Development of rivaroxaban microemulsion-based hydrogel for transdermal treatment and prevention of venous thromboembolism

Araújo, Cristina da Costa Bernardes; Simon, Alice; Honorio, Thiago da Silva; Silva, Silvia Valéria Cruz da; Valle, Isabella Mourão M.; Silva, Luiz Cláudio Rodrigues Pereira da; Rodrigues, Carlos Rangel; Sousa, Valéria Pereira de; Cabral, Lúcio Mendes; Sathler, P.C; Carmo, Flávia Almada do

doi:10.1016/j.colsurfb.2021.111978

Cited by 7 publications

(4 citation statements)

References 66 publications

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“…The system consists of a donor compartment and a recipient compartment, which are separated by a synthetic membrane or pig ear skin. The system simulates what happens when a formulation is applied on the skin [28][29][30].…”

Section: Ex Vivo Permeation Profilementioning

confidence: 99%

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Development of SEDDS formulation containing caffeine for dermal delivery

Almeida

Honorio

Carmo

et al. 2023

Intern J of Cosmetic Sci

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Objective: The objective of this work was to develop a self-emulsifying drug delivery system (SEDDS) containing caffeine for the treatment of cellulite.Methods: SEDDS were prepared using the solution method. 0.5% (w/v) caffeine was added to the previously selected excipients. The system was characterized by droplet size, zeta potential, emulsification time and long-term stability. In vitro release and skin permeation were investigated using Franz-type diffusion cells.The cytotoxicity was evaluated on normal human keratinocytes.Results: Caffeine SEDDS were thermodynamically stable, with a zeta potential less than -22 mV and droplet size around 30 nm, and were long-term stable. The permeation study showed that the formulation promoted caffeine accumulation in the skin layers, suggesting an increase in local circulation. Cytotoxicity studies on HaCaT cells were not conclusive as the surfactant used indicated false-positive results due to its high molar mass. Conclusion:It was possible to obtain a stable SEDDS that could cause an increase in blood flow in the applied area, resulting in cellulite reduction.

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Section: Ex Vivo Permeation Profilementioning

confidence: 99%

“…Skins with cuts or holes on the surface were discarded. The experimental protocol does not need to be authorized by an ethics committee as this biological material was obtained from a local butcher for human consumption [30,31].…”

Section: Ex Vivo Permeation Profilementioning

confidence: 99%

Development of SEDDS formulation containing caffeine for dermal delivery

Almeida

Honorio

Carmo

et al. 2023

Intern J of Cosmetic Sci

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“…A recently explored alternative to this is the creation of a hybrid system in which the bioactive compound is sequestered within gel-loaded emulsions . Carmo and co-workers reported transdermal delivery of the anticoagulant rivaroxaban (RVX) from surfactant-stabilized emulsions that were encapsulated within a polymer-based topical gel.…”

Section: Macroscale Materialsmentioning

confidence: 99%

“…A recently explored alternative to this is the creation of a hybrid system in which the bioactive compound is sequestered within gel-loaded emulsions. 70 Carmo and co-workers reported transdermal delivery of the anticoagulant rivaroxaban (RVX) from surfactant-stabilized emulsions that were encapsulated within a polymer-based topical gel. Using a multiparametric optimization approach, the team identified conditions that would afford emulsions ∼100 nm in size that could be stability loaded into propylene glycol hydrogels.…”

Section: ■ Microscale Vehiclesmentioning

confidence: 99%

Biomaterials-Enabled Antithrombotics: Recent Advances and Emerging Strategies

Hale

Medina

2022

Mol. Pharmaceutics

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Antithrombotic and thrombolytic therapies are used to prevent, treat, and remove blood clots in various clinical settings, from emergent to prophylactic. While ubiquitous in their healthcare application, short half-lives, off-target effects, overdosing complications, and patient compliance continue to be major liabilities to the utility of these agents. Biomaterials-enabled strategies have the potential to comprehensively address these limitations by creating technologies that are more precise, durable, and safe in their antithrombotic action. In this review, we discuss the state of the art in anticoagulant and thrombolytic biomaterials, covering the nano to macro length scales. We emphasize current methods of formulation, discuss how material properties affect controlled release kinetics, and summarize modern mechanisms of clot-specific drug targeting. The preclinical efficacy of these technologies in an array of cardiovascular applications, including stroke, pulmonary embolism, myocardial infarction, and blood contacting devices, is summarized and performance contrasted. While significant advances have already been made, ongoing development efforts look to deliver bioresponsive "smart" biomaterials that will open new precision medicine opportunities in cardiology.

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