Safety and Tolerability of Topical Ophthalmic Triamcinolone Acetonide-Loaded Liposomes Formulation and Evaluation of Its Biologic Activity in Patients with Diabetic Macular Edema.

Intravitreal injections (IVTs) of corticosteroids as triamcinolone acetonide (TA) are frequently used for the treatment of many vitreous and retinal disorders. However, IVTs are related to severe ocular complications. Lately, a topical ophthalmic TA-loaded liposomes formulation (TALF) was designed to transport TA into the posterior segment of the eye when instilled on the ocular surface. To evaluate the safety, tolerability, and biological activity of TALF, an animal study and a phase I clinical assay were performed. Moreover, four patients with diabetic macular edema (DME) were treated with TALF in order to explore the biological activity of the formulation. No inflammation, lens opacity, swelling, or increase in intraocular pressure were recorded after the instillation of TALF in any of the animal or clinical studies. Mainly, mild and transient adverse events such as dry eye and burning were reported. TALF significantly improves visual acuity and diminishes central foveal thickness in patients with DME. The current data demonstrate the safety, tolerability, and biological activity of TALF. It seems that TALF can be used topically to treat vitreous and retinal diseases that respond to TA such as DME, avoiding the use of corticosteroid IVTs and their associated hazards.

Synthesis and Biological Activity of Hydrazones and Derivatives: A Review.

Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer's, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue, we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and derivatives, making it clear that the synthesis of these molecules can lead to new drug prototypes. Our goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution to the development of potential new drugs for the treatment of various diseases.

Atributos físicos e químicos de agregados pedogênicos e de coprólitos de minhocas em diferentes classes de solos da Paraíba / Physical and chemical attributes of pedogenic aggregates and earthworm casts in different soil classes of Paraíba

A estrutura do solo é constituída de agregados pedogênicos e biogênicos, formados respectivamente pela hierarquização de agregados e pela ação da macrofauna, sobretudo a das minhocas. Neste estudo, objetivou-se a comparação entre agregados do solo (pedogênicos) e coprólitos de minhocas (biogênicos) de diferentes tamanhos e classes de solos. As coletas de amostras indeformadas de solos e coprólitos de minhocas (Pontoscolex corethrurus Muller, 1857) foram realizadas em quatro solos de classes diferentes do Estado da Paraíba (Latossolo Amarelo, Argissolo Vermelho Amarelo, Luvissolo Crômico e Nitossolo Vermelho). As caracterizações físicas e químicas de agregados e coprólitos foram realizadas após secagem à sombra e separação em três classes de diâmetros (20,0 - 9,52; 9,52 - 6,35 e 6,35 - 4,76 mm). A granulometria mostrou ser similar para cada tipo de agregado (pedogênico e biogênico), independentemente do tamanho dos agregados. Em geral, os coprólitos apresentaram maiores proporções de argila, silte e areia fina e menor proporção da fração areia grossa, maior estabilidade e maiores teores de carbono orgânico e cátions trocáveis, comparativamente aos agregados pedogênicos. Os resultados refletem um processo genético peculiar e sugerem a importância dos agregados biogênicos como indicadores da qualidade do solo.

The soil structure is composed by pedogenic and biogenic aggregates, formed respectively by aggregate hierarchy and macrofauna activity, especially by earthworms. The objective of this study was to compare soil aggregates and earthworm casts with different aggregate-size classes and soil classes. The sampling of undisturbed soil and earthworm casts (Pontoscolex corethrurus, Muller, 1857) was made in four soils of different classes in the State of Paraíba (Oxisol, Ultisol, Alfisol and Nitisol). The chemical and physical evaluations of aggregates and earthworm casts were determined after dry and split into three aggregate-size classes (20.0 to 9.52, 9.52 to 6.35 and 6.35 to 4.76 mm). The particle-size distribution was similar to aggregates and earthworm casts, independent of aggregate-size classes. Earthworm casts had higher proportions of clay, silt and fine sand, lower coarse sand, higher physical stability and more organic carbon and cations contents than the pedogenic aggregates. These results show a peculiar genetic process that makes biogenic aggregates an important indicator of soil quality.

Atividade biológica de Solanum lycocarpum (Solanaceae) procedente de regiões fitogeográficas distintas sobre Biomphalaria glabrata (Planorbidae) / Biological activity of Solanum lycocarpum (Solanaceae) coming from different fitogeographic regions in bioassays with Biomphalaria glabrata (Planorbidae)

A esquistossomose mansônica no Brasil constitui-se um grave problema para a saúde pública, o que tem motivado inúmeras pesquisas envolvendo formas alternativas de controle do molusco hospedeiro, Biomphalaria glabrata. O presente estudo teve por objetivos: (1) avaliar o potencial moluscicida de Solanum lycocarpum procedente da Estação Ecológica Pirapitinga, TrêsMarias, MG e do campus Seropédica da Universidade Federal Rural do Rio de Janeiro, RJ através de bioensaios com B. glabrata e (2) verificar efeitos crônicos, nos moluscos sobreviventes, da exposição ao extrato aquoso da planta sobre a reprodução (número de massas ovígeras) e mortalidade. Folhas da planta, após secas a temperatura ambiente, foram picotadas e pesadas para a preparação da infusão a 10%, a partir da qual foram obtidas as concentrações 2,5 e 5%. Os moluscos utilizados nos bioensaios apresentavam 9-13 mm de diâmetro de concha. Os extratos obtidos da planta, na concentração de 10%, determinaram as maiores taxas de mortalidade ao final do bioensaio, 100 e 93,4% respectivamente para as duas localidades de coleta. Sendo dessa forma, comprovada sua ação moluscicida. Decorridos 90 dias de observação, verificou-se a influência dos extratos sobre o parâmetro mortalidade dos moluscos sobreviventes aos bioensaios.(AU)

Schistosomiasis, in Brazil, is a serious problem for the public health, which has motivated numerous studies involving alternative forms of control the host snail, Biomphalaria glabrata. The objectives of the present study were: (1) to evaluate the molluscicidal potential of Solanum lycocarpum coming from the Estação Ecológica de Pirapitinga, Três Marias, Minas Gerais state and from campus Seropédica of the Universidade Federal Rural do Rio de Janeiro, Rio de Janeiro state through bioassays with B. glabrata and (2) to verify chronic effect, in the surviving snails, of the exposition to the aqueous extract of the plant on the reproduction (number the egg mass) and mortality. Leaves of the plant were droughts in ambient temperature, cut and weighed for the infusion preparation 10%, from which concentrations 2.5 and 5% were prepared. The snails used in the bioassays showed 9-13 mm shell diameter. Strong molluscicidal activity was observed, already in first the 24 hours of observation with the 10% concentration, for the plants came from the two analyzed localities. After 90 days of observation the influence of extracts on the parameter mortality of the surviving snails to the bioassays was observed.(AU)

Atividade biológica de Solanum lycocarpum (Solanaceae) procedente de regiões fitogeográficas distintas sobre Biomphalaria glabrata (Planorbidae) / Biological activity of Solanum lycocarpum (Solanaceae) coming from different fitogeographic regions in bioassays with Biomphalaria glabrata (Planorbidae)

A esquistossomose mansônica no Brasil constitui-se um grave problema para a saúde pública, o que tem motivado inúmeras pesquisas envolvendo formas alternativas de controle do molusco hospedeiro, Biomphalaria glabrata. O presente estudo teve por objetivos: (1) avaliar o potencial moluscicida de Solanum lycocarpum procedente da Estação Ecológica Pirapitinga, TrêsMarias, MG e do campus Seropédica da Universidade Federal Rural do Rio de Janeiro, RJ através de bioensaios com B. glabrata e (2) verificar efeitos crônicos, nos moluscos sobreviventes, da exposição ao extrato aquoso da planta sobre a reprodução (número de massas ovígeras) e mortalidade. Folhas da planta, após secas a temperatura ambiente, foram picotadas e pesadas para a preparação da infusão a 10%, a partir da qual foram obtidas as concentrações 2,5 e 5%. Os moluscos utilizados nos bioensaios apresentavam 9-13 mm de diâmetro de concha. Os extratos obtidos da planta, na concentração de 10%, determinaram as maiores taxas de mortalidade ao final do bioensaio, 100 e 93,4% respectivamente para as duas localidades de coleta. Sendo dessa forma, comprovada sua ação moluscicida. Decorridos 90 dias de observação, verificou-se a influência dos extratos sobre o parâmetro mortalidade dos moluscos sobreviventes aos bioensaios.

Schistosomiasis, in Brazil, is a serious problem for the public health, which has motivated numerous studies involving alternative forms of control the host snail, Biomphalaria glabrata. The objectives of the present study were: (1) to evaluate the molluscicidal potential of Solanum lycocarpum coming from the Estação Ecológica de Pirapitinga, Três Marias, Minas Gerais state and from campus Seropédica of the Universidade Federal Rural do Rio de Janeiro, Rio de Janeiro state through bioassays with B. glabrata and (2) to verify chronic effect, in the surviving snails, of the exposition to the aqueous extract of the plant on the reproduction (number the egg mass) and mortality. Leaves of the plant were droughts in ambient temperature, cut and weighed for the infusion preparation 10%, from which concentrations 2.5 and 5% were prepared. The snails used in the bioassays showed 9-13 mm shell diameter. Strong molluscicidal activity was observed, already in first the 24 hours of observation with the 10% concentration, for the plants came from the two analyzed localities. After 90 days of observation the influence of extracts on the parameter mortality of the surviving snails to the bioassays was observed.