Potential of propolis antifungal activity for clinical applications.

The high incidence of skin diseases of microbial origin along with the widespread increase of microbial resistance demand for therapeutic alternatives. Research on natural compounds has been opening new perspectives for the development of new therapies with health-positive impacts. Propolis, a resinous mixture produced by honeybees from plant exudates, is widely used as a natural medicine since ancient times, mainly due to its antimicrobial properties. More recently, antioxidant, anti-tumour, anti-inflammatory, hepatoprotective and immunomodulatory activities were also reported for this natural product, highlighting its high potential pharmacological interest. In the present work, an extensive review of the main fungi causing skin diseases as well as the effects of natural compounds, particularly propolis, against such disease-causing micro-organisms was organized and compiled in concise handy tables. This information allows to conclude that propolis is a highly effective antimicrobial agent suggesting that it could be used as an alternative skin treatment against pathogenic micro-organisms and also as a cosmeceutical component or as a source of bioactive ingredients.

Poloxamer 407 based-nanoparticles for controlled release of methotrexate.

Poloxamer 407 (P407)-based nanoparticles were produced by the high pressure homogenization method for the encapsulation and delivery of methotrexate (MTX), aiming intravenous therapeutic applications. The surface of these nanoparticles was functionalized by conjugation of P407 with folic acid (FA) or with MTX, which served as targeting ligand agents. MTX-P407 conjugate was also developed to increase the final drug cargo. Two hydrophobic derivatives of MTX, MTX di-ethylated ester (MTX-OEt) and the ionic complex MTX-dimethyldioctadecylammonium bromide (MTX-DODAB) were produced and entrapped onto P407-based nanoparticles. All formulations developed revealed a monodisperse character comprising small and narrow nanoparticles (<100 nm). P407 nanoparticles (functionalized with FA) and MTX-P407 nanoparticles, both loaded with MTX-OEt, demonstrated a slow drug release profile. The effect of lipase from Aspergillus oryzae on the hydrolysis of the linkage between the P407 and MTX, and consequent MTX release profile, was also evaluated. We observed a controlled and slow release of MTX (<50% of release after 11 days) in the presence of enzyme. These MTX-P407 nanoparticles loaded with MTX-OEt induced a great effect against Caco-2 cancer cells (≈40% of cell death after 72 h of incubation), demonstrating higher efficiency than the free MTX at the same concentration.

PTS micelles for the delivery of hydrophobic methotrexate.

Polyoxyethanyl-α-tocopheryl sebacate (PTS) is an amphiphilic compound with self-emulsifying properties known to form micelles. In this work, we report the production of PTS micelles for the encapsulation and delivery of a hydrophobic derivative of methotrexate, MTX di-ethylated (MTX-OEt). We optimized the micelles production by testing two different techniques: auxiliary solvent and sonication. Small and homogeneous micelles (≈40 nm) were obtained through the auxiliary solvent method performed at 30 °C and using 15 mg/mL of PTS. The produced micelles with the most promising physicochemical properties did not induce cytotoxicity when tested in normal human cells (BJ5ta cells), being considered for the encapsulation of MTX-OEt. This prodrug was achieved by Fisher esterification using ethanol, being isolated in good yield (η = 68%). MTX-OEt was efficiently encapsulated onto the produced micelles which preserved their physicochemical properties. The PTS micelles loaded with MTX-OEt, free MTX-OEt and free unmodified MTX revealed similar biological effect against cancer cells (Caco-2 cells). These results demonstrated that the biological activity of MTX is not altered after modification. The developed PTS micelles revealed a promising intracellular delivery performance with potentiality for cancer therapy.

Outcomes of phacoemulsification in patients with uveitis at a tertiary center in São Paulo, Brazil: a review of cases from 2007 to 2012.

PURPOSE:: To evaluate the outcomes of phacoemulsification with intraocular lens (IOL) implantation in eyes with uveitis. METHODS:: Consecutive patients with uveitis and cataracts who had phacoemulsification and acrylic IOL implantation during 2007-2012 were evaluated for visual outcomes, etiology, and complications. Inflammation was controlled for at least 3 months before surgery, and oral prednisone (0.5 mg/kg/day) was administered to patients with non-infectious uveitis. RESULTS:: This study investigated 45 eyes in 38 patients with a mean age of 52 ± 12.5 years. The most common etiologies among non-infectious causes (n=32; 73.3%) were Vogt-Koyanagi-Harada disease (n=9), Fuchs heterochromic iridocyclitis (n=4), and sympathetic ophthalmia (n=3). Four cases were idiopathic. Among infectious cases (n=13; 28.9%), the most common causes were toxoplasmosis (n=6) and presumed ocular tuberculosis (n=4). An acrylic IOL was implanted in-the-bag in all cases. After 1-year follow-up, an improvement in visual acuity of two or more lines was observed in 38 eyes (84.4%), and 28 eyes (62.2%) achieved a postoperative visual acuity of ≥0.5. Posterior capsule opacification was observed in 10 eyes (22.2%). Persistent postoperative inflammation (of >6 months) was observed in seven eyes (15.5%) and recurrence occurred in four eyes (8.8%). IOL was explanted in one eye. Intraocular hypertension was observed in six eyes (13.3%). CONCLUSIONS:: Phacoemulsification with IOL implantation improved vision in most patients with coexisting cataracts and uveitis. Good preoperative and postoperative control of inflammation plays an important role in achieving favorable visual outcomes. Furthermore, the final visual outcome depends on the posterior segment status.

Outcomes of phacoemulsification in patients with uveitis at a tertiary center in São Paulo, Brazil: a review of cases from 2007 to 2012 / Resultado da facoemulsificação em pacientes com uveíte em um centro terciário em São Paulo, Brasil: revisão de casos de 2007 a 2012

ABSTRACT Purpose: To evaluate the outcomes of phacoemulsification with intraocular lens (IOL) implantation in eyes with uveitis. Methods: Consecutive patients with uveitis and cataracts who had phacoemulsification and acrylic IOL implantation during 2007-2012 were evaluated for visual outcomes, etiology, and complications. Inflammation was controlled for at least 3 months before surgery, and oral prednisone (0.5 mg/kg/day) was administered to patients with non-infectious uveitis. Results: This study investigated 45 eyes in 38 patients with a mean age of 52 ± 12.5 years. The most common etiologies among non-infectious causes (n=32; 73.3%) were Vogt-Koyanagi-Harada disease (n=9), Fuchs heterochromic iridocyclitis (n=4), and sympathetic ophthalmia (n=3). Four cases were idiopathic. Among infectious cases (n=13; 28.9%), the most common causes were toxoplasmosis (n=6) and presumed ocular tuberculosis (n=4). An acrylic IOL was implanted in-the-bag in all cases. After 1-year follow-up, an improvement in visual acuity of two or more lines was observed in 38 eyes (84.4%), and 28 eyes (62.2%) achieved a postoperative visual acuity of ≥0.5. Posterior capsule opacification was observed in 10 eyes (22.2%). Persistent postoperative inflammation (of >6 months) was observed in seven eyes (15.5%) and recurrence occurred in four eyes (8.8%). IOL was explanted in one eye. Intraocular hypertension was observed in six eyes (13.3%). Conclusions: Phacoemulsification with IOL implantation improved vision in most patients with coexisting cataracts and uveitis. Good preoperative and postoperative control of inflammation plays an important role in achieving favorable visual outcomes. Furthermore, the final visual outcome depends on the posterior segment status.

RESUMO Objetivos: Avaliar os resultados da facoemulsificação com implante de lente intraocular em olhos com uveíte. Métodos: Foram incluídos pacientes consecutivos com catarata e uveíte, submetidos a facoemulsificação com implante de lente intraocular acrílica no período de 2007 a 2012, onde avaliou-se resultados visuais, etiologia e complicações. A inflamação estava quiescente por pelo menos três meses e foi usado prednisona oral (0,5 mg/kg/dia) em pacientes com uveíte não infecciosa. Resultados: Este estudo incluiu 45 olhos de 38 pacientes com idade media de 52±12.5 anos. As etiologias mais frequentes, entre as causas não-infecciosas (n=32; 73,3%), foram doença de Vogt-Koyanagi-Harada (n=9), idiopáticas (n=4), iridociclite heterocrômica de Fuchs (n=4) e oftalmia simpática (n=3). Entre as causas infecciosas (n=13; 28,9%), as mais frequentes foram toxoplamose (n=6) e tuberculose ocular presumida (n=4). Uma lente de acrílico foi implantada no saco capsular em todos os casos. Com um ano de seguimento, 38 olhos (84,4%) melhoraram 2 ou mais linhas; 28 olhos (62,2%) atingiram uma acuidade visual pós-operatória de 0,5 ou melhor. Opacidade de cápsula posterior foi observada em 10 olhos (22,2%). Inflamação pós-operatória persistente (>6 meses) foi observada em 7 olhos (15,5%) e a recorrência ocorreu em 4 olhos (8,8%). Houve necessidade de explante da lente em um olho. Hipertensão intraocular foi observada em 6 olhos (13,3%). Conclusões: Facoemulsificação com implante de lente intraocular melhorou a visão na maioria dos pacientes com catarata e uveíte. O controle adequado pré e pós-operatório da inflamação desempenha um papel reconhecidamente importante para obtenção de bons resultados visuais. O resultado visual final depende de alterações prévias do segmento posterior.