Extended Delivery of Pirfenidone with Novel, Soft Contact Lenses In Vitro and In Vivo

Abstract

The aim of this study was to fabricate pirfenidone (PFD)-loaded soft contact lenses (SCLs), explore their characteristics, and evaluate their efficiency on extended delivery of PFD in vitro and in vivo. Methods: PFD-loaded SCLs were fabricated by embedding an insert of PFD and polyvinyl alcohol (PVA) into 2 layers of silicone elastomer. The optical transparency, water content, and protein deposition were measured. Transformed human corneal epithelial cells were used to test the cytotoxicity of SCLs. The release rate of PFD by SCLs in vitro was evaluated by an ultraviolet-visible spectrophotometer. Toxicity of SCLs was assessed by inspection of ocular surface irritation in rabbits before and after contact lens wear. The concentrations of PFD in tears and aqueous humor of rabbits' eyes as a function of time were determined by high-performance liquid chromatography for SCLs and 30 mL of 0.5% PFD eye drops. Results: SCLs possessed good light transmittance. Blank SCLs had poor water content (0.548%-0.330), and an improved water content was found in PVA film-loaded SCLs (11.022%-1.508, P = 0.010). No lysozyme and human serum albumin were found in SCLs. There was no significant toxicity of SCLs in vitro and in vivo. SCLs prolonged the residence time of PFD in tears and aqueous humor of rabbit eyes by 5 times compared with the eye drop instillation while around 1/10 of the eye drop dosage was loaded in SCLs. Conclusions: PFD-loaded SCLs can significantly prolong the residence time of PFD and may be a promising ocular drug delivery system.

Functionalization of breast implants by cyclodextrin in-situ polymerization: a local drug delivery system for augmentation mammaplasty

“…The maximum released amount of each drug, reached in the equilibrium time, is reported in Table 2 . Results show that both pristine samples (S-Control and T-Control) were able to release considerable amounts of PFD, demonstrating the chemical compatibility between the chemical structure of PFD and silicone substrates ( Wu et al, 2021 ). In the case of functionalized samples, those polymerized with HPBCD presented higher amounts of released PFD than samples polymerized with BCD.…”

“…To attain a deeper perception of the mechanisms that govern the release of PFD, RB, and KR-12 from the functionalized samples, release profiles were fitted to the Korsmeyer-Peppas model ( Wu et al, 2021 ). The diffusion coefficients were obtained using the monolithic solution model ( Siepmann et al, 2012 ).…”

Pirfenidone: A Promising Drug in Ocular Therapeutics

“…[19] A formulation approach for extended drug delivery of pirfenidone using silicone soft contact lens was developed Wu C. et al and tested in vivo in rabbit model which significantly prolonged the residence time of pirfenidone and may be a promising ocular drug delivery system. [83] Altogether, these outcomes hold the potential of pirfenidone in offering additional therapeutic approaches for addressing PVR. Conducting additional clinical studies will be valuable in assessing the practical clinical use of pirfenidone.…”

Therapeutic applications of contact lens-based drug delivery systems in ophthalmic diseases

“…Furthermore, the addition of PVA makes the lens equipped with higher oxygen permeability and lower protein adsorption characteristics. PFD-PVA-loaded contact lens is a promising drug delivery system for inhibiting proliferative ocular diseases (Wu et al., 2021a , 2021b ).…”