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Int J Mol Sci ; 22(12)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200719


The potential of bacterial cellulose as a carrier for the transport of ibuprofen (a typical example of non-steroidal anti-inflammatory drugs) through the skin was investigated. Ibuprofen and its amino acid ester salts-loaded BC membranes were prepared through a simple methodology and characterized in terms of structure and morphology. Two salts of amino acid isopropyl esters were used in the research, namely L-valine isopropyl ester ibuprofenate ([ValOiPr][IBU]) and L-leucine isopropyl ester ibuprofenate ([LeuOiPr][IBU]). [LeuOiPr][IBU] is a new compound; therefore, it has been fully characterized and its identity confirmed. For all membranes obtained the surface morphology, tensile mechanical properties, active compound dissolution assays, and permeation and skin accumulation studies of API (active pharmaceutical ingredient) were determined. The obtained membranes were very homogeneous. In vitro diffusion studies with Franz cells were conducted using pig epidermal membranes, and showed that the incorporation of ibuprofen in BC membranes provided lower permeation rates to those obtained with amino acids ester salts of ibuprofen. This release profile together with the ease of application and the simple preparation and assembly of the drug-loaded membranes indicates the enormous potentialities of using BC membranes for transdermal application of ibuprofen in the form of amino acid ester salts.

Aminoácidos/química , Anti-Inflamatórios não Esteroides/farmacologia , Celulose/química , Ésteres/química , Ibuprofeno/farmacologia , Absorção Cutânea/efeitos dos fármacos , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Bactérias/metabolismo , Sistemas de Liberação de Medicamentos , Ibuprofeno/administração & dosagem , Ibuprofeno/química , Suínos
Molecules ; 25(1)2019 Dec 25.
Artigo em Inglês | MEDLINE | ID: mdl-31881750


The development of ionic liquids based on active pharmaceutical ingredients (API-ILs) is a possible solution to some of the problems of solid and/or hydrophobic drugs such as low solubility and bioavailability, polymorphism and an alternative route of administration could be suggested as compared to the classical drug. Here, we report for the first time the synthesis and detailed characterization of a series of ILs containing a cation amino acid esters and anion ketoprofen (KETO-ILs). The affinity and the binding mode of the KETO-ILs to bovine serum albumin (BSA) were assessed using fluorescence spectroscopy. All compounds bind in a distance not longer than 6.14 nm to the BSA fluorophores. The estimated binding constants (KA) are in order of 105 L mol-1, which is indicative of strong drug or IL-BSA interactions. With respect to the ketoprofen-BSA system, a stronger affinity of the ILs containing l-LeuOEt, l-ValOBu, and l-ValOEt cation towards BSA is clearly seen. Fourier transformed infrared spectroscopy experiments have shown that all studied compounds induced a rearrangement of the protein molecule upon binding, which is consistent with the suggested static mechanism of BSA fluorescence quenching and formation of complexes between BSA and the drugs. All tested compounds were safe for macrophages.

Líquidos Iônicos/síntese química , Líquidos Iônicos/metabolismo , Cetoprofeno/síntese química , Soroalbumina Bovina/metabolismo , Animais , Bovinos , Morte Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ésteres/síntese química , Ésteres/química , Transferência Ressonante de Energia de Fluorescência , Líquidos Iônicos/química , Líquidos Iônicos/toxicidade , Cetoprofeno/química , Cetoprofeno/toxicidade , Cinética , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Secundária de Proteína , Células RAW 264.7 , Soroalbumina Bovina/química , Solubilidade , Solventes/química , Água/química
Orthopedics ; 30(10 Suppl): S144-7, 2007 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17983118


In this study, we present a new 2.5-dimensional ultrasonic navigation system for measuring axes, lengths, and torsions preoperatively, intraoperatively, and postoperatively. The system comprises an ultrasound unit with a 5-MHz linear probe (TELEMED Echoblaster 128; Telemed, Vilnius, Lithuania) and a navigation system (OrthoPilot; B. Braun Aesculap, Tuttlingen, Germany) with a Polaris camera (Northern Digital, Waterloo, Canada). Specialized software developed for this application allows for selecting any body region on a virtual 3D skeleton. With a virtual ultrasound probe, planes needed for measurements can be defined. For each section, the respective surface contour of the bone, which is also shown in the ultrasound image, is displayed. Alternatively, the clinician can use established standard sections. Finally, the required length, axes, and torsions are defined. The accuracy and precision of the system were tested using a plastic model. The measurements of length, torsion, and axis values were accurate to -0.1 +/- 0.3 mm (95% CI), 0.1 degree +/- 0.2 degree (95% CI), and 0.0 degree +/- 0.006 degree (95% CI), respectively. The precision variances for length, torsion, and axis were 1.17 mm (standard deviation) and 0.94 degree and 0.66 degree. These results suggest that the new sonographic method is more accurate than conventional radiographic techniques.

Artroplastia de Quadril/métodos , Osteoartrite do Quadril/diagnóstico por imagem , Cirurgia Assistida por Computador/métodos , Ultrassonografia/instrumentação , Desenho de Equipamento , Humanos , Processamento de Imagem Assistida por Computador/instrumentação , Osteoartrite do Quadril/cirurgia , Reprodutibilidade dos Testes