Treatment for chemical burning using liquid crystalline nanoparticles as an ophthalmic delivery system for pirfenidone

Author(s)

Silva, Rummenigge Oliveira ^[1] ; da Costa, Bruna Lopes ^[1] ; da Silva, Flavia Rodrigues ^{[1, 2]} ; da Silva, Carolina Nunes ^[1] ; de Paiva, Mayara Brandao ^[1] ; Nunes Dourado, Lays Fernanda ^[1] ; Malachias, Angelo ^[3] ; de Souza Araujo, Adriano Antunes ^[4] ; Nunes, Paula Santos ^[2] ; Silva-Cunha, Armando ^[1]

Affiliation

^[1] Univ Fed Minas Gerais, Fac Pharm, BR-31270901 Belo Horizonte, MG - Brazil

^[2] Univ Fed Sergipe, Grad Program Appl Sci Hlth, BR-49400000 Lagarto, SE - Brazil

^[3] Univ Fed Minas Gerais, Exact Sci Inst, Dept Phys, BR-31270901 Belo Horizonte, MG - Brazil

^[4] Univ Fed Sergipe, Dept Pharm, BR-49100000 Lagarto, SE - Brazil

• Document type: Journal article
• Source: International Journal of Pharmaceutics; v. 568, SEP 10 2019.
• Web of Science Citations: 0

Abstract

Some recent studies have shown that pirfenidone (PFD) has favorable results in the healing process of the cornea. However, PFD in solution exhibits short half-life after topical application, and in this context, a liquid crystal nanoparticle system containing PFD (PFD-LCNPs) was developed. The nanoparticles were characterized by transmission electron microscopy, atomic force microscopy, small angle X-ray diffraction and polarized light microscopy. The PFD-LCNPs had particle size and zeta potential of 247.3 nm and -33.60 mV (stores at 4 degrees C), respectively, and 257.5 nm and -46.00 mV (stored at 25 degrees C), respectively. The pH of the formulation was 6.9 and the encapsulation efficiency was 35.9%. The in vitro release profiles indicated that PFD sustained release from PFD-LCNPs for up to 12 h. In vitro study of ocular irritation (HET-CAM test) concluded that components of the formulation are well tolerated for ocular administration. Corneal re-epithelialization time after chemical burning was significantly reduced in rabbits treated with PFD-loaded LCNPs when compared to the group treated with a vehicle. In addition, the anti-inflammatory action of pirfenidone was observed by reducing myeloperoxidase activity (MPO) and inflammatory cells in the histology of the tissues of animals treated with PFD-LCNPs. These findings indicated that the PFD-LCNPs might have the potential for effective ocular drug delivery. (AU)

• FAPESP's process: 14/50928-2 - INCT 2014: Pharmaceutical Nanotechnology: a transdisciplinary approach
• Grantee: Maria Vitória Lopes Badra Bentley
• Support Opportunities: Research Projects - Thematic Grants