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1.
J Vis Exp ; (185)2022 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-35969097

RESUMO

The low aqueous solubility of many drugs reduces their bioavailability in the blood. Oils have been used for centuries to enhance the solubility of drugs; however, they can disturb the lipid profile of the patients. In this study, self-nanoemulsifying drug delivery systems of omega-3 fatty acids-rich oils are prepared and optimized for the delivery of lipophilic drugs. Rosuvastatin, a potent hypolipidemic drug, was used as a model lipophilic drug. Fish oil showed more than 7-fold higher solubility of rosuvastatin than other oils and therefore it was selected for the development of self-nanoemulsifying drug delivery systems (SNEDDS). Different combinations of surfactants and co-surfactants were screened and a surfactant mixture of Tween 80 (surfactant) and Capryol PGMC (cosurfactant) were selected for compatibility with fish oil and rosuvastatin. A pseudoternary phase diagram of oil, surfactant, and co-surfactant was designed to identify the emulsion region. The pseudoternary phase diagram predicted a 1:3 oil and surfactant mixture as the most stable ratio for the emulsion system. Then, a response-surface methodology (Box-Behnken design) was applied to calculate the optimal composition. After 17 runs, fish oil, Tween 80, and Capryol PGMC in proportions of 0.399, 0.67, and 0.17, respectively, were selected as the optimized formulation. The self-nanoemulsifying drug delivery systems showed excellent emulsification potential, robustness, stability, and drug release characteristics. In the drug release studies, SNEDDS released 100% of the payload in around 6 h whereas, release of the plain drug was less than 70% even after 12 h. Therefore, omega-3 fatty acids-rich healthy lipids have enormous potential to enhance the solubility of lipophilic drugs whereas, self-emulsification can be used as a simple and feasible approach to exploit this potential.


Assuntos
Ácidos Graxos Ômega-3 , Nanopartículas , Administração Oral , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos/métodos , Emulsões , Óleos de Peixe , Tamanho da Partícula , Polissorbatos , Rosuvastatina Cálcica , Solubilidade , Tensoativos
2.
BMJ Open Respir Res ; 7(1)2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-33199402

RESUMO

OBJECTIVE: To study the frequency of venous thromboembolism in hospitalised patients with COVID-19 and correlation with the D-dimers and thromboprophylaxis. DESIGN: Cross-sectional descriptive study. PLACE AND DURATION OF STUDY: Queen Elizabeth Hospital, 20 April 2020-13 May 2020. PATIENTS AND METHODS: One hundred and seven (n=107) patients of PCR-confirmed COVID-19 pneumonia admitted to Queen Elizabeth Hospital, Birmingham, between 20 April 2020 and 13 May 2020 were included in the study using consecutive sampling. Data were collected using the Excel audit tool and included age, gender, weight, estimated eGFR, D-dimer values on admission, intensive care unit admission, presence of respiratory failure, imaging results for evaluation of venous thromboembolism (VTE) and anticoagulation received on admission. The data were entered in the SPSS (V.17) and were analysed. Data were summarised as means±SD, number or percentage as appropriate. A p value of less than 0.05 was considered significant. RESULTS: The frequency of VTE was found to be 11.2% in patients hospitalised with COVID-19 pneumonia. The mean D-dimers were 3322.24 ng/mL±9603 ng/mL with the values significantly higher for patients with VTE and those requiring intensive care unit admission. All of the seven patients (100%) with D-dimers value above 2000 ng/mL who underwent imaging were found to have VTE. CONCLUSION: VTE is frequent in patients with COVID-19 pneumonia despite anticoagulation. A higher D-dimers value correlates well with the risk of VTE in these patients and further evaluation of such patients for VTE is necessary especially with D-dimers values above 2000 ng/mL.


Assuntos
COVID-19/epidemiologia , COVID-19/metabolismo , Produtos de Degradação da Fibrina e do Fibrinogênio/metabolismo , SARS-CoV-2/metabolismo , Tromboembolia Venosa/epidemiologia , Tromboembolia Venosa/metabolismo , Idoso , Comorbidade , Estudos Transversais , Feminino , Humanos , Masculino , Estudos Retrospectivos , Reino Unido/epidemiologia
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