Claudia Amaral, Mariana Magalhaes, Celia Cabral, Francisco Veiga and Ana Figueiras* Pages 1401 - 1408 ( 8 )
Introduction: Currently, there are a significant number of drugs getting approval with poor biopharmaceutical characteristics, as low solubility and bioavailability. These facts lead to a decrease of the therapeutic effect and to an increase of the drug dosage. In this regard, there is a need to overcome this problem, in which the development of new drug delivery systems (DDS) arises as a promising strategy, since these systems could improve some drug characteristics, like solubility and dissolution rate, increasing their therapeutic effect with a lower dose. Therefore, the aim of this work consisted in the development and characterization of a new formulation of mixed polymeric micelles based on Pluronics® P123 and F68 to improve the administration of meloxicam (MLX).
Methods: Firstly, polymeric micelles were prepared by the thin-film method. Secondly, it was performed the physicochemical characterization of the systems through the evaluation of their size, increment of solubility (IS) and encapsulation efficiency (EE) by DLS and UV spectroscopy, respectively. Besides this, it was also evaluated the morphology of the polymeric micelles by transmission electronic microscopy (TEM) and their chemical structure by FTIR spectroscopy and differential scanning calorimetry (DSC). Moreover, it was determined the physical stability of these systems and their cytotoxicity in vitro.
Results: The obtained results show that the formulation FM2, (Pluronic P123 and MLX) and the formulation FM3, (Puronic P123 and F68 and MLX) have presented the better results for size, polydispersion index (PDI), IS and EE. Being, these results related to the capacity of these formulations to protect and to avoid the sequestration of MLX by the liver and spleen and, consequently, to improve the bioavailability of MLX. Besides this, these systems have the better results for the assay representing the physical stability in the passage for the gastrointestinal (GI) tract and they have a low toxicity for the cells, even at bigger concentrations.
Conclusion: Thus, these formulations can be considered promising systems to improve the solubility of MLX and other poor soluble drugs in an oral administration.
Pluronic P123, pluronic F68, polymeric micelles, meloxicam, drug delivery systems, oral administration.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, P.O. Box: 3000- 548, Coimbra