How Do Lipids Improve the Properties of Small Molecule Drugs

Lipids have a wide range of applications in therapeutics for many years. Recently, lipid nanoparticles have been used for the delivery of mRNA which can resist SARS-COVID-2 virus, and they have also been applied as the delivery carriers of CRISPR/Cas-9 gene-editing technologies. Lipodomics recognize and quantify the level of biological lipids using lipid standards. The researchers hope to translate the data into clinical biomarkers of diseases. Some lipids have even been used for the treatments of specific diseases, acting as small molecule drugs. In addition, some of the drawbacks of other small molecule drugs can be improved by lipids.

In the development stage, the drug molecules need to overcome economical, biological and chemical barriers to be eventually used for clinical experiments. Containing epithelium, endothelium, and elimination, the biological barriers work on the drugs by restricting their access to the target site of the action.

Several strategies can be used to address the barriers and assist the drugs to reach their targets. As is mentioned previously, lipid nanoparticles have been used to deliver therapeutic drugs with their role to protect their load from biological barriers and deliver it to cell interior. In addition, the active drug can be conjugated with a non-toxic and non-active pro-moiety to create a pro-drug. The non-toxic and non-active pro-moiety is separated from the active drug as soon as it arrives its target. Then, it is rapidly excreted.

Researchers often choose biocompatible compounds, such as lipids, peptides or amphipathic polymers as the non-active and non toxic moieties which are conjugated with small molecule active drugs. Lipids are strong candidates for small molecule lipidic pro-drugs as they are  abundant, easily available, non-toxic, biocompatible and biodegradable. Many small molecule lipidic pro-drugs can also assemble themselves into stable nanostructure.

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