Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

Abstract

Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.

Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases

“…The ZP values above 30 mV correspond to suitable ZP, as it allows stabilizing the NLCs dispersion while preventing the possible aggregation due to the repulsive interaction among particles [46]. Lastly, higher RLZ amounts increased the EE, as NLCs possess high loading capacity due to the liquid lipids added, and also because RLZ lipophilic and low solubility nature favors the interaction with the lipid matrix [47,48]. Therefore, the DoE led to an optimized formulation of RLZ-NLCs with values adequate for skin application purposes (Z av around 200 nm; PI < 0.2; ZP ± 30 mV and EE ≥ 70 %) [49,50].…”

Recent Developments of Nanostructures for the Ocular Delivery of Natural Compounds

“…Some of the surfactants are more toxic than others and irritate the eye and should be eliminated once the nanocarriers are formulated. According to Leonardi et al (2014) findings, some surfactants caused no irritation to the eye such as Kolliphor ® P188, and some made irritation in a high concentration such as Tween ® 80, and some of them like sodium dodecyl sulfate made severe irritation ( Üner et al, 2021 ). Cationic nanocarriers in comparison to neutral or anionic carriers can bind more effectively to the negatively charged mucin (in corneal and conjunctival epithelium), enhance the retention time, and the therapeutic effect of the entrapped drugs.…”