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Revista Colombiana de Ciencias Químico - Farmacéuticas

versão impressa ISSN 0034-7418versão On-line ISSN 1909-6356

Resumo

VILLARREAL, Oscar Santiago et al. Physicochemical characterization and in vitro evaluation of self-emulsifying indomethacin release systems. Rev. colomb. cienc. quim. farm. [online]. 2022, vol.51, n.1, pp.185-212.  Epub 17-Dez-2023. ISSN 0034-7418.  https://doi.org/10.15446/rcciquifa.v51n1.95366.

Aim:

To load indomethacin into self-emulsifying delivery systems in order to increase, water-solubility, rate dissolution and in vitro permeation.

Methodology:

Equilibrium solubility tests were carried out to prepare formulations with the excipients, in which indomethacin presented a greater increase in solubility; the systems were characterized by self-emulsification time, physical stability, particle size, zeta potential, dissolution profiles and permeation through synthetic membrane.

Results:

The experimental design of self-emulsifying delivery systems allowed to create formulations that increase the solubility of indomethacin in an order of 105 times with respect to the aqueous solubility. The feasible formulations presented autoemulsification times less than 60 seconds, in addition, the particle size distributions of the dispersions were less than 300 nm, with polydispersity index smaller than 0.3, and zeta potential values lower than -25 mV. The dissolution profiles showed that the formulations comply with a similarity factor value greater than 50, in addition, the permeability through a synthetic membrane is higher for the self-emulsifying formulations than the reference product.

Conclusion:

The formulation of indomethacin into self-emulsifying delivery systems enhances the solubility in aqueous medium, increases dissolution and accelerate release. These results suggest that the oral administration of indomethacin incorporated into self-emulsifying delivery systems can accelerate the onset of the pharmacological effect.

Palavras-chave : Indomethacin; solubility; dissolution; lipid formulations.

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