Affiliation:
1. Department of Drugs and Medicines, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara,
14800-903, SP, Brazil
Abstract
Background:
A drug with poor water-solubility, like Dexamethasone acetate, can present
lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in
the raw material can lead to drug quality problems.
Objective:
In this study, nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer
(HPH) method in surfactant poloxamer 188 (P188) solid dispersion and the bioavailable in
raw material with polymorphism presence was evaluated.
Methods:
The powder pre-suspension was prepared by the HPH process, and the nanoparticles formed
were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of
XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric
analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in
vitro evaluation by dissolution studies.
Results:
The characterization techniques were adequate to show the presence of raw material with physical
moisture between two dexamethasone acetate polymorphs. The nanocrystals formed in the presence
of the P188 in the formulation showed a considerable increase in the rate of dissolution of the drug in
the medium and in the size of the stable nanocrystals, even in the presence of dexamethasone acetate
polymorphs.
Conclusion:
The results showed that it was possible to produce dexamethasone nanocrystals by HPH
process with regular size by the presence of the small amount of P188 surfactant. This article presents a
novelty in the development of dexamethasone nanoparticles that have different polymorphic forms in
their physical composition.
Funder
CNPq, Conselho Nacional de Desenvolvimento Científico e Tecnológico
Fundação de Amparo à Pesquisa do Estado de São Paulo
Publisher
Bentham Science Publishers Ltd.
Subject
Biomedical Engineering,Pharmaceutical Science