Therapeutic nanoemulsions in ophthalmic drug administration: Concept in formulations and characterization techniques for ocular drug delivery

Singh, Mahendra; Bharadwaj, Shiv; Lee, Jun Young; Kang, Sang Gu

doi:10.1016/j.jconrel.2020.10.025

Cited by 81 publications

(68 citation statements)

References 185 publications

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“…Currently explored applications of lipid nanoparticles incorporating biologically active fatty acids and monoglycerides are focused on skin and systemic infections, while another key opportunity would be the utilization of biologically active lipids to treat ocular infections. The eye is an organ that is inaccessible from other systemic sites due to blood-aqueous, blood-retinal, and blood-vitreous barriers [ 112 ]. Therefore, topical ophthalmic delivery is the most frequent way to deliver drugs to the eye.…”

Section: Discussionmentioning

confidence: 99%

“…Indeed, the eye is a complicated organ with sophisticated dynamic (reflex blinking, tear secretion, dose spillage, and nasolacrimal drainage) and static (poor permeability of corneal epithelium) barriers that significantly limit ophthalmic product residence on the eye surface, restrict drug absorption, and obstruct the treatment of ocular diseases, including infections [ 119 ]. Cationic oil-in-water NEs are promising systems for topical ophthalmic drug delivery due to increased residence time on the eye surface, which is attributed to electrostatic interactions of positively charged oil nanodroplets with negatively charged ocular surface mucins [ 112 ]. The oil nanodroplets gradually break down over time and the released oil molecules can subsequently intercalate into the lipid layer of the tear film whereas the surfactant molecules can merge with the muco-aqueous gel layer [ 120 , 121 ].…”

Section: Discussionmentioning

confidence: 99%

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Lipid Nanoparticle Technology for Delivering Biologically Active Fatty Acids and Monoglycerides

Tan

Yoon

Cho

et al. 2021

IJMS

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There is enormous interest in utilizing biologically active fatty acids and monoglycerides to treat phospholipid membrane-related medical diseases, especially with the global health importance of membrane-enveloped viruses and bacteria. However, it is difficult to practically deliver lipophilic fatty acids and monoglycerides for therapeutic applications, which has led to the emergence of lipid nanoparticle platforms that support molecular encapsulation and functional presentation. Herein, we introduce various classes of lipid nanoparticle technology and critically examine the latest progress in utilizing lipid nanoparticles to deliver fatty acids and monoglycerides in order to treat medical diseases related to infectious pathogens, cancer, and inflammation. Particular emphasis is placed on understanding how nanoparticle structure is related to biological function in terms of mechanism, potency, selectivity, and targeting. We also discuss translational opportunities and regulatory needs for utilizing lipid nanoparticles to deliver fatty acids and monoglycerides, including unmet clinical opportunities.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Lipid Nanoparticle Technology for Delivering Biologically Active Fatty Acids and Monoglycerides

Tan

Yoon

Cho

et al. 2021

IJMS

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“…As the chorioallantoic membrane (CAM) vascularization is resemblant to the mucosal tissue of humans, it is possible to use CAM to evaluate the irritating effect of tested materials and formulations in vitro prior to the in vivo and clinical tests. 17 Freshly harvested fertilized hen eggs incubated for 3 days at 37 ± 0.5 °C are used for the test. In the fertilized eggs, a hole is made above the air chamber, through which the internal egg shell membrane (IESM) is moistened with a 0.9% sodium chloride solution.…”

Section: Ocular Nanoemulsions Research Methodsmentioning

confidence: 99%

“… 16 The prolonged precorneal retention time and high penetration capacity of nanoemulsions result in enhanced ocular bioavailability. 17 The surfactants and cosurfactants present in nanoemulsion formulations act as penetration enhancers facilitating corneal transport of the drug. They remove the mucus layer and disrupt tight junctional complexes enabling increased API penetration into the deeper layers of the eye.…”

Section: Introductionmentioning

confidence: 99%

“… 18 − 23 Increased ocular absorption of the drug from nanoemulsions, as compared with conventional eye drops, may reduce the number of doses and ultimately simplify a dosing scheme, resulting in better patients' compliance. 17 , 18 Dissolution of hydrophobic API in the lipid phase of a nanoemulsion provides reproducible dose administration as compared with ophthalmic suspensions, gels, and ointments. 24 − 27 For example, the o/w nanoemulsion with 0.4% concentration of brinzolamide confirmed enhanced penetration into the corneal tissue and higher therapeutic efficacy in vivo in comparison with the commercially available 1% brinzolamide suspension.…”

Section: Introductionmentioning

confidence: 99%

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Ophthalmic Nanoemulsions: From Composition to Technological Processes and Quality Control

et al. 2021

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Nanoemulsions are considered as the most promising solution to improve the delivery of ophthalmic drugs. The design of ophthalmic nanoemulsions requires an extensive understanding of pharmaceutical as well as technological aspects related to the selection of excipients and formulation processes. This Review aims at providing the readers with a comprehensive summary of possible compositions of nanoemulsions, methods for their formulation (both laboratory and industrial), and differences between technological approaches, along with an extensive outline of the research methods enabling the confirmation of in vitro properties, pharmaceutical performance, and biological activity of the obtained product. The composition of the formulation has a major influence on the properties of the final product obtained with low-energy emulsification methods. Increasing interest in high-energy emulsification methods is a consequence of their scalability important from the industrial perspective. Considering the high-energy emulsification methods, both the composition and conditions of the process (e.g., device power level, pressure, temperature, homogenization time, or number of cycles) are important for the properties and stability of nanoemulsions. It is advisible to determine the effect of each parameter on the quality of the product to establish the optimal process parameters’ range which, in turn, results in a more reproducible and efficient production.

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Design and Nanoengineering of Photoactive Antimicrobials for Bioapplications: from Fundamentals to Advanced Strategies

Xin,

Liu,

Xiao

et al. 2024

Adv Funct Materials

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Currently, microbial infections have posed an arduous challenge to global public health, whereas the rise of antibiotic resistance is rendering traditional antibiotic therapies futile, prompting the development of new antimicrobial technologies. Photoactive nanomaterials have thus garnered a thriving interest for disinfection owing to their superior antibacterial efficaciousness, favorable biosafety, and rapidness and spatiotemporal precision in excreting bactericidal actions. The review summarizes recent advances and emerging trends in the design, nanoengineering, and bioapplications of photoactive antimicrobials. It commences by elaborating fundamental theories on bacterial resistance, and antibacterial mechanisms of nanomaterials and phototherapy. Subsequently, the regulation of the antibacterial effectiveness of photoactive nanomaterials is comprehensively discussed, centering on criteria and strategies for tuning photoabsorption spectra, photothermal conversion, and photocatalytic efficiency, alongside tactics for enabling synergistic therapies. This is followed by comparative analyses of techniques and modalities for synthesizing and engineering photoactive nanomaterials with diverse structures, forms, and functionalities. Thereafter, the state‐of‐the‐art applications of phototherapies across various medical sectors are portrayed, and key challenges and opportunities are finally discussed to spur future innovations and translation. This review is envisaged to provide useful guidance for devising and developing nanomaterials‐based photoresponsive antimicrobials with application‐specific materials properties and biological functions.

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Therapeutic nanoemulsions in ophthalmic drug administration: Concept in formulations and characterization techniques for ocular drug delivery

Cited by 81 publications

References 185 publications

Lipid Nanoparticle Technology for Delivering Biologically Active Fatty Acids and Monoglycerides

Lipid Nanoparticle Technology for Delivering Biologically Active Fatty Acids and Monoglycerides

Ophthalmic Nanoemulsions: From Composition to Technological Processes and Quality Control

Design and Nanoengineering of Photoactive Antimicrobials for Bioapplications: from Fundamentals to Advanced Strategies

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