Pre-clinical safety of topically administered sunitinib-loaded lipid and polymeric nanocarriers targeting corneal neovascularization

Souza, Leonardo Gomes de; Sousa-Junior, Ailton A.; Cintra, Bertilha Alves Santana; Vieira, Jorge Luís; Nascimento, Thais Leite; Mendes, Lívia Palmerston; Vieira, Marcelo de Souza; Ducas, Rafael do Nascimento; Valadares, Marize Campos; Mendanha, Sebastião Antônio; Lima, Eliana Martins

doi:10.1016/j.ijpharm.2023.122682

Cited by 6 publications

(2 citation statements)

References 49 publications

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“…The pre-clinical safety of SLNs was evaluated in polymeric nanospheres and liposomes in a recent study conducted by Gomes Souza et al The authors elaborated sunitinib-loaded nanocarriers as topical formulation strategies for corneal neovascularization treatment. The sunitinib-loaded SLNs were selected as the optimal formulation due to their excellent tolerability profile, controlled drug release, and highest corneal retention [ 165 ].…”

Section: Feasibility Of Lipid Nanoparticles In Ophthalmologymentioning

confidence: 99%

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

Gugleva

Andonova

2023

Pharmaceuticals

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Sufficient ocular bioavailability is often considered a challenge by the researchers, due to the complex structure of the eye and its protective physiological mechanisms. In addition, the low viscosity of the eye drops and the resulting short ocular residence time further contribute to the observed low drug concentration at the target site. Therefore, various drug delivery platforms are being developed to enhance ocular bioavailability, provide controlled and sustained drug release, reduce the number of applications, and maximize therapy outcomes. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) exhibit all these benefits, in addition to being biocompatible, biodegradable, and susceptible to sterilization and scale-up. Furthermore, their successive surface modification contributes to prolonged ocular residence time (by adding cationic compounds), enhanced penetration, and improved performance. The review highlights the salient characteristics of SLNs and NLCs concerning ocular drug delivery, and updates the research progress in this area.

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Section: Feasibility Of Lipid Nanoparticles In Ophthalmologymentioning

confidence: 99%

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

Gugleva

Andonova

2023

Pharmaceuticals

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“…As STB free base is a BCS (Biopharmaceutics Classification System) IV compound with low permeability within the physiological pH range ( Gomes Souza et al, 2023 ), the malate form of STB has been developed and the market is present (Sutent) that has an aqueous solubility of 25 mg/mL over the pH range of 1.2–6.8 (Sunitinib, Center for drug evaluation and research, Application number: NDA 21–938 (GIST) and NDA 21–968 (MRCC), which is significantly improved the solubility of STB in aqueous media. To enhance the corneal permeability and the bioavailability of topically administered STB, Gomes Souza and coworkers ( Gomes Souza et al, 2023 ) recently loaded STB free base into three different types of nanocarriers polymeric nanospheres (NS), liposomes (LIP) and solid lipid nanoparticles (SLN), respectively to topically apply for treatment of CNV and SLN demonstrated the potential translation for treatment of CNV-targeting. It has been reported that STB base was encapsulated into liposomes to treat choroidal neovascularization in mouse model via the intravitreal injection and revealed inhibitory effect on established neovascularization ( Tavakoli et al, 2022 ).…”

Section: Introductionmentioning

confidence: 99%

Preparation of a Sunitinib loaded microemulsion for ocular delivery and evaluation for the treatment of corneal neovascularization in vitro and in vivo

Shi

Yang

et al. 2023

Front. Pharmacol.

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Background: Corneal neovascularization (CNV) is a pathological condition that can disrupt corneal transparency, thus harming visual acuity. However, there is no effective drug to treat CNV. Sunitinib (STB), a small-molecule multiple receptor tyrosine kinase inhibitor, was shown to have an effect on CNV. The purpose of this study was to develop an STB microemulsion (STB-ME) eye drop to inhibit CNV by topical application.Methods: We successfully prepared an STB-ME by the phase inversion emulsification method, and the physicochemical properties of STB-MEs were investigated. The short-term storage stability, cytotoxicity to human corneal epithelial cells, drug release, ocular irritation, ocular pharmacokinetics and the inhibitory effect on CNV were evaluated in vitro and in vivo.Results: The optimal formulation of STB-ME is composed of oleic acid, CRH 40, Transcutol P, water and sodium hyaluronate (SH). It is a uniform spherical particle with a mean droplet size of 18.74 ± 0.09 nm and a polydispersity index of 0.196 ± 0.004. In the in vitro drug release results, STB-ME showed sustained release and was best fitted by a Korsmeyer-Peppas model (R2 = 0.9960). The results of the ocular pharmacokinetics in rabbits showed that the formulation containing SH increased the bioavailability in the cornea (2.47-fold) and conjunctiva (2.14-fold). STB-ME (0.05% and 0.1%), administered topically, suppressed alkali burn-induced CNV in mice more effectively than saline, and high-dose (0.1%) STB-ME had similar efficacy to dexamethasone (0.025%).Conclusion: This study provides a promising formulation of STB-ME for the inhibition of CNV by topical administration, which has the excellent characteristics of effectiveness, sustained release and high ocular bioavailability.

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Effect of a protein kinase B (Akt) inhibitor on the angiogenesis of HUVECs and corneal neovascularization

Wang

2023

Wien Klin Wochenschr

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Pre-clinical safety of topically administered sunitinib-loaded lipid and polymeric nanocarriers targeting corneal neovascularization

Cited by 6 publications

References 49 publications

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

Preparation of a Sunitinib loaded microemulsion for ocular delivery and evaluation for the treatment of corneal neovascularization in vitro and in vivo

Effect of a protein kinase B (Akt) inhibitor on the angiogenesis of HUVECs and corneal neovascularization

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