Microcapsules based on alginate and guar gum for co-delivery of hydrophobic antitumor bioactives.

The main goal was the development of a polysaccharide microcapsule for anticancer application based on guar gum and sodium alginate for the controlled release of hesperidin and betulinic acid by spray drying technique. The microcapsule showed an Encapsulation Efficiency of 98.15 ± 0.34 % for hesperidin and 99.76 ± 0.22 % for betulinic acid. In the release study, the Korsmeyer-Peppas mathematical model was identified as the most adequate to explain the observed release mechanism. In vivo tests were performed in zebrafish model, revealing that the microcapsules did not alter the locomotor activity and were not toxic within 96 h by oral administration, suggesting their biological safety. In vitro cytotoxic activity against HL-60 cells confirmed an IC50 value of 2.52 ± 0.23 µg mL-1 in 72 h. Additionally, a decrease in the cytotoxic activity of betulinic acid against L-929 (non-tumor) cells was evidenced. Therefore, the microcapsules synthesized in this work represent a promising formulation for anticancer applications.

Starch-based magnetic nanocomposite for targeted delivery of hydrophilic bioactives as anticancer strategy.

Magnetic nanocomposites were synthesized for the targeted delivery of hydrophilic bioactives through guidance generated by a magnetic field. Superparamagnetic iron oxide nanoparticles (SPIONs) were used to generate hydroxyethyl starch magnetic nanocapsules (HES MNCs). This synthesis allowed the co-encapsulation of oncocalyxone A (onco A) and surface-modified magnetite nanoparticles (Fe3O4@citrate) into the same nanostructure. The synthesized nanocapsules exhibited a core-shell morphology, with an average diameter of 143 nm. This nanocomposite showed potential anticancer activity (IC50) against four human tumor cell lines: glioblastoma SNB-19 (1.010 µgmL-1), colon carcinoma HCT-116 (2.675 µgmL-1), prostate PC3 (4.868 µgmL-1), and leukemia HL-60 (2.166 µgmL-1). Additionally, in vivo toxicity and locomotor activity were evaluated in a zebrafish (Danio rerio) model. The nanocomposite exhibited in vitro cytotoxicity, prolonged drug release profile and also responded to an applied magnetic field, representing a versatile compound with perspectives for highest concentration of different hydrophilic bioactives in a target tissue through magnetic vectorization.

Antibacterial activity of fluoxetine-loaded starch nanocapsules.

This work proposes the development of a starch-based drug carrier for fluoxetine (FLX) delivery and evaluate the improvement of the drug antibacterial activity. The starch nanocapsules were prepared via interfacial polyaddition reaction presenting a core-shell morphology, based on polyurethane linkage, with a particle size in the range 250-300 nm. Furthermore, FLX-loaded nanocapsules were evaluated regarding antibacterial potential against Staphylococcus aureus (ATCC® 6538P ™) and its clinical strains of methicillin-resistant. As expected, the FLX-loaded presented lower minimum inhibitory concentration (MIC) values, in the range of 190-95 µg mL-1, against all isolated microorganisms in comparison to FLX, 255 µg mL-1. According to results, the FLX-loaded starch nanocapsules have successfully improved drug antibacterial activity, generating promising perspectives on the field of the hydrophilic drug delivery systems.

Valor prognóstico da troponina I de alta sensibilidade versus troponina T nas síndromes coronarianas agudas / Prognostic value of high-sensitivity troponin I versus troponin T in acute coronary syndromes

FUNDAMENTO: Apesar da superior precisão diagnóstica das troponinas cardíacas de alta sensibilidade, seu valor prognóstico ainda não foi validado contra troponinas cardíacas convencionais. OBJETIVO: Testar o valor prognóstico da troponina I de alta sensibilidade (TnI-as) em comparação com a troponina T convencional (TnT-c) no cenário de síndromes coronarianas agudas sem supradesnivelamento do segmento ST (SCA). MÉTODOS: No momento da admissão, uma amostra de plasma foi coletada de 103 pacientes consecutivos com angina instável ou infarto agudo do miocárdio sem supradesnivelamento do segmento ST. Nessa amostra, a troponina foi medida tanto pelo método TnI-as quanto pelo método TnT-c. O valor prognóstico das duas troponinas foi comparado em relação à ocorrência de evento cardiovascular maior, definido como o composto de morte, infarto agudo do miocárdio não fatal ou angina instável refratária durante a internação. RESULTADOS: Durante uma hospitalização mediana de 8 dias (intervalo interquartil = 5-11), a incidência de eventos cardiovasculares foi 10% (5 mortes, 3 infartos não fatais e 2 anginas refratárias não fatais). Troponina I de alta sensibilidade predisse significativamente eventos cardiovasculares, com C-estatísticas de 0,73 (95% CI = 0,59-0,87), à semelhança da TnT-c (0,70; 95% CI = 0,55-0,84) - P = 0,75. A definição de troponina positiva que proporcionou melhor acurácia prognóstica foi TnI-as > 0,055 mg / L e TnT-c > 0,010 mg / L, com sensibilidade de 90% e especificidade de 52% para ambos os ensaios. CONCLUSÃO: Troponina I de alta sensibilidade prediz eventos cardiovasculares de forma semelhante à troponina T convencional no cenário de SCA. (Arq Bras Cardiol. 2012; [online].ahead print, PP.0-0).

BACKGROUND: Despite superior diagnostic accuracy of high-sensitivity cardiac troponins, their prognostic value has not been validated against conventional cardiac troponins. OBJECTIVE: To test the prognostic value of high-sensitivity cardiac troponin I (hs-cTnI), compared with conventional cardiac troponin T (cTnT) in the setting of non-ST elevation acute coronary syndromes. METHODS: At hospital admission, a plasma sample was collected from 103 consecutive patients with unstable angina or non-ST elevation acute myocardial infarction. In this sample, troponin was measured both by hs-cTnI and cTnT methods. Their prognostic value was compared as to the occurrence of major cardiovascular events, defined as a combination of death, nonfatal acute myocardial infarction or refractory unstable angina during hospitalization. RESULTS: During median hospitalization of 8 days (interquartile range = 5 - 11), the incidence of cardiovascular events was 10% (5 deaths, 3 non-fatal myocardial infarctions and 2 non-fatal refractory anginas). High-sensitivity troponin I significantly predicted cardiovascular events, with a C-statistics of 0.73 (95% CI = 0.59 - 0.87), similarly to cTnT (0.70; 95% CI = 0.55 - 0.84) - P = 0.75. The definition of positive cardiac marker that provided the best prognostic accuracy was hs-cTnI > 0.055 µg/L and cTnT > 0.010 µg/L, with equal sensitivity of 90% and specificity of 52% for both assays. Positive hs-cTnI was associated with 17% incidence of events, compared with 2% in patients with negative hs-cTnI (P = 0.02). CONCLUSION: High-sensitivity troponin I predicts cardiovascular events similarly to conventional troponin T in the setting of non-ST-elevation ACS. (Arq Bras Cardiol. 2012; [online].ahead print, PP.0-0).

Prognostic value of high-sensitivity troponin I versus troponin T in acute coronary syndromes.

BACKGROUND: Despite superior diagnostic accuracy of high-sensitivity cardiac troponins, their prognostic value has not been validated against conventional cardiac troponins. OBJECTIVE: To test the prognostic value of high-sensitivity cardiac troponin I (hs-cTnI), compared with conventional cardiac troponin T (cTnT) in the setting of non-ST elevation acute coronary syndromes. METHODS: At hospital admission, a plasma sample was collected from 103 consecutive patients with unstable angina or non-ST elevation acute myocardial infarction. In this sample, troponin was measured both by hs-cTnI and cTnT methods. Their prognostic value was compared as to the occurrence of major cardiovascular events, defined as a combination of death, nonfatal acute myocardial infarction or refractory unstable angina during hospitalization. RESULTS: During median hospitalization of 8 days (interquartile range = 5 - 11), the incidence of cardiovascular events was 10% (5 deaths, 3 non-fatal myocardial infarctions and 2 non-fatal refractory anginas). High-sensitivity troponin I significantly predicted cardiovascular events, with a C-statistics of 0.73 (95% CI = 0.59 - 0.87), similarly to cTnT (0.70; 95% CI = 0.55 - 0.84) - P = 0.75. The definition of positive cardiac marker that provided the best prognostic accuracy was hs-cTnI > 0.055 µg/L and cTnT > 0.010 µg/L, with equal sensitivity of 90% and specificity of 52% for both assays. Positive hs-cTnI was associated with 17% incidence of events, compared with 2% in patients with negative hs-cTnI (P = 0.02). CONCLUSION: High-sensitivity troponin I predicts cardiovascular events similarly to conventional troponin T in the setting of non-ST-elevation ACS.