The exchange of lipids with cells and other lipoproteins is a crucial process in HDL metabolism and for HDL antiatherogenic function. Here, we tested a practical method to quantify the simultaneous transfer to HDL of phospholipids, free-cholesterol, esterified cholesterol and triacylglycerols and to verify the lipid transfer in patients with coronary artery disease (CAD) or undergoing statin treatment. Twenty-eight control subjects without CAD, 27 with CAD and 25 CAD patients under simvastatin treatment were studied. Plasma samples were incubated with a donor nanoemulsion prepared by ultrasonication of the constituent lipids and labeled with radioactive lipids; % lipids transferred to HDL were quantified in the HDL-containing supernatant after chemical precipitation of non-HDL fractions and the nanoemulsion. The assay was precise and reproducible. Increase of temperature (4-37 degrees C), of incubation period (5 min to 2 h), of HDL-cholesterol concentration (33-244 mg/dL) and of mass of nanoemulsion lipids (0.075-0.3 mg/microL) resulted in increased lipid transfer from the nanoemulsion to HDL. In contrast, increasing pH (6.5-8.5) and albumin concentration (3.5-7.0 g/dL) did not affect lipid transfer. There was no difference between CAD and control non-CAD with regard to the lipid transfer, but statin treatment reduced the transfer to HDL of all four lipids. The test herein described is a valid and practical tool for exploring an important aspect of HDL metabolism.
A cholesterol-rich microemulsion (LDE) that binds to low-density lipoprotein (LDL) receptors is selectively taken up by malignant cells that overexpress those receptors and may be used as vehicle for antineoplastic agents. This study aimed to develop the association of etoposide with LDE. It was firstly observed that etoposide poorly associates with the microemulsion, therefore the experiments were performed with a lipophilic fatty acid derivative of the drug. The association of etoposide oleate with LDE was almost 100% and was tested for physical and chemical stability, as well as for cellular uptake, toxicity in mice and cytotoxic activity against a neoplastic cell line (NCI-H292). Uptake and cytotoxic activity of LDE-etoposide oleate by NCI-H292 cells was mediated by LDL receptors. The anti-proliferative activity of LDE-etoposide oleate against the neoplastic cells was smaller than that of etoposide oleate (IC50 (drug concentration required to inhibit 50% of the cell growth) = 0.48 and 0.19 mM, respectively). This difference, however, can be ascribed to the activity of the commercially used vehicle and not the drug itself because when this vehicle was added to the cultures with LDE-etoposide oleate, the IC50 decreased. On the other hand, the tolerability of LDE-etoposide oleate to mice was remarkable, such that its lethal dose (LD50) was about five-fold that of the commercial formulation (LD50 = 315 and 58 mg kg(-1), respectively). In conclusion, LDE-etoposide oleate association is stable and the cytostatic activity of the drug is preserved while its toxicity to animals is small. By diminishing the side effects and directing etoposide to neoplastic tissues, LDE may be regarded as an advance in chemotherapy with this drug.
A cholesterol-rich nanoemulsion (LDE) may be used as a vehicle to target antineoplastic drugs against cancer cells. The association of an etoposide derivative to LDE is stable and retains the cytotoxic activity of etoposide. We have evaluated the toxicity and antitumoral action of this new preparation in-vivo. Melanoma-bearing mice and control mice were administered LDE-etoposide oleate or commercial etoposide, either with or without radioactive labelling. The maximum tolerated dose (MTD), tissue distribution, plasma decay curves, pharmacokinetic parameters and antitumoral activity were determined. Association to LDE drastically reduced the drug toxicity, since MTD was approximately five-fold greater than in commercial etoposide. LDE-etoposide oleate was concentrated four-fold in the tumour compared with the normal adjacent tissues, was removed faster from plasma in tumour-bearing mice than in controls, and remained in the bloodstream longer than commercial etoposide. The tumour growth inhibition rate and survival were greater in animals treated with LDE-etoposide oleate compared with commercial etoposide. However, increasing the dose from 17 to 85 M kg À1 did not result in further improvement of the antitumour action. The incorporation of etoposide oleate to LDE resulted in markedly reduced toxicity and superior antitumoral activity. LDE-etoposide oleate is a promising new weapon for cancer treatment.
The pharmacist, through pharmaceutical care, may follow the pharmacotherapy, guiding and intervening when necessary, seeking improvements in health education and quality of life of the patient. The aim of this study was to review literature on the importance of pharmaceutical care to identify and solve drug-nutrient interactions, highlighting the implications of these interactions in the therapeutic effect of the drug or nutritional status. The research was conducted in books and scientific papers in databases such as Science Direct, Pubmed and Scielo between 2000 and 2014. The results showed numerous possibilities for drug-nutrient interactions, which can interfere with the effect of the drug and/or the nutritional state of the patient. Such interactions are often not identified, because the lack of knowledge of health professionals about the theme or due to the fasting requirement for bioavailability tests of drugs. Thus, the pharmacist, through pharmaceutical care and its extensive knowledge, may collaborate, reducing the risk of drug-nutrient interactions, increasing the patient's confidence and essence of the profession.Keywords: pharmaceutical care; food-drug interaction; patient care RESUMO O farmacêutico, por meio da atenção farmacêutica, pode acompanhar a farmacoterapia, orientando e intervindo quando necessário, buscando melhoria na educação em saúde e na qualidade de vida do paciente. O objetivo deste trabalho foi realizar uma revisão bibliográfica sobre a importância da atenção farmacêutica na identificação e resolução das interações fármaco-nutriente, evidenciando as implicações dessas interações no efeito terapêutico do fármaco ou no estado nutricional. Foram realizadas pesquisas em livros e artigos científicos em bases de dados como Science Direct, Pubmed e Scielo, no período de 2000 a 2014. Os resultados mostraram que existem inúmeras possibilidades de interações fármaco-nutriente, as quais podem causar prejuízos ao efeito do fármaco e/ou ao estado nutricional do paciente, e essas muitas vezes não são identificadas, por falta de conhecimento dos profissionais da saúde ou devido aos testes de biodisponibilidade dos medicamentos serem realizados em jejum, por exigência dos órgãos sanitários. Desse modo, vê-se a necessidade da atuação do farmacêutico, que por meio do seu amplo conhecimento, pode colaborar com a diminuição dos riscos dessas interações fármaco-nutriente e nutriente-fármaco, resgatando assim a confiança do paciente e a essência da profissão.Palavras Chave: atenção farmacêutica; interações alimento-fármaco; assistência ao paciente.
Objective: Analyzing studies related to Adverse Drug Events (ADE) in hospitalized patients in Brazil. Method: integrative review, for which the National Library of Medicine (PubMed), Biblioteca Virtual de Saúde (BVS), Repository of the Fundação Oswaldo Cruz (FIOCRUZ) and Capes Journals databases were selected for searching the studies primary, with the descriptors: Patient Safety, Drug-related side effects and adverse reactions, Patient harm, Hospitalization, Inpatients. Results: Twenty articles were identified, 50% (10) were from the southeast region of Brazil. Regarding the methodology adopted to identify the ADEs, 70% (14) used the retrospective data review. The trackers were used in 5 (25%) articles, 3 of which used the triggers proposed by the Institute for Healthcare Improvement, and the other 2 the trackers used were proposed by the researchers themselves. The number of adverse drug reactions ranged from 12 to 96, while the occurrence of AE ranged from 4 to 122. In one study 50% (41) of participants had at least one adverse drug event. Conclusion: There is great variability in scientific production in Brazil, and in the occurrence of Adverse Drug Events as well. There is a need for strategies to identify these events and create strategies to promote patient safety.
Objetivo: Investigar evidências sobre tipos de intervenções, dando ênfase às intervenções farmacêuticas, e seus respectivos desfechos clínicos, epidemiológicos, de acesso, humanístico e econômicos em portadores de HIV/Aids em atendimento de média complexidade. Métodos: Revisão sistemática com estratégia de busca nos estudos publicados nas bases Cochrane Library, Epistemonikos, Health Evidence, Health Systems Evidence, Biblioteca Virtual de Saúde e Google Scholar; incluindo Medical Subject Headings (MeSH) e Descritores em Ciências da Saúde (DeCS), incluindo os domínios “Pharmaceutical attention”, “Pharmaceutical Care”, “Pharmaceutical Interventions”, “Pharmaceutical Services”, “HIV/AIDS”, “Medium Complexity Attention” e “Medium Complexity Care”, sendo adaptada para as distintas bases eletrônicas, utilizando-se dos operadores booleanos OR e AND. Resultados: Há evidências de que as intervenções farmacêuticas profissionais, financeiras, governamentais e multifacetadas, melhoram os desfechos clínicos, epidemiológicos, de acesso e equidade, humanístico e econômicos em portadores de HIV/Aids em atendimento de média complexidade. Considerações finais: Diversas intervenções farmacêuticas ao portador de HIV/Aids se mostraram importantes na melhora de desfechos clínicos, epidemiológicos, humanísticos e de acesso e equidade, tendo assim o cuidado farmacêutico se mostrado importante para fortalecer as estratégias do uso racional de medicamentos e promovendo a melhoria da qualidade de vida do paciente.
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