Evaluation of the Pharmacokinetics and Ocular Tolerance of a Microemulsion Containing Tacrolimus

Silva-Cunha, Armando; Silva, Gisele Rodrigues da; Castro, Whocely Victor de; Fialho, Sílvia Ligório

doi:10.1089/jop.2013.0128

Cited by 20 publications

(7 citation statements)

References 17 publications

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“…The increasing efficiency of lipid-based nanocarriers over the last years has made them a target for constant and thorough research. In fact, these formulations have been already used in both preclinical and clinical practice demonstrating favorable outcomes treating ocular diseases [ 10 , 11 , 16 , 51 , 87 , 91 , 98 , 103 , 126 , 131 , 145 , 146 , 147 , 148 , 149 , 150 , 151 , 152 , 153 , 154 , 155 , 156 , 157 , 158 , 159 , 160 , 161 , 162 , 163 , 164 , 165 , 166 , 167 , 168 , 169 ]. With all these promising results and taking advantage of the new technologies, researchers, pharmacists, and clinical professionals must continue this line of investigation and encourage the use of these new formulations in the near future in clinical medical practice.…”

Section: Discussionmentioning

confidence: 99%

Lipid-Based Nanocarriers as Topical Drug Delivery Systems for Intraocular Diseases

et al. 2021

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Effective drug delivery to intraocular tissues remains a great challenge due to complex anatomical and physiological barriers that selectively limit the entry of drugs into the eye. To overcome these challenges, frequent topical application and regular intravitreal injections are currently used to achieve the desired drug concentrations into the eye. However, the repetitive installation or recurrent injections may result in several side effects. Recent advancements in the field of nanoparticle-based drug delivery have demonstrated promising results for topical ophthalmic nanotherapies in the treatment of intraocular diseases. Studies have revealed that nanocarriers enhance the intraocular half-life and bioavailability of several therapies including proteins, peptides and genetic material. Amongst the array of nanoparticles available nowadays, lipid-based nanosystems have shown an increased efficiency and feasibility in topical formulations, making them an important target for constant and thorough research in both preclinical and clinical practice. In this review, we will cover the promising lipid-based nanocarriers used in topical ophthalmic formulations for intraocular drug delivery.

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Section: Discussionmentioning

confidence: 99%

Lipid-Based Nanocarriers as Topical Drug Delivery Systems for Intraocular Diseases

et al. 2021

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“…Additionally, w/o µEs are particularly interesting for oral protein delivery due to their increased oral bioavailability through the gastrointestinal tract and their protection capacity [ 144 ]. A large number of drugs, such as antibiotics [ 141 , 142 , 143 , 144 , 145 , 146 ], antifungals [ 147 , 148 , 149 ], anti-inflammatory [ 150 , 151 , 152 , 153 , 154 ] and immunosuppressive [ 155 ] molecules have been used in μEs systems.…”

Section: Achievements and Challengesmentioning

confidence: 99%

Microemulsion Microstructure(s): A Tutorial Review

et al. 2020

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Microemulsions are thermodynamically stable, transparent, isotropic single-phase mixtures of two immiscible liquids stabilized by surfactants (and possibly other compounds). The assortment of very different microstructures behind such a univocal macroscopic definition is presented together with the experimental approaches to their determination. This tutorial review includes a necessary overview of the microemulsion phase behavior including the effect of temperature and salinity and of the features of living polymerlike micelles and living networks. Once these key learning points have been acquired, the different theoretical models proposed to rationalize the microemulsion microstructures are reviewed. The focus is on the use of these models as a rationale for the formulation of microemulsions with suitable features. Finally, current achievements and challenges of the use of microemulsions are reviewed.

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“…Moreover, this system is suitable for ocular drug delivery because the small droplet size of MEs can enhance ocular drug bioavailability by either prolonging drug release and/or improving drug penetration through the ocular tissues. MEs are safe and biocompatible for the treatment of ocular diseases with better penetrability and have a suitable pharmaceutical effect [ 15 , 16 , 17 , 18 , 19 , 20 ]. However, passive penetration of MEs only might be unable to deliver drugs through the ocular tissue at the therapeutically effective dose.…”

Section: Introductionmentioning

confidence: 99%

Optimal Design of Novel Microemulsions-Based Two-Layered Dissolving Microneedles for Delivering Fluconazole in Treatment of Fungal Eye Infection

et al. 2022

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The optimal design of novel microneedles (MNs) for the ocular delivery system is necessary and useful for improving the effectiveness of medication. The objective of this study was to design and develop the optimal fluconazole (FLUZ)-microemulsions (MEs)-loaded two-layered dissolving MNs as a potential treatment for fungal eye infection. The experimental designs using the simplex-lattice design were used to select the optimal formulation. The two-layered dissolving MNs were fabricated from 3% chitosan and 20% polyvinyl alcohol (PVA) in a weight ratio of 1:4 as an outer layer and FLUZ-loaded MEs containing eugenol, tween 80, PEG400, and water as an inner layer. The physical appearance, mechanical properties, penetration ability, dissolution time, in vitro/ex vivo ocular drug delivery, and antifungal activity were evaluated. From the results, the optimal two-layered dissolving MNs exhibited good physical properties, complete insertion, minimally invasive ocular tissue, and high stability at 4 °C and 25 °C for 3 months. Moreover, the optimal two-layered dissolving MNs showed significantly higher FLUZ permeation into the ocular tissue than other formulations, while providing highly potential antifungal activity. In conclusion, the optimal MEs-loaded two-layered MNs’ formulation had appropriate properties for ocular delivery of FLUZ, resulting in an improvement of fungal keratitis treatment.

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Evaluation of the Pharmacokinetics and Ocular Tolerance of a Microemulsion Containing Tacrolimus

Abstract: The developed microemulsion could be an alternative to reduce the systemic adverse effects of tacrolimus and, consequently, increase the patient compliance to the treatment.

Cited by 20 publications

References 17 publications

Lipid-Based Nanocarriers as Topical Drug Delivery Systems for Intraocular Diseases

Lipid-Based Nanocarriers as Topical Drug Delivery Systems for Intraocular Diseases

Microemulsion Microstructure(s): A Tutorial Review

Optimal Design of Novel Microemulsions-Based Two-Layered Dissolving Microneedles for Delivering Fluconazole in Treatment of Fungal Eye Infection

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