Development and characterization of biocompatible isotropic and anisotropic oil-in-water colloidal dispersions as a new delivery system for methyl dihydrojasmonate antitumor drug

Abstract

Microemulsions (MEs) are colloidal systems that can be used for drug-delivery and drug-targeting purposes. These systems are able to incorporate drugs modifying bioavailability and stability and reducing toxic effects. The jasmonate compounds belong to a group of plant stress hormones, and the jasmonic acid and its methyl ester derivative have been described as having anticancer activity. However, these compounds are very poorly water-soluble, not allowing administration by an intravenous route without an efficient nanostructured carrier system. In this work, biocompatible MEs of appropriate diameter size for intravenous route administration, loaded and unloaded with methyl dihydrojasmonate (MJ), were developed and described in a pseudo-ternary phase diagram. The compositions of the MEs were carefully selected from their own regions in the pseudo-ternary phase diagram. The formulations were analyzed by light scattering, polarized light microscopy, and X-ray diffraction. Also, a study on rheological profile was performed. The results showed that the droplet size decreased with both MJ incorporation and oil phase/surfactant ratio. All compositions of the studied MEs showed rheological behavior of pseudoplastic fluid and amorphous structures. In the absence of MJ, most of the studied MEs had thixotropic characteristics, which became antithixotropic in the presence of the drug. Almost all MJ-unloaded MEs presented anisotropic characteristics, but some formulations became isotropic, especially in the presence of MJ. The results of this study support the conclusion that the studied system represents a promising vehicle for in vivo administration of the MJ antitumor drug.

Development, Characterization, andIn VitroBiological Performance of Fluconazole-Loaded Microemulsions for the Topical Treatment of Cutaneous Leishmaniasis

“…The PDI is an index that reflects the relative homogeneity of particle sizes in a sample. The PDI values varied from 0.174 to 0.703 demonstrating a good size distribution of the oil droplets in the ME system, reflecting the size homogeneity of the droplets in the bulk ME [ 45 , 46 ].…”

“…The absence of high peaks in Figure 3 shows that the FLU-loaded ME and FLU-unloaded ME exhibited low intensity peaks with amorphous halos present that is common and desirable characteristic for microemulsion systems [ 46 ].…”

Structural Characterization andIn VitroAntioxidant Activity of Kojic Dipalmitate Loaded W/O/W Multiple Emulsions Intended for Skin Disorders

“…The KDP-unloaded ME formulation behaved as a pseudoplastic shear thinning fluid because its viscosity ( η * ) decreased with increasing stress. This may be due to the breaking of organized structures that promote the formation of droplets, which are less organized structures [ 33 ].…”

“…The increase in the apparent viscosity of the ME formulations with time at a constant shear was most likely due to the reorganization of the droplets by strong forces. The high viscosity of the MEs could retard the free motion of the droplets, thus delaying creaming, flocculation, and coalescence of the system [ 33 ]. The conclusion from these results is that stable MEs can be obtained with the components used in this study only under the application of vigorous stirring during preparation so that viscosity is incorporated and the destabilization of the system is avoided.…”

Estratégias Tecnológicas Para Formulações De Anfotericina B Em Sistemas Lipídicos Disponíveis No Mercado Farmacêutico E Outros Promissores Sistemas De Administração

“…Formam-se sistemas reservatórios que modificam a velocidade de liberação de fármacos. Estes sistemas podem alterar os parâmetros farmacocinéticos, aumentar o índice terapêutico, e como consequência, diminuir a toxicidade e aumentar a eficácia clínica da AmB (21,22,23,24). Entre os sistemas de liberação comerciais para a AmB, destacam-se o Ambisome®, formulação lipossomal que permite administrar dose de até 7,5 mg/kg/dia com um perfil de segurança adequado, maior do que a fórmula convencional de Fungizone® (18).…”