Publication

Abstract : In this study an inclusion complex between Brinzolamide (BRZ) and 2-Hydroxypropyl Beta Cyclodextrin (2-HP-β-CD) was prepared and incorporated into Chitosan (CS)/Tripolyphosphate (TPP) nanogels to provide sustained release of BRZ with increased retention time in the corneal region. Further to this, an attempt was made to increase the viscosity of the prepared CS/TPP nanogels using CS/PVA (polyvinyl alcohol) biopolymer composite. BRZ, is a second line therapy for glaucoma but suffers from poor aqueous solubility leading to lesser absorption and side effects on its administration in ocular delivery. Thus by increasing the solubility and ocular retention will reduce its frequency of administration and dose followed by increases its absorption.BRZ was complexed with 2-HP-β-CD by solvent evaporation and confirmed by FTIR, XRD and SEM. The complex was incorporated into chitosan nanogels and evaluated for in vitro drug release, ex vivo mucoadhesive and permeation studies.BRZ-2-HP-β-CD complex (1:1 molar ratio) showed improved aqueous solubility and dissolution as compared to BRZ aqueous dispersion. Chitosan nanogels showed particle size of 219.1 ± 0.94 nm, zeta potential of +26.63 ± 0.28 mV, entrapment efficiency of 80.2837 ± 1.7635% having sustained release and following Fickian diffusion. CDNG1 exhibited 15.32 fold increases in the in vitro corneal permeability coefficient in comparison with commercial Brinolar® and exhibited mucoadhesive properties.The results imply the potential of BRZ-HP-β-CD complex loaded Chitosan Nanogels as a novel formulation of BRZ for ocular delivery. © 2019, Advanced Scientific Research. All rights reserved.