Enhanced transdermal delivery of lutein via nanoethosomal gel: Formulation optimization, in-vitro evaluation, and in-vivo assessment

Abstract

Lutein has low oral bioavailability and penetration through the skin. Therefore, the major objective is the development of ethosomal gel loaded with lutein to enhance dermal deposition of lutein. Lutein-loaded formulation (Lut-eth) was developed and optimized using QbD software. The characterization of Lut-eth formulation was performed using zeta sizing (131.3 ± 1.10 nm) and zeta potential (−21.9 mV) which was later validated by electron microscopy. The lut-eth gel was prepared and values for content uniformity, spreadability, consistency, firmness, and toughness were found to be 97.89 ± 1.05%, 7.29 ± 0.015 gcm/s, 2.495 ± 0.24 g s, 0.210 ± 0.01g, and 0.37 ± 0.01 respectively. Rheological investigation reveals viscosity was 2.56.2 mPa s (millipascal second) and shows high elasticity and stability. whereas, consistency, firmness, toughness, the force of adhesion, and work of adhesion was found to be 2.495 ± 0.24 g s, 0.210 ± 0.01g, 0.37 ± 0.01, −0.23 ± 0.05 N, and −55.61 ± 0.11 N s respectively. The lut-eth gel had a maximum plasma concentration of 9.428 ± 3.5 ng/mL in 4 h with AUC0-1279. 679 ± 9.87 ng h mL−1. The drug release study shows sustain release behavior of prepared formulation and a similar sustain release pattern was observed in and Ex-vivo release studies. Confocal laser microscopy, In-vitro, antioxidant study shows better deposition and improved antioxidant effect of formulation which was further validated by Ex-vivo antioxidant assay. Therefore, bearing in mind all these findings, it can be said that Lut-eth gel could be a novel formulation to improve lutein deposition on skin.