Comparative assessment of efficacy and safety potential of multifarious lipid based Tacrolimus loaded nanoformulations

Publication date: Available online 19 March 2019Source: International Journal of PharmaceuticsAuthor(s): Sanyog Jain, Ramu Addan, Varun Kushwah, Harshad Harde, Rahul R. MahajanAbstractThe present work reports the development, optimization and characterization of novel lipid based nanoformulations viz., Liquid crystalline nanoparticles (LCNP), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) and liposomes loaded with Tacrolimus (Tac) for topical delivery. Different nanoformulations were developed after screening lipids and suitable surfactants depending upon emulsification ability. The various nanoformulations were then optimized (to achieve higher entrapment efficacy, lower particle size, PDI and zeta potential), characterized and loaded into gel. The gels loaded with nanoformulations were also characterized depending upon rheology and viscosity. The gels were analyzed for in vitro drug release, HaCaT cell lines studies and skin permeation studies. The in vivo efficacy studies were carried out using mouse tail model and skin irritation studies using Draize patch test and measurement of TEWL. The developed nanoformulations showed optimum particle size (<200 nm), polydispersity index (PDI<0.3), zeta potential (≥-10 mV) and higher entrapment efficiency (>85 %). The nanoformulations showed higher penetration of Tac into skin. Tac-LCNP, Tac-SLN, Tac-NLC and Tac-liposomes loaded gels showed 14, 11.5, 12.5 and 3.7 folds increment in dermal bioavailab...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research