Baig, MS, Owida, H, Njoroge, W, Siddiqui, A-U-R and Yang, Y (2019) Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin. Journal of Drug Delivery Science and Technology, 55. ISSN 1773-2247

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Besifloxacin hydrochloride (BSF) is a new ophthalmic antibiotic. However, its low water solubility limits its therapeutic efficacy. This article reported a novel lipid based drug delivery system to enhance ocular bioavailability of BSF. Cationic nanostructured lipid carriers (CNLC) were prepared and optimized by Box-Behnken design of using Design Expert Software®. Effect of concentration of three independent variables, Stabilizer, Solid lipid and Liquid Lipid were studied on three dependent variables Particle size, Polydispersity Index (PDI) and zeta potential of the CNLC particles. The surfactant, hexadecyltrimethylammonium bromide (CTAB) was used to optimize the surface charge of the nano-particles. The BSF loaded nano-particles, CNLC-BSF, were characterized fully. Rhodamine was trapped to CNLC-BSF for imaging. The cytotoxicity and cellular infiltration of CNLC-BSF were assessed by 2-dimensional (2D) and 3-dimensional (3D) conjunctival tissue model. It was revealed that the CNLC’s values, particle size, PDI and zeta potential remained stable over 2-week storage. The entrapment efficiency was around 80% for optimum formulation. The cell internalization of CNLC increased when CTAB concentration increased in CNLC-BSF. The formulation showed good penetration property through 3D tissue model. The cytotoxicity assessed by MTT assay showed minimum 60% cell viability on conjunctival fibroblast model for the optimized formula with inclusion of 0.6 mg/mL BSF.

Item Type: Article
Additional Information: This is the accepted author manuscript (AAM). The final published version (version of record) is available online via Elsevier at - please refer to any applicable terms of use of the publisher.
Uncontrolled Keywords: Cationic nanostructured lipid carrier; CNLC; Ophthalmic drug delivery; Bioavailability; Infiltration; Besifloxacin; Box-Behnken; Design-Expert
Subjects: R Medicine > R Medicine (General)
Divisions: Faculty of Medicine and Health Sciences > Institute for Science and Technology in Medicine
Depositing User: Symplectic
Date Deposited: 06 Jan 2020 16:14
Last Modified: 26 Jan 2021 16:36

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