidiques sont composées de médicaments d'acide nucléique et de lipides, l'acide nucléique comprenant tous les vaccins à base d'ARNm, l'ARN immunostimulateur, l'ARNmi, l'ARNsi, l'ADNp, l'ODN antisens, l'ADNp et analogues. Les lipides des nanoparticules lipidiques comprennent des lipides à base de tréhalose, des lipides d'ionisation, des phospholipides, des PEG-lipides et des lipides structuraux. Parmi ceux-ci, les lipides structuraux fournissent une composition pouvant remplacer le cholestérol couramment utilisé avec un dérivé d'acide lithocholique, un dérivé d'acide glycyrrhétinique, ou un composé dérivé de diosgénine. Les nanoparticules lipidiques selon la présente invention peuvent être utilisées en tant que vaccin ou agent thérapeutique selon le type de médicament à base d'acide nucléique utilisé. 본 발명은 핵산 약물의 안정화 및 체내 전달력 증진을 위한 지질나노입자의 신규 조성물에 관한 것이다. 지질나노입자는 핵산 의약품과 지질로 구성되어 있으며, 핵산은 mRNA 기반 백신, 면역증강제 RNA, miRNA, siRNA, pDNA, antisense ODN，ｐDNA 등을 모두 포함한다. 지질나노입자의 지질은 트레할로즈 기반 지질, 이온화 지질, 인지질, PEG-지질 및 구조 유지 지질을 포함한다. 이중 구조 유지 지질은 통상적으로 사용되는 콜레스테롤을 리토콜산 유도체, 글리시레틴산 유도체 또는 디오스게니 유도체 화합물로 대체 가능한 조성을 제공한다. 본 발명의 지질나노입자는 사용하는 핵산의약품의 종류에 따라 백신 또는 치료제로 활용될 수 있다.