Desenvolvimento, caracterizaÃÃo e estudo de permeaÃÃo cutÃnea de diclofenaco de dietilamÃnio em sistemas tÃpicos nanoemulsionados

AUTOR(ES)

Josà Alexsandro da Silva

DATA DE PUBLICAÇÃO

2008

RESUMO

The nanoemulsions (NE) are transparent, isotropic and thermodynamically stable systems, formed spontaneously under a specific set of experimental conditions from mixtures of water and oil phases stabilized by a surfactant or a mixture of surfactant and cosufactant. Because of their properties, especially the ability to carry lipophilic and hydrophilic drugs into their lipophilic and hydrophilic phases, respectively; and amphiphilic drugs into their oil/water interface, they present a large potencial as a drug delivery system. Dicoflenac diethylamine (DDA) is a non-steroidal antiinflammatory drug (AINEs), powerful inhibitor of prostaglandin synthesis which when is managed topically, penetrates an enough amount into skin for reaching the local. DDA presents hepatic metabolism, a short life span, and a low partition coefficient, and besides, is able to form micelles and lyotropic liquid crystals in water. In reason for dicoflenac gastrintestinal toxity, nowadays, there is a great motivation by the scientific community in developing new pharmaceutical ways in dispersed systems, among them, is found NE with the objective to reduce these collateral effects. The aims of this research were develop and characterize nanoemulsions pharmaceutical forms for propagation of the DDA, through cutaneous kinetic permeation in swine and human being. The resulted formula from the pseudo-ternary phase diagrams, had been characterized and evaluated such its macroscopic aspects, efficiency of encapsulation, electric conductivity, pH, rheology, refractive index, density, zeta potential, microscopy for light scattering and microscopy of polarized light. The study in vitro of cutaneous permeation and retention was made through the Franz model and the antiedematogenic activity in vivo was determined by an animal model, using pawâs edema induced technique by carrageenan. The used technique to determine the pseudo-ternary phase diagram of these systems showed simple and reproductible. The gotten NE samples had presented the same limpidity, transparency and isotropy after the incorporation of the DDA, showing that the pharmaco did not influence the interfacial tension between the aqueous phase and the oily one, not disturbing the thermodynamic stability of the systems. The systems studied in the characterization behaved as Newtonian time-independent fluid, therefore they had kept constant viscosity, with the applied speed of shear. The analytical methods proposed in this paper had been developed in order to expose analytical procedures for DDA quantification in nanoemulsion pharmaceutical form and in human being skin, for this reason, the absence of official methods destined to these types of assays, the same could be considered as a methodological alternative for DDA dosage in pharmaceutical forms. The methods had been simple and presented trustworthiness and security in analytical procedures. The verified parameters had guaranteed speedy, selectivity, linearity, accuracy and precision, presenting this way, validate according to RE 899/2003 (ANVISA). It was possible to understand the kinetic phenomena of order and pseudo-first order (Higuchi model) in swine skin such as human being as well. Finally, these systems had presented great thermodynamic stability for the DDA, promoting high solubility in aqueous way, besides presenting droplets of water in appropriate size to transdermical systems of controlled discharging. On the other hand, the in vivo study in animal model, showed that the NE had presented antiedematogenic activity able to inhibit the inflammation. This way, it can be concluded that the developeded NE follow the safety and effectiveness requested norms for utilization in transdermic way

ASSUNTO(S)

nanoemulsÃes cinÃtica de permeaÃÃo farmacia caracterizaÃÃo diclofenaco dietilamÃnio nanoemulsion diagrama fases dicoflenac diethylamine pseudo-ternary phase diagrams permeation kinetic characterization

Documentos Relacionados

• Estudo de permeaÃÃo in vitro e avaliaÃÃo tÃrmica de emulgel tÃpico a base de lapachol
• Desenvolvimento, caracterizaÃÃo e aplicaÃÃo de um jato de plasma de baixa densidade de corrente.
• AvaliaÃÃo do tratamento tÃpico com a lectina de Eugenia mallaccensis frente à cicatrizaÃÃo cutÃnea em camundongos
• Desenvolvimento, caracterizaÃÃo e estimativas de erros de genotipagem de locos microssatÃlites de tabebuia Ãurea (bignoniaceae)
• Ensaio e anÃlise de reparos estruturais tÃpicos em revestimento de aeronaves tolerantes a dano.