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Título: Incorporation of 2-styrylchromones in liposomes: preliminaries studies
Autor: Carlos, M.
Almeida, D.
Gomes, A.
Fernandes, Eduarda
Lima, José Costa
Silva, Artur
Pinto, Diana
Santos, Clementina M.M.
Cavaleiro, José
Gaspar, R.
Corvo, M.L.
Issue Date: 2008
Citação: Carlos, M.; Almeida, M.; Fernandes, Eduarda; Costa Lima, José; Silva, Artur; Pinto, Diana; Santos, Clementina M.M.; Gaspar, R.; Corvo, M.L. (2008) - Incorporation of 2-styrylchromones in liposomes: preliminaries studies. In 1º Encontro Nacional de Química Terapêutica. Porto
Resumo: Several compounds with a 2-styrylchromone chemical structure have been shown to hold a high antioxidant activity in vitro, at low concentrations, which indicates a potential therapeutic value that needs to be confirmed in vivo [1-2] . The evaluation of the antioxidant potential of 2- styrylcromones, in vivo, is expected to beneficiate from a formulation that delivers the compound to specific target sites. Due to the structural analogies of 2-styrylcromones with flavonoids, a controlled delivery system - liposomes - was chosen to take advantage of the well known pharmacokinetic behaviour of liposome-incorporated flavonoids. Liposomes are lamellar lipidic structures which form almost spontaneously when certain lipids are hydrated in aqueous media [3 ,4]. This work presents, for the first rime, the results of the incorporation of 2-styrylcromones in liposomes. The characterization of the obtained formulations was based in the study of the encapsulation efficiency of the compound in liposomes, the knowledgment of the primary concentration of compound in the incorporation process and the effect of the addition of freeze-drying protector, threalose to the formulation. The obtained results showed that 2-syrylcromones could be encapsulated in lipossomes with high incorporation efficiency. The highest encapsulation efficiency was achieved with a concentration of drug of 1 μmol of total lipid. The results concerning the addition of threalose to the formulation indicated that the use of the freeze-drying protector reduces the effects caused by freeze-drying, such as the growth of the vesicles. This liposomal formulations is expected to allow the diffusion of these compounds to the target site in therapeutic concentrations.
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