Abstract
Microspheres loaded by 2-aminopyrimidine (2-AP) and based on cellulose derivatives as polymeric matrices: ethylcellulose (EC) and cellulose acetate butyrate (CAB), were prepared by double emulsion solvent evaporation method (w/o/w). The main objective of this research is to conceptualize the fabrication of new formulations with high encapsulation efficiency and a large range of size for a controlled drug release of a water-soluble drug. The effects of the process variables, namely, nature of the matrix, stirring speed, surfactant nature and concentration on the mean particle size and distribution, drug loaded, encapsulation efficiency and drug release were investigated. The microspheres were characterized by SEM, optical microscopy, FT-IR spectroscopy and the size and size distribution (δ) were determined. SEM images showed spherical and porous microspheres with different structures. We have obtained systems with large ranges of size (d32, 45–219 µm with EC; d32, 37–160 µm with CAB using Polyvinyl alcohol (PVA) as emulsifier; and d32, 294–779 µm with Tween 80) by modifying the process parameters. Furthermore, the mean diameter d32 and the dispersion can be controlled particularly by stirring speed of emulsion and the emulsifier nature and concentration. The drug entrapment and encapsulation efficiency were improved by controlling certain factors, especially by using PVA as a stabilizer in the continuous phase, by increasing PVA concentration (2% PVA) and when using EC as a matrix. The drug release was established in simulated gastric medium at pH 1.2 and 37 °C by UV–Vis analysis to estimate the drug content. The kinetics results revealed that the drug release is governed by the diffusion mechanism and the release rate can be adjusted by varying the encapsulation factors that have a significant effect on the particle size and size distribution.
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Mouffok, M., Abdelmalek, I., Mesli, A. et al. Investigation of Factors Affecting Particle Size Distribution and Sustained Release of a Water-Soluble Drug from Cellulose Derivatives Microspheres. Chemistry Africa 6, 163–173 (2023). https://doi.org/10.1007/s42250-022-00323-6
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DOI: https://doi.org/10.1007/s42250-022-00323-6