RESUMO
OBJECTIVES: The major objective is to target diethylcarbamazine citrate (DEC) to the lymphatics and to increase its retention time. The effect of various excipients on the physicochemical characteristics of the nanoparticles was also studied. MATERIALS AND METHODS: Solid lipid nanoparticles (SLNs) of DEC were prepared by ultrasonication by varying the concentrations of compritol 888 ATO, poloxamer 188 and soya lecithin. The SLNs were evaluated for size, shape, texture, surface charge, physical nature of the entrapped drug, entrapment efficiency and in vitro drug release. In vivo animal studies were carried out to estimate the pharmacokinetic parameters in blood and drug concentration in lymph after oral administration. RESULTS: The size of the spherical particles was in the range of 27.25 ± 3.43 nm to 179 ± 3.08 nm and a maximum entrapment efficiency of 68.63 ± 1.53% was observed. In vitro release studies in pH 7.4 PBS displayed a rapid release and the maximum time taken for the complete drug to release was 150 min. In vivo studies indicated an enhancement in the amount of drug that reached lymphatics when administered via SLNs. CONCLUSION: Targeting of DEC to the lymphatics is possible through SLNs and the retention time in the lymphatics can also be enhanced.
Assuntos
Dietilcarbamazina/administração & dosagem , Sistemas de Liberação de Medicamentos , Excipientes/química , Nanopartículas , Administração Oral , Animais , Dietilcarbamazina/farmacocinética , Portadores de Fármacos/química , Ácidos Graxos/química , Lecitinas/química , Lipídeos/química , Sistema Linfático/metabolismo , Masculino , Tamanho da Partícula , Poloxâmero/química , Ratos , Ratos Sprague-Dawley , Glycine max/química , Fatores de TempoRESUMO
A new microwave-assisted derivatisation and LC-MS/MS method has been developed for the analysis of nitrofuran metabolites - 3-amino-5-morpholino-methyl-1,3-oxa-zolidinone (AMOZ), 3-amino-2-oxazolidinone (AOZ), 1-aminohydantoin (AHD) and semicarbazide (SEM) - in farm-raised prawns (Penaeus monodon) from the coastal regions of South India. Analysis was carried out by reverse-phase column (Phenomenex Luna C18) with gradient elution using mobile phase A (0.02% acetic acid in water) and mobile phase B (0.02% acetic acid in acetonitrile), at a flow rate of 200 µl min(-1) and an injection volume of 20 µl. Microwave-assisted derivatisation was achieved in 6 min with good recovery. The results showed that the samples collected from Andhra Pradesh and Karnataka contained residues of nitrofuran metabolites in the range from 5.0 to 40 ng g(-1). This work emphasises the importance of ensuring the safety of seafood and that a new method of derivatisation is applicable for the analysis of nitrofuran metabolites in seafood.
Assuntos
Antibacterianos/análise , Resíduos de Drogas/análise , Contaminação de Alimentos/análise , Nitrofuranos/análise , Penaeidae/química , Frutos do Mar/análise , Animais , Antibacterianos/efeitos adversos , Antibacterianos/metabolismo , Aquicultura , Resíduos de Drogas/efeitos adversos , Resíduos de Drogas/metabolismo , Índia , Micro-Ondas , Nitrofuranos/efeitos adversos , Nitrofuranos/metabolismo , Penaeidae/metabolismo , Frutos do Mar/efeitos adversos , Espectrometria de Massas em TandemRESUMO
Sulphonamides and chloramphenicol antibiotics were analysed by using liquid chromatography-tandem mass spectrometry (LC-MS/MS) in sea and farmed prawn (Penaeus monodon) samples obtained from the coastal region of southern India during 2011-2012. Average recoveries were 77-99% and precision was between 1% and 8%. The results revealed that in sea prawn samples neither of the two antibiotics was detected, but in farmed samples from coastal Andhra Pradesh some sulphonamides were detected in a concentration range greater than the maximum residual limit as set by Council Directive 2377/90 EC.
