Development and Charecterization of Caffeine and Quercetin Loaded Nasal Niosomal In-Situ Gel for Treatment of Depression

Abstract

Caffeine and Quercetin both are used in combination for the treatment of patient with depression as they are adenosine antagonist due to which they elevate the level of neurotransmitters. The study was designed with two aims. First, is to enhance the solubility and bioavailability of BCS Class II i.e. Quercetin; secondly to ease administration of the formulation to the patient with depression. The culmination of this study, the caffeine and quercetin loaded niosomal in-situ gel for nose-to-brain delivery was formulated. Niosomes were prepared and optimized by using definitive screening design whereas, the Niosomal in-situ gel were prepared and optimized using central composite design. The vesicle size of the optimized batch was found to be 0.281±0.26µm. The % EE of all niosomal batches was found to be in a range of 81.52±0.21% to 98.72±0.16% for Caffeine and 94.3±0.31 to 99.73±0.23 for Quercetin and the cumulative % release was found to be in a range of 72.09±0.18% to 103.3±0.26% for Caffeine and 10.9±0.31% to 37.06±0.15% for Quercetin at 4hrs. DSC, FTIR studies were performed for pure drug and optimized niosomal batch. All the gels as per design were formulated, where the Spreadability was found to be in range of 5.1±0.26cm to 7.9±0.16cm and viscosity after gelation in range of 1800±0.11cps to 4780±0.26cps. The % drug permeated was found to be in range of 85.86±0.015% to 98.61±0.024% for Caffeine and 22.65±0.19% to 33.23±0.34% for Quercetin at 6hrs. These results indicated that niosomal In-situ gel can be used to enhance the bioavailability of drug by directly delivering the drug to the brain by avoiding first pass effect.