[Cayman] Lipid Nanoparticle (LNP) Formulation: 기본 개념 및 준비 과정

Lipid-based Drug Delivery (LBDD), Lipid Nanoparticle (LNP)

Cayman에서 제공하는 Lipid Nanoparticle (LNP) 관련 article입니다. 

mRNA 기반 COVID-19 백신의 성공은 Lipid-based Drug Delivery (LBDD)에 대한 수십 년의 연구가 없었다면 불가능했을 것입니다. LBDD 시스템은 small molecule inhibitors와 vaccine 성분과 같은 다양한 bioactive molecule을 표적 세포와 조직에 전달하기 위해 사용되어 왔습니다. LBDD는 기존 약물 전달 방법에 비해 약물 안정성, bioavailability 및 distribution을 포함한 몇 가지 장점이 있습니다. LBDD 시스템의 하위 집합인 Lipid Nanoparticles (LNP)은 oligonucleotide 기반 치료제의 전달에 있어 중요한 발전이었습니다. LNP 내에 캡슐화된 oligonucleotide는 전달 과정 동안 enzymatic degradation으로부터 보호되고, 치료용 단백질로 translation되어 세포에 효율적으로 전달됩니다. LNP가 oligonucleotide 기반 치료제의 혁신을 일으키는 엄청난 잠재력을 고려해 볼 때, 연구자들은 각자의 application으로 활용하기 위해 LNPs를 쫓고 있습니다.

Articel에서는 LNP에 중점을 두고, 일반적인 LBDD 시스템의 기본 개념과 그들이 운반하는 물질에 대해 소개하고 있습니다. 또한 LNP가 oligonucleotide를 전달하는 이유와 방법을 이해하기 위한 기초 이론과 LNP preparation을 위한 개념과 과정을 다루고 있습니다.
본 article은 연구자들 자신의 연구 영역과 응용 분야에서 LNP를 어떻게 활용할 수 있는지 이해하는 데 유용한 자료가 될 수 있을 것입니다.

주요 용어 정리

  • Lipid nanoparticles (LNPs): a lipid shell surrounding an internal core composed of reverse micelles that encapsulate and deliver oligonucleotides, like siRNA, mRNA, and plasmid DNA (pDNA) (Table 1).

  • Liposomes: contain one or more lipid bilayers and an aqueous core. They are further classified by lamellarity and size. Liposomes can be used for the delivery of hydrophobic and/or hydrophilic small molecules. 

  • Solid lipid nanoparticles (SLNs): a surfactant shell surrounding a core matrix composed of solid lipids. They are used for the encapsulation of hydrophobic and/or hydrophilic cargo.

  • Nanostructured lipid carriers (NLCs): a surfactant shell surrounding a core matrix composed of solid and liquid lipids. They are used for the encapsulation of hydrophobic and/or hydrophilic cargo.

  • Micelles: self-assemblies of lipid monolayers in aqueous solutions. They have a hydrophobic core, where the phospholipid tails are oriented towards the interior, and can be used for the encapsulation of small hydrophobic cargo.

  • Reverse micelles: an inverted structure compared with traditional micelles. They form a hydrophilic core, with the phospholipid tails oriented towards the exterior, and can be used for the encapsulation of small hydrophilic cargo, like oligonucleotides in LNPs.  

Table 1: Comparison of LNPs to other LBDD systems

 
Lipid Nanoparticel
Liposome
Solid Lipid Nanoparticle
Nanostructured Lipid Carrier
  lipid_nanoparticle liposome solid_lipid_nanoparticle nanostructured_lipid_carrier
Lipid Shell Monolayer Bilayer Surfactant Surfactant
Internal Core Reverse micelles Aqueous Solid lipids Solid and liquid lipids
Cargo Oligonucleotides Hydrophobic and/or hydrophilic small molecules Hydrophobic and/or hydrophilic small molecules Hydrophobic and/or hydrophilic small molecules
Size ~20 – 100 nm ~50 – 1,000 nm ~40 – 1,000 nm ~40 – 1,000 nm
lipid_construct

Available from Cayman

LBDD systems are at the forefront of gene therapy, vaccine formulations, and targeted drug delivery. The use of high-quality lipids is critical for the success of an LBDD system. Cayman has decades of experience in lipid synthesis and assay development. Our extensive catalog contains numerous lipids that can be used to form LBDD particles, as well as LNP Exploration Kits that contain reagents for the formation of SM-102- or ALC-0315-containing LNPs. We also offer Custom Lipid Synthesis services to assist in the formulation and characterization of your LBDD system.

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