Lipid Nanoparticles for Drug Delivery

Xu, LT; Wang, X; Liu, Y; Yang, GZ; Falconer, RJ; Zhao, CX

Abstract

Lipid nanoparticles have attracted significant interests in the last two decades, and have achieved tremendous clinical success since the first clinical approval of Doxil in 1995. At the same time, lipid nanoparticles have also demonstrated enormous potential in delivering nucleic acid drugs as evidenced by the approval of two RNA therapies and mRNA COVID-19 vaccines. In this review, an overview on different classes of lipid nanoparticles, including liposomes, solid lipid nanoparticles, and nanostructured lipid carriers, is first provided, followed by the introduction of their preparation methods. Then the characterizations of lipid nanoparticles are briefly reviewed and their applications in encapsulating and delivering hydrophobic drugs, hydrophilic drugs, and RNAs are highlighted. Finally, various applications of lipid nanoparticles for overcoming different delivery challenges, including crossing the blood-brain barrier, targeted delivery, and various routes of administration, are summarized. Lipid nanoparticles as drug delivery systems offer many attractive benefits such as great biocompatibility, ease of preparation, feasibility of scale-up, nontoxicity, and targeted delivery, while current challenges in drug delivery warrant future studies about structure-function correlations, large-scale production, and targeted delivery to realize the full potential of lipid nanoparticles for wider clinical and pharmaceutical applications in future.

Keywords: drug delivery; large-scale production; lipid nanoparticles; microfluidics; nanostructured lipid carriers; RNA delivery; solid lipid nanoparticles

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Lipids

Lipid nanoparticles are revolutionizing the field of drug delivery, providing a sophisticated method to transport therapeutic agents effectively within the body. These nanoparticles are tiny, spherical particles composed of lipids, which are naturally occurring molecules such as fats and oils. Due to their biocompatibility and ability to encapsulate both hydrophilic (water-soluble) and hydrophobic (fat-soluble) drugs, lipid nanoparticles are becoming increasingly popular in medical research and treatment. One of the key advantages of lipid nanoparticles is their ability to protect drugs from degradation in the body's harsh environment, ensuring that the therapeutic agents remain stable and active until they reach their target. This encapsulation can enhance the bioavailability of drugs, meaning that a greater amount of the drug reaches the bloodstream and the intended site of action. This is particularly beneficial for drugs that are otherwise poorly soluble or easily degraded. Additionally, lipid nanoparticles can be engineered to achieve controlled and sustained release of drugs, providing a steady therapeutic effect over time and reducing the need for frequent dosing. They can also be designed to target specific tissues or cells, which is crucial for treating diseases such as cancer, where it is essential to deliver drugs directly to the tumor while minimizing impact on healthy cells.