Title:Preparation and Characterization of Mixed Polymeric Micelles as a Versatile Strategy for Meloxicam Oral Administration
VOLUME: 14 ISSUE: 12
Author(s):Claudia Amaral, Mariana Magalhaes, Celia Cabral, Francisco Veiga and Ana Figueiras*
Affiliation: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
Keywords:Pluronic P123, pluronic F68, polymeric micelles, meloxicam, drug delivery systems, oral administration.
Abstract: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.
