Improved release of triamcinolone acetonide from medicated soft contact lenses loaded with drug nanosuspensions

Abstract

Drug nanosuspensions (NSs) show a significant potential to improve loading and release properties of the poorly water soluble drug triamcinolone acetonide (TA) from poly(hydroxyethyl methacrylate) (pHEMA) soft contact lenses. In this work, TA NSs were developed by a controlled precipitation method using a fractional factorial Plackett-Burmann design. Poloxamer 407 (PL) and polyvinyl alcohol (PVA) as stabilizing agents were selected. NSs were characterized in terms of their drug content, particle size and morphology. Results indicate that all studied factors, except homogenization speed and sonication, have significant influence on the drug incorporation yield into NSs. Drug nanoparticles showed an interesting size that may be suitable for their incorporation into topical ocular drug delivery systems, as hydrogels. pHEMA hydrogels and daily-wear Hilafilcon B commercial contact lenses (SCLs) were employed to study TA loading capacity and drug release properties using NSs as loading system. Hydrogels have been synthesised by copolymerization of 2-hydroxyethyl methacrylate (HEMA) with methacrylic acid (MA) in accordance with a previous work (García-Millán et al., 2015). Both synthesised hydrogels and SCLs were characterized in terms of their mechanical and physical properties and TA loading and release properties. Selected TA NS was further characterized by studying its physical-chemical stability during the loading process. Results show that the use of TA NSs as loading medium significantly increases drug loading capacity and release of soft contact lenses in comparison with drug saturated solution. Synthesised pHEMA hydrogels and SCLs lenses have good properties as ophthalmic drug delivery systems, but SCLs load higher quantities of drug and release TA in shorter time periods than synthesised pHEMA hydrogel.

Keywords: 2,2′-Azo-bis(isobutyronitrile) AIBN (CID 6547); 2-Hydroxyethyl methacrylate HEMA (CID 13360); Ethyleneglycol dimethacrylate EGDMA (CID:7355) Poloxamer 407; Medicated soft contact lenses; Methacrylic acid MA (CID: 4093); Nanosuspensions; Ocular; Ocular drug release; Polyvinyl alcohol PVA (CID 11199); Triamcinolone Acetonide TA (CID: 6436); Triamcinolone acetonide; pHEMA hydrogels.