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1.
J Microencapsul ; 37(2): 160-169, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31916886

RESUMO

The aim of this study was to develop levosulpiride-loaded solid lipid nanoparticles (SLNs) with enhanced solubilisation and bioavailability. The levosulpiride loaded-SLNs were composed of levosulpiride, stearic acid, and tween 80 in their respective weight ratios of (1, 5, and 1.5 mg) dissolved in 1 ml distilled water. Physicochemical properties of the SLNs such as particle size, shape, crystallinity, and chemical interaction were evaluated. Further, the in vitro drug dissolution, pharmacokinetic and stability studies of the SLNs were performed. The SLNs were rounded shaped stable nanoparticles with average diameter of 200 nm. They demonstrate 1.5- and 3-fold better drug dissolution when compared with the commercial product and levosulpiride powder, respectively. The SLNs enhanced the bioavailability of levosulpiride 3 times and 7 times, respectively, when compared with the commercial product and levosulpiride powder. It can be concluded that SLNs are capable to improve the dissolution and bioavailability of levosulpiride, even more than the commercial product.


Assuntos
Portadores de Fármacos , Lipídeos , Nanopartículas/química , Sulpirida/análogos & derivados , Animais , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Lipídeos/química , Lipídeos/farmacocinética , Lipídeos/farmacologia , Masculino , Ratos , Ratos Sprague-Dawley , Sulpirida/química , Sulpirida/farmacocinética , Sulpirida/farmacologia
2.
Nanomedicine (Lond) ; 15(2): 183-203, 2020 01.
Artigo em Inglês | MEDLINE | ID: mdl-31916472

RESUMO

Aim: In this study, the targeting of rifampicin (RIF)-loaded nanotransfersomes (NTs) incorporated in chitosan gel for leishmania-infected macrophages via the topical route was investigated. Materials & methods: NTs were prepared through a thin-film hydration process and incorporated into chitosan gel. Results: The mean particle size of the NTs was 190 nm, with 83% encapsulation efficiency. The permeation rate of the NTs was threefold higher than that of the RIF solution. The NTs improved cellular internalization via passive targeting, which was confirmed by macrophage uptake evaluation. A low IC50 value, flow cytometry analysis and in vivo study demonstrated the RIF-loaded NTs enhanced apoptosis and had better antileishmanial effects. Conclusion: RIF-loaded NT gel could be a fitting carrier for the delivery of antileishmanial drugs in cutaneous leishmaniasis.


Assuntos
Quitosana/farmacologia , Leishmaniose Cutânea/tratamento farmacológico , Polietilenoglicóis/farmacologia , Polietilenoimina/farmacologia , Rifampina/farmacologia , Administração Tópica , Animais , Antiprotozoários/química , Antiprotozoários/farmacologia , Quitosana/química , Modelos Animais de Doenças , Sistemas de Liberação de Medicamentos , Citometria de Fluxo , Humanos , Leishmaniose Cutânea/parasitologia , Leishmaniose Cutânea/patologia , Macrófagos/efeitos dos fármacos , Camundongos , Nanogéis , Nanopartículas/química , Ratos , Rifampina/química
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