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1.
Drug Discov Today ; 28(1): 103416, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36280041

RESUMO

Pterygium is a fibrovascular tissue growth invading the cornea. Adjunctive treatment post-surgery includes conventional immunosuppressants as well as antiviral drugs. The use of large- and small-molecule antivascular endothelial growth factor (VEGF) agents remains an integral part of pterygium treatment as well as other neovascular conditions of the eye. Naturally occurring polyphenolic compounds have favorable characteristics for treating neovascular and inflammatory eye conditions, including good efficacy, stability, cost-effectiveness, and the versatility of their chemical synthesis. In this review, we discuss pharmacological treatments of pterygium. Natural products, such curcumin, ellagic acid, and chalcones, are reviewed, with emphasis on their potential as future pterygium treatments.


Assuntos
Produtos Biológicos , Pterígio , Humanos , Pterígio/tratamento farmacológico , Pterígio/metabolismo , Pterígio/cirurgia , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Produtos Biológicos/metabolismo , Túnica Conjuntiva/metabolismo , Córnea/metabolismo
2.
Adv Drug Deliv Rev ; 177: 113957, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34481032

RESUMO

Non-oral long-acting drug delivery systems (LADDS) encompass a range of technologies for precisely delivering drug molecules into target tissues either through the systemic circulation or via localized injections for treating chronic diseases like diabetes, cancer, and brain disorders as well as for age-related eye diseases. LADDS have been shown to prolong drug release from 24 h up to 3 years depending on characteristics of the drug and delivery system. LADDS can offer potentially safer, more effective, and patient friendly treatment options compared to more invasive modes of drug administration such as repeated injections or minor surgical intervention. Whilst there is no single technology or definition that can comprehensively embrace LADDS; for the purposes of this review, these systems include solid implants, inserts, transdermal patches, wafers and in situ forming delivery systems. This review covers common chronic illnesses, where candidate drugs have been incorporated into LADDS, examples of marketed long-acting pharmaceuticals, as well as newly emerging technologies, used in the fabrication of LADDS.


Assuntos
Doença Crônica/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Polímeros/administração & dosagem , Animais , Formas de Dosagem , Humanos
3.
J Org Chem ; 84(15): 9811-9818, 2019 08 02.
Artigo em Inglês | MEDLINE | ID: mdl-31293163

RESUMO

The reactivity of hydrogen peroxide and catalytic hydroiodic acid toward 3,6-dimethoxy-2-(cycloamino)anilines is tunable to give ring-fused benzimidazoles or 1,4,6,9-tetramethoxyphenazine in high yield. Mechanisms via a detected nitroso-intermediate are proposed for oxidative cyclization and the unexpected intermolecular displacement of the oxazine. An aqueous solution of molecular iodine is capable of the same transformations. Oxidative demethylation gave targeted benzimidazolequinones, including without cleavage of the incorporated oxetane.


Assuntos
Antineoplásicos/química , Benzimidazóis/química , Descoberta de Drogas , Éteres Cíclicos/química , Morfolinas/química , Fenazinas/química , Quinonas/química , Ácidos/química , Antineoplásicos/síntese química , Benzimidazóis/síntese química , Catálise , Ciclização , Peróxido de Hidrogênio/química , Compostos de Iodo/química , Estrutura Molecular , Oxirredução , Fenazinas/síntese química , Quinonas/síntese química
4.
J Mater Chem B ; 5(47): 9384-9394, 2017 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-32264541

RESUMO

Porous biomedical implants hold great potential in preventing stress shielding while improving bone osseointegration and regeneration. In this paper, a novel approach is introduced to control the porosity of 316L stainless steel implants by using canister-free hot isostatic pressing (CF-HIPing). The proposed approach uses cold isostatic pressing (CIPing) to generate powder compacts with various particle sizes, followed by CF-HIPing. 316L stainless steel samples with controlled porosity, and mechanical and biological properties were successfully achieved. The results showed a significant increase in the samples' porosity with increasing powder size. Porous structures with a strength of 108-360 MPa, Vickers hardness of 25-49 HV and elastic modulus between 17 and 50 GPa were produced using a particle size range of 5-50 µm. The effect of samples with various porosities on the in vitro response of mouse pre-osteoblastic cells in terms of toxicity and proliferation was studied. All samples showed that they had a minimal toxic effect on the osteoblasts. Samples with low porosity, prepared using a particle size of 5 µm, were believed to hinder the transport of nutrients and oxygen to the cells and hence had lower proliferation. In addition, samples prepared using a particle size range of 16-50 µm were associated with an increased proliferation and are therefore expected to improve the rate of bone osseointegration.

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