Sustained delivery of epalrestat to the retina using PEGylated solid lipid nanoparticles laden contact lens (Retracted article. See vol. 624, 2022)

Currently to treat diabetic eye diseases like cataract or diabetic retinopathy oral or intravitreal route is used, and there is still a demand for the efficient dosage forms. Contact lens can be used to deliver drug to the ocular tissues, however, the presence of hydrophobic drug like epalrestat alter the critical lens properties. In this study, Pluronic (R) F68 stabilized pegylated solid lipid nanoparticles laden contact lens was designed to deliver epalrestat to the anterior and posterior side of the eye without affecting the critical lens properties. The characterization studies indicate that the pegylated-solid lipid nanoparticles (p-SLNs) were more spherical and smaller in size in comparison to the non-pegylated-SLNs. The in vitro release studies suggest that the direct p-SLNs laden contact lenses (DL-EP-p-SLN) showed promising results (low burst release and sustain release up to 196 h) in comparison to the p-SLNs soaked contact lenses (SM-EP-p-SLN, high burst release and sustain release up to 144 h). The selected DL-EP-p-SLN-100 batch was found to be safe in ocular irritation study. In tear fluid (rabbit model) studies, the DL-EP-p-SLN-100 batch showed high epalrestat concentration at all-time points in comparison to the SM-EP-p-SLN-100 batch. The bio-distribution study indicate high epalrestat accumulation in the various ocular tissues including retina, which suggest the potential of p-SLNs laden contact lenses to deliver drug to the posterior side of the eye to treat diabetic eye conditions like cataract and diabetic retinopathy.