Ocular Inserts for Sustained Release of the Angiotensin-Converting Enzyme 2 Activator, Diminazene Aceturate, to Treat Glaucoma in Rats

Foureaux, Giselle; Franca, Juçara Ribeiro; Nogueira, José Carlos; Fulgêncio, Gustavo de Oliveira; Ribeiro, Tatiana G.; Castilho, Rachel Oliveira; Yoshida, María Irene; Fuscaldi, Leonardo Lima; Fernandes, Simone Odília Antunes; Cardoso, Valbert Nascimento; Cronemberger, Sebastião; Faraco, André Augusto Gomes; Ferreira, Anderson J.

doi:10.1371/journal.pone.0133149

Cited by 31 publications

(19 citation statements)

References 58 publications

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“…Quantification of the active substance from the inserts was performed with the UV-Vis spectrometer and in vitro release studies using a Franz cell. The authors concluded that inserts reduce intraocular pressure by up to 4 weeks [143].…”

Section: Inserts and Implantsmentioning

confidence: 99%

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

Popa¹,

Ghica²,

Dinu-Pîrvu³

et al. 2018

Chitin-Chitosan - Myriad Functionalities in Science and Technology

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This chapter focuses on the eye, one of the most important organs of humans. Current data on pathophysiology of the human eye are presented in direct correlation with a range of therapeutic products, with a well-known and widely used material, namely chitosan. Applications of chitosan biopolymer are described in the development of innovative, modern, therapeutic devices and solutions. Thus, chitosan is a good excipient either for classic drop-type ocular systems, as well as for complex drug systems such as nanostructures (nanoparticles, nanomicelles and nanosuspensions), liposomes, microemulsions, microspheres, in situ hydrogels and inserts or implants. A number of disadvantages for ocular administration of the drugs are thus overcome.

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Section: Inserts and Implantsmentioning

confidence: 99%

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

Popa¹,

Ghica²,

Dinu-Pîrvu³

et al. 2018

Chitin-Chitosan - Myriad Functionalities in Science and Technology

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show abstract

“…Similarly, FA-loaded inserts released 70% ± 26%, 93% ± 9% and 100% of peptide in 10, 20 and 30 min, respectively. It should be noticed that under physiological conditions the volume of tears is limited and thus the insert could hydrate, adhere to the mucus on the ocular surface and release the drug more slowly [51,52]. Strong antioxidant activity of FA has been reported for concentrations of 1 mg/mL [53], which could be provided by the inserts (0.14 mg FA in the 2.5 mg insert) on the ocular surface in few minutes after application.…”

Section: Ocular Inserts Of Nanofibers Crosslinked With ε-Polylysinementioning

confidence: 99%

Crosslinked Hyaluronan Electrospun Nanofibers for Ferulic Acid Ocular Delivery

Grimaudo

Concheiro

2020

Pharmaceutics

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Electrospun nanofibers are gaining interest as ocular drug delivery platforms that may adapt to the eye surface and provide sustained release. The aim of this work was to design an innovative ophthalmic insert composed of hyaluronan (HA) nanofibers for the dual delivery of an antioxidant (ferulic acid, FA) and an antimicrobial peptide (ε-polylysine, ε-PL). Polyvinylpyrrolidone (PVP) was added to facilitate the electrospinning process. Fibers with diameters of approx. 100 nm were obtained with PVP 5%-HA 0.8% w/v and PVP 10%-HA 0.5% w/v mixtures in ethanol:water 4:6 v/v. An increase in PVP concentration to 20% w/v in both presence and absence of HA rendered fibers of approx. 1 µm. PVP 5%-HA 0.8% w/v fibers were loaded with 83.3 ± 14.0 µg FA per mg. After nanofibers crosslinking with ε-PL, blank and FA-loaded inserts showed a mean thickness of 270 ± 21 µm and 273 ± 41 µm, respectively. Blank and FA-loaded inserts completely released ε-PL within 30 min under sink conditions, whereas FA-loaded inserts released the antioxidant within 20 min. Both blank and FA-loaded inserts were challenged against Pseudomonas aeruginosa and Staphylococcus aureus, demonstrating their efficacy against relevant microbial species.

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“…Interestingly, however, Ang (1-7) injections delivered either intracamerally or intravitreally, did not promote AH outflow. Rats with experimentally induced ocular hypertension showed a significant decrease in IOP, less retinal ganglion cell death as well as reduced optic nerve degeneration when treated with chitosan inserts that released ACE2 continuously activating DIZE [215]. In contrast to Ang (1-7), Ang II has mainly negative effects on human eye although some results are controversial.…”

Section: The Effects Of Raas Components On Iopmentioning

confidence: 99%

Local ocular renin–angiotensin–aldosterone system: any connection with intraocular pressure? A comprehensive review

2020

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The renin-angiotensin system (RAS) is one of the oldest and most extensively studied human peptide cascades, well-known for its role in regulating blood pressure. When aldosterone is included, RAAS is involved also in fluid and electrolyte homeostasis. There are two main axes of RAAS: (1) Angiotensin (1-7), angiotensin converting enzyme 2 and Mas receptor (ACE2-Ang(1-7)-MasR), (2) Angiotensin II, angiotensin converting enzyme 1 and angiotensin II type 1 receptor (ACE1-AngII-AT1R). In its entirety, RAAS comprises dozens of angiotensin peptides, peptidases and seven receptors. The first mentioned axis is known to counterbalance the deleterious effects of the latter axis. In addition to the systemic RAAS, tissue-specific regulatory systems have been described in various organs, evidence that RAAS is both an endocrine and an autocrine system. These local regulatory systems, such as the one present in the vascular endothelium, are responsible for long-term regional changes. A local RAAS and its components have been detected in many structures of the human eye. This review focuses on the local ocular RAAS in the anterior part of the eye, its possible role in aqueous humour dynamics and intraocular pressure as well as RAAS as a potential target for anti-glaucomatous drugs. KEY MESSAGES Components of renin-angiotensin-aldosterone system have been detected in different structures of the human eye, introducing the concept of a local intraocular renin-angiotensin-aldosterone system (RAAS). Evidence is accumulating that the local ocular RAAS is involved in aqueous humour dynamics, regulation of intraocular pressure, neuroprotection and ocular pathology making components of RAAS attractive candidates when developing new effective ways to treat glaucoma.

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Ocular Inserts for Sustained Release of the Angiotensin-Converting Enzyme 2 Activator, Diminazene Aceturate, to Treat Glaucoma in Rats

Cited by 31 publications

References 58 publications

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

Crosslinked Hyaluronan Electrospun Nanofibers for Ferulic Acid Ocular Delivery

Local ocular renin–angiotensin–aldosterone system: any connection with intraocular pressure? A comprehensive review

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