Effective Ocular Delivery of Eplerenone Using Nanoengineered Lipid Carriers in Rabbit Model

Abstract

Background: Eplerenone (Epl) is a selective mineralocorticoid-receptor antagonist used for chronic central serous chorioretinopathy treatment. Our goal was to enhance the corneal performance of Epl-loaded nanostructured lipid carriers (NLCs) through surface modification using different coating polymers. Methods: Epl-loaded modified NLCs (Epl-loaded MNLCs) were prepared by coating the surface of Epl-loaded NLCs using different polymers, namely hyaluronic acid, chitosan oligosaccharide lactate, and hydrogenated collagen. A 3 1 ×4 1 full factorial design was used to evaluate the effect of the surface modification on the properties of the prepared systems. Selected optimal Epl-loaded MNLCs were further evaluated for in vitro drug release, morphology, pH, rheological properties, corneal mucoadhesion, irritation, and penetration. Results: Epl-loaded MNLCs were successfully prepared with high drug-entrapment efficiency and nanosized particles with low size distribution. Transmission electron microscopy revealed nanosized spherical particles surrounded by a coating layer of the surface modifier. The pH, refractive index, and viscosity results of the Epl-loaded MNLCs confirmed the ocular compatibility of the systems with no blurring of vision. The safety and ocular tolerance of the optimal MNLCs were confirmed using the hen's egg test on chorioallantoic membrane and by histopathological evaluation of rabbit eyes treated with the optimal systems. Confocal laser-scanning microscopy of corneal surfaces confirmed successful transcorneal permeation of the Epl-loaded MNLCs compared to the unmodified Epl-loaded NLCs, revealed by higher corneal fluorescence intensity at all time intervals. Conclusion: Overall, the results confirmed the potential of Epl-loaded MNLCs as a direct approach for Epl ocular delivery.

Formulation and Evaluation of Timolol Maleate Proniosomal Gel for Ocular Drug Delivery

“…Liposomes and niosomes containing vesicles exhibit the security issues like accumulation, spillage, combination, and sedimentation of vesicles because of the fluid idea of the framework. 14 The provesicular framework created to defeat these issues for an extraordinary novel methodology incorporates proliposomes and proniosomes. Provesicles are dry, anhydrous definitions, covered with a non-ionic surfactant, go about as a transporter blended in with water when required.…”

Oküler İlaç Taşiyici Si̇stem Olarak Li̇pi̇t Bazli Nanoparti̇küller

“…Sahip olduğu yüksek viskozite, diğer NLT modellerine kıyasla hiyalüronik asitle modifiye edilmiş NLT'lerin uzun süreli ilaç salımına sebep olmuştur. Draize testinde seçilen optimal formülasyonların (hiyalüronik asit/kitosan oligosakkarit laktat kaplı) oküler tolere edilebilirliğinin yüksek olduğu gösterilmiştir [48].…”

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

“…The higher viscosity determined the superior sustained drug release from hyaluronic acid-modified NLCs compared to the other NLCs models. The selected optimal formulations (hyaluronic acid/chitosan oligosaccharide lactate-coated) were characterized by an excellent ocular tolerability, as confirmed by the Draize test [ 187 ].…”