Research Spotlight: Lipopolymers and Lipids from Lung Surfactants in Association with N-acetyl-l-cysteine: Characterization and Cytotoxicity

Posted on March 30, 2021

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"Lipopolymers and Lipids from Lung Surfactants in Association with N-acetyl-l-cysteine: Characterization and Cytotoxicity"

Liposome formulations often have benefits as drug-delivery agents such as reduced toxicity and enhancement of drug efficacy. UV irradiation of phospholipids creates photopolymerized lipids by cross-linking them through a diacetylene group and ultimately can result in lipopolymers with enhanced rigidity and stability. Lipids such as DMPC can be added to the formulation to increase the polymerization efficiency. Many illnesses affect the respiratory system and result in an increased production of mucous. Common respiratory illnesses include cystic fibrosis and pulmonary fibrosis. In cystic fibrosis, clearance of the mucus is hindered due to the loss of CFTR function. It would be useful if there were a method to effectively transport drugs with mucolytic activity directly to airways where mucus production is abnormal.

Thiol-based drugs are considered mucolytically active because they can interact with mucoproteins and reduce their viscosity by reducing the number of disulfide bonds present. NAC is one of these thiol-based mucolytically active drugs that is approved for use in humans. Nadia and her team looked to deliver NAC in a way that would allow its treatment to be exerted in areas of the respiratory system experiencing abnormal mucus production.

To do this, they used phospholipids (DMPC, DPPC, and PMPC) known to be major components of lung surfactants to increase the probability that the liposomes would deliver the drug to lung tissue. They tested a wide variety of lipid mixtures and studied their polymerization efficiency. These formulations were characterized by biophysical methods. The formulations were then tested for safety by assessing the cell toxicity on a line of human lung carcinoma cells.

The prepared formulations all exhibited a high polymerization profile, but those with a higher concentration of DMPC were the most efficient. When assessing the cell toxicity of the NAC carrying liposomes, the activity of mitochondrial enzymes in the A549 line of human lung carcinoma cells was slightly modified and decreased. The formulations thus present a mild toxic effect on cell viability.

Although further studies are warranted to assess cellular uptake and efficiency of these lipopolymer formulations, this work takes a huge step toward the repositioning of NAC in drug development.

Thank you, Nadia, for sharing your work with us! We’re excited to see what else you will accomplish with the help of our products! Don't forget to keep sending us your publications using Avanti products and connecting with us on social media!

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