Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin

Baig, Mirza Salman; Owida, Hamza Abu; Njoroge, Wanjiku; Siddiqui, Aquil-Ur-Rahim; Yang, Ying

doi:10.1016/j.jddst.2019.101496

Cited by 22 publications

(24 citation statements)

References 26 publications

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“…A manufacturing advantage of using high-energy methods is the low size dispersion obtained. The sonication and high-energy mixing allow the obtention of PdI around 0.1–0.3 [ 43 ]. In our formulation, the low size distribution is attributed to the cooling process.…”

Section: Resultsmentioning

confidence: 99%

Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation

et al. 2021

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Lipid nanocarriers have a great potential for improving the physicochemical characteristics and behavior of poorly water-soluble drugs, such as aqueous dispersibility and oral bioavailability. This investigation presents a novel nanostructured lipid carrier (NLC) based on a mixture of solid lipid glycerides, fatty acid esters of PEG 1500 (Gelucire® 44/14), and an oil mix composed of capric and caprylic triglycerides (Miglyol® 812). These NLCs were developed by a simple low-energy method based on melt emulsification to yield highly encapsulating and narrowly distributed nanoparticles (~100 nm, PdI = 0.1, and zeta potential = ~−10 mV). Rhodamine 123 was selected as a poorly water-soluble drug model and owing to its spectroscopic properties. The novel NLCs were characterized by dynamic light scattering (DLS), zeta potential, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and colloidal stability. The drug release was determined through a dialysis bag and vertical Franzs’ cells to provide insights about the methods’ suitability, revealing similar performance regardless of their different fluid dynamics. Rhodamine 123 followed a characteristic biphasic release profile owing to the swelling of the hydrophilic polymer coating and diffusion process from the lipid core as revealed by the Korsmeyers–Peppas kinetic modeling. Moreover, to elucidate the formation and incorporation of Rhodamine 123 into the NLC core, several molecular dynamics simulations were conducted. The temperature was shown to be an important condition to improve the formation of the nanoparticles. In addition, the liquid lipid incorporation to the formulation forms nanoparticles with imperfect centers, in contrast to nanoparticles without it. Moreover, Miglyol® 812 improves hydrophobic molecule solubility. These results suggest the potential of novel NLC as a drug delivery system for poorly water-soluble drugs.

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Section: Resultsmentioning

confidence: 99%

Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation

et al. 2021

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“…The presented research on lipid-based nanocarriers has also shown that one optimisation problem can be approached following different experimental designs, still arriving, in any case, at valid polynomials [97]. For instance, the same formulation problem regarding solid lipid nanoparticles has been optimised by a three-level full factorial, central composite, Box-Behnken or Taguchi designs [120,125,134,155]. It is important to underline that one single experimental design will in most cases not offer all the responses and that meticulous planification and statistical analysis are more important than experimental work.…”

Section: Discussionmentioning

confidence: 99%

“…Quadratic effects were observed for three of the responses, while entrapment efficiency demonstrated to be not influenced by the variables under study. A robust optimised formulation, stable over 1 month if stored between 2 and 8 • C, was obtained with up to 3% of effectively loaded ibuprofen that showed no burst release and a sustained release over 12 h. Following a three-factor Box-Behnken design, Baig and colleagues [134] prepared besifloxacin-loaded cationic nanostructured lipid carriers. Besifloxacin is a practically insoluble fourth-generation fluoroquinolone, approved as suspension by the FDA for the treatment of bacterial conjunctivitis [140].…”

Section: Box-behnken Designs (Bbds)mentioning

confidence: 99%

“…A good number of examples are available in the literature for the optimisation of lipid-based nanocarriers, as depicted in Table 4 [ 116 , 134 , 135 , 136 , 137 , 138 , 139 ].…”

Section: Optimising the Outcomes: Statistical Design Of Experiments (Doe)mentioning

confidence: 99%

“…Following a three-factor Box–Behnken design, Baig and colleagues [ 134 ] prepared besifloxacin-loaded cationic nanostructured lipid carriers. Besifloxacin is a practically insoluble fourth-generation fluoroquinolone, approved as suspension by the FDA for the treatment of bacterial conjunctivitis [ 140 ].…”

Section: Optimising the Outcomes: Statistical Design Of Experiments (Doe)mentioning

confidence: 99%

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Lipid-Based Nanocarriers for Ophthalmic Administration: Towards Experimental Design Implementation

González-Fernández

Bianchera

Gasco³

et al. 2021

Pharmaceutics

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Nanotherapeutics based on biocompatible lipid matrices allow for enhanced solubility of poorly soluble compounds in the treatment of ophthalmic diseases, overcoming the anatomical and physiological barriers present in the eye, which, despite the ease of access, remains strongly protected. Micro-/nanoemulsions, solid lipid nanoparticles (SLN) or nanostructured lipid carriers (NLC) combine liquid and/or solid lipids with surfactants, improving drug stability and ocular bioavailability. Current research and development approaches based on try-and-error methodologies are unable to easily fine-tune nanoparticle populations in order to overcome the numerous constraints of ocular administration routes, which is believed to hamper easy approval from regulatory agencies for these systems. The predictable quality and specifications of the product can be achieved through quality-by-design (QbD) implementation in both research and industrial environments, in contrast to the current quality-by-testing (QbT) framework. Mathematical modelling of the expected final nanoparticle characteristics by variation of operator-controllable variables of the process can be achieved through adequate statistical design-of-experiments (DoE) application. This multivariate approach allows for optimisation of drug delivery platforms, reducing research costs and time, while maximising the understanding of the production process. This review aims to highlight the latest efforts in implementing the design of experiments to produce optimised lipid-based nanocarriers intended for ophthalmic administration. A useful background and an overview of the different possible approaches are presented, serving as a starting point to introduce the design of experiments in current nanoparticle research.

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Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin

Cited by 22 publications

References 26 publications

Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation

Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation

Lipid-Based Nanocarriers for Ophthalmic Administration: Towards Experimental Design Implementation

Research on scale inhibition law of high sulfate mine water based on response surface methodology

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