RESUMO
Aim of the present work is to study the effects of oil and drug concentrations on droplets size of a nanoemulsion. Newly introduced oil, palm oil esters (POEs) by Universiti Putra Malaysia researchers was selected for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Nanoemulsions were prepared with different concentrations of oil and drug and their effects on droplets size were studied by laser scattering spectroscopy (Nanophox). The results of droplets size analysis shows the droplets size increase with increasing concentration of oil and drug concentrations. It can be concluded from this study, that oil and drug concentrations have an effect on the droplets size of POEs nanoemulsion system.
Assuntos
Ésteres , Cetoprofeno/administração & dosagem , Nanopartículas , Óleos de Plantas , Química Farmacêutica , Emulsões , Ésteres/administração & dosagem , Cetoprofeno/química , Óleo de Palmeira , Tamanho da Partícula , Óleos de Plantas/administração & dosagemRESUMO
Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Edema/tratamento farmacológico , Ésteres/química , Cetoprofeno/farmacologia , Nanoestruturas/química , Óleos de Plantas/química , Analgésicos/síntese química , Analgésicos/química , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Carragenina , Edema/induzido quimicamente , Emulsões/síntese química , Emulsões/química , Emulsões/farmacologia , Hiperalgesia/induzido quimicamente , Hiperalgesia/tratamento farmacológico , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Cetoprofeno/análogos & derivados , Cetoprofeno/química , Masculino , Dor/induzido quimicamente , Dor/tratamento farmacológico , Ratos , Ratos Sprague-DawleyRESUMO
This study sets out to investigate the in vitro permeation of ketoprofen from the formulated nanoemulsions through excised rat skin. In vitro permeation of ketoprofen nanoemulsion through rat skin was evaluated in Franz diffusion cells and compared with marketed product (Fastum gel). Limonene which has been reported to be a good enhancer for ketoprofen was selected. Moreover the effects of limonene which was added to the nanoemulsion formulations at levels of 1%, 2%, 3% and on rat skin permeation of ketoprofen were also evaluated. The selected optimized formulation was further studied for skin irritation. Utilization of limonene as a penetration enhancer increased the permeation of ketoprofen from the formulated nanoemulsion with increasing concentrations of limonene. The results obtained showed that nanoemulsion with 3% limonene produced similar and comparable skin permeation of ketoprofen with marketed formulation and the skin irritation study on rats showed the optimized formulation prepared was safe.
Assuntos
Cicloexenos/farmacologia , Ésteres , Cetoprofeno/metabolismo , Nanopartículas , Óleos de Plantas , Pele/metabolismo , Terpenos/farmacologia , Animais , Relação Dose-Resposta a Droga , Emulsões , Técnicas In Vitro , Limoneno , Masculino , Óleo de Palmeira , Permeabilidade/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Absorção Cutânea/efeitos dos fármacos , Estimulação QuímicaRESUMO
The aim of the present study is to formulate and investigate the potential of nanoemulsion formulation for topical delivery of ketoprofen. In this study, Palm Oil Esters (POEs) a newly introduced oil by Universiti Putra Malaysia researchers was chosen for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Oil-in-water nanoemulsion was prepared by spontaneous emulsification method. The droplets size was studied by laser scattering spectroscopy (Nanophox) and Transmission Electron Microscopy (TEM). Franz diffusion cells were used, to determine the drug release and drug transferred through methyl acetate cellulose membrane (artificial membrane). The results of droplets size analysis shows the droplets are in the range of nanoemulsion which is below than 500 nm. The in vitro release profile shows a sufficient percentage of drugs released through the methyl acetate cellulose membrane. This initial study showed that the nanoemulsion formulated using POEs has great potential for topical delivery of ketoprofen.