Pirfenidone-loaded chitosan nanoparticles are stable after 6 months, a new study published in the Future Journal of Pharmaceutical Sciences found. The nanoparticles could be used as a better alternative to treat idiopathic pulmonary fibrosis (IPF) since they can enhance the concentration of pirfenidone in deep lung tissues with a single, lower dose.

Pirfenidone has already been approved by the US Food and Drug Administration for the treatment of IPF. However, the fact that the drug is delivered orally means that it has reduced bioavailability in the presence of food. Therefore, a higher dose of treatment is needed, which leads to side effects such as dyspepsia, anorexia, and photosensitivity.

In the present study, 2 researchers from India prepared and tested an inhalable powder containing pirfenidone-loaded chitosan nanoparticles.


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They found that all nanoparticles were spherical. The optimum particles had a size between 436.9 nm and 444.7 nm in diameter, a zeta potential between 35.5 mV and 37.1 mV, an entrapment efficiency between 30.96% and 34.56%, and a percent drug release rate at 12 hours between 91.61% and 98.89%.

When the amount of chitosan was increased, the rate of drug release from the nanoparticles was reduced. Moreover, when the stabilizer concentration increased, the entrapment of pirfenidone into chitosan nanoparticles decreased.

Aerodynamic studies showed that the nanoparticles’ mass median aerodynamic diameter was 1.28 μm, which means that they could penetrate deep into the lungs and therefore be effective for the treatment of IPF. The authors concluded that the nanoparticles could be “a suitable alternative to the currently available therapy.”

Even though the exact mechanism of action of pirfenidone is not clear, it is known that the treatment has antifibrotic, anti-inflammatory, and antioxidant properties. It has also been shown to inhibit fibroblast proliferation and differentiation and collagen synthesis.

Reference

Dudhat K, Patel H. Preparation and evaluation of pirfenidone loaded chitosan nanoparticles pulmonary delivery for idiopathic pulmonary fibrosis. Futur J Pharm Sci. 2022;8:29. doi:10.1186/s43094-022-00419-3