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1.
Curr Drug Deliv ; 18(6): 770-778, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33583376

RESUMO

BACKGROUND: Lipid nanocarriers have been widely tested as drug delivery systems to treat diseases due to their bioavailability, controlled release, and low toxicity. For the pulmonary route, the Food and Drug Administration favors the use of substances generally recognized as safe, as well as biodegradable and biocompatible to minimize the possibility of toxicity. Tuberculosis (TB) remains a public health threat worldwide, mainly due to the long treatment duration and adverse effects. Therefore, new drug delivery systems for treating TB are needed. OBJECTIVE: Physicochemical characterization of different lipid-based nanocarriers was used to optimize carrier properties. Optimized systems were incubated with Mycobacterium tuberculosis to assess whether lipid-based systems act as the energy source for the bacteria, which could be counterproductive to therapy. METHODS: Several excipients and surfactants were evaluated to prepare different types of nanocarriers using high-pressure homogenization. RESULTS: A mixture of trimyristin with castor oil was chosen as the lipid matrix after differential scanning calorimetry analysis. A mixture of egg lecithin and PEG-660 stearate was selected as an optimal surfactant system, as this mixture formed the most stable formulations. Three types of lipid nanocarriers, solid lipid nanoparticles, nanostructured lipid carriers (NLC), and nanoemulsions, were prepared, with the NLC systems showing the most suitable properties for further evaluation. It may provide the advantages of increasing the entrapment efficiency, drug release, and the ability to be lyophilized, producing powder for pulmonary administration as an alternative to entrap poor water-soluble molecules. CONCLUSION: Furthermore, the NLC system can be considered for use as a platform for the treatment of TB through the pulmonary route.


Assuntos
Portadores de Fármacos , Nanopartículas , Tuberculose , Excipientes , Humanos , Lipídeos , Tamanho da Partícula , Tuberculose/tratamento farmacológico
2.
Assay Drug Dev Technol ; 18(7): 298-307, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-33054379

RESUMO

Tuberculosis (TB) remains a major global health problem. Conventional treatments fail either because of poor patient compliance with the drug regimen or due to the emergence of multidrug-resistant TB. Thus, not only has the discovery of new compounds and new therapeutic strategies been the focus of many types of research but also new routes of administration. Pulmonary drug delivery possesses many advantages, including the noninvasive route of administration, low metabolic activity, and control environment for systemic absorption, and avoids first-pass metabolism. The use of lipid nanocarriers provides several advantages such as protection of the compound's degradation, increased bioavailability, and controlled drug release. In this study, we review some points related to how the use of lipid nanocarriers can improve TB treatment with inhaled nanomedicines. This review also discusses the current approaches and formulations developed to achieve optimal pulmonary drug delivery systems with nanocarriers targeting alveolar macrophages.


Assuntos
Antituberculosos/uso terapêutico , Lipídeos/química , Nanopartículas/química , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico , Administração por Inalação , Antituberculosos/administração & dosagem , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Humanos , Macrófagos Alveolares/efeitos dos fármacos , Macrófagos Alveolares/metabolismo , Tuberculose Resistente a Múltiplos Medicamentos/metabolismo
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