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BRINZOLAMIDE-2-HYDROXYPROPYL BETA CYCLODEXTRIN COMPLEX LOADED CHITOSAN NANOGEL FOR OCULAR DRUG DELIVERY
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| Author:
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DHANAJA PILLAI, SABITHA M, SWATI GUPTA
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| Abstract:
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In this study an inclusion complex between Brinzolamide (BRZ) and 2- Hydroxypropyl Beta Cyclodextrin (2-HP-ß-
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-ß-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-ß-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-ß-CD complex loaded Chitosan Nanogels as a novel
formulation of BRZ for ocular delivery
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| Keyword:
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Brinzolamide, 2- Hydroxypropyl Beta Cyclodextrin, Chitosan Nanogels, Mucoadhesive, Ocular delivery
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| EOI:
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| DOI:
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