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 MANGALATHILLUM, SWATI GUPTA
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Abstract:
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Objective: 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.
Significance: 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.
Methods: 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.
Results: 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.
Conclusions: 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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https://doi.org/10.31838/ijpr/2019.11.02.002
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