This project was carried out to investigate the feasibility of using microemulsions for transdermal delivery of lapachol. From the screening of surfactants and oils, a range of microemulsions were developed using oleic acid, a mixture of Cremophor EL and Tween 20 and water. The solubility of lapachol was determined in these ingredients and in the formulated microemulsions. The microemulsions were characterised using cross-polarising light microscopy, their electrical conductivity, pH, zeta potential and rheology were analysed, and they were also investigated using small-angle X-ray scattering and differential scanning calorimetry. Ex vivo studies were performed using porcine ear skin and Franz diffusion cells to investigate the permeation and retention of lapachol. Systems containing different concentrations of Cremophor EL (8.4-41.6%), Tween 20 (5.4-41.6%) and oleic acid (12-31.9%) are able to form microemulsions. Lapachol was delivered more effectively through the skin from all of the microemulsions tested than by the control (oleic acid). These studies indicated that microemulsions incorporating lapachol were formed successfully and that these enhanced drug delivery and retention in the skin. Microemulsion systems may, therefore, provide promising vehicles for percutaneous delivery of lapachol.
The adequate management of analgesia, by pharmacological methods or not, is a great challenge. Local anesthetics are used for pain relief, mainly by parenteral, intramuscular, catheter, and other routes of administration. The use of in situ forming systems becomes an alternative for the control of pain. The present research investigates development of thermogels containing poloxamer and levobupivacaine. All formulations were prepared by the cold method; the compatibilities of the excipients were evaluated by DSC, rheology and viscosities, transition temperature, syringeability, release kinetics, and permeation. The compatibility of the tested excipients with the drug was initially observed; all formulations had a viscosity increase at 37°C. Different delivery rates were observed in both the release and permeation studies. The developed systems maintained the in vitro release of the drug for a long period, likely decreasing side effects in vivo and avoiding the need for supplementary analgesia by other routes.
As verrugas genitais são lesões epiteliais induzidas pelo Papillomavirus Humano (HPV). Atualmente, as técnicas utilizadas para tratamento dessas lesões são dolorosas e as recidivas costumam acontecer em um curto espaço de tempo. Diversos estudos têm demonstrado a eficácia do cidofovir no tratamento de HPV entre outras infecções virais. O objetivo desta revisão de literatura é fazer uma abordagem sobre o fármaco e a sua utilização clínica no tratamento de HPV, apresentando a forma farmacêutica, posologia, reações adversas e dados sobre sua eficácia. Os resultados da pesquisa bibliográfica mostram que o uso intralesional e epidérmico do cidofovir em formulações extemporâneas tem se mostrado eficaz no manejo dos condilomas. A utilização tópica do cidofovir se apresenta, portanto, como uma alternativa clínica aos tratamentos convencionais, minimizando os efeitos colaterais locais e evitando a ocorrência de efeitos adversos sistêmicos. Diante disso, faz-se necessária a padronização de uma formulação tópica através de estudos de pré-formulação e demais ensaios clínicos visando a obtenção de uma preparação estável, segura e eficaz para tratamento das lesões associadas ao HPV.
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