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|Title:||Loading of 5-aminosalicylic in solid lipid microparticles (SLM): Solubility screening of lipid excipients and physicochemical characterization|
|Author(s):||Silveira, Elisânia F.|
da Silva, Classius F.
Chaud, Marco V.
Barbosa, Raquel de M.
Junior, Ricardo L. C. A.
Costa, Luiz P. da
|Keywords:||Solid lipid microparticles|
|Journal:||Journal of Thermal Analysis and Calorimetry|
|Citation:||Silveira, Elisânia F.; Rannier, Lucas; Nalone, Luciana; da Silva, Classius F.; Chaud, Marco V.; de M. Barbosa, Raquel; Junior, Ricardo L. C. A.; da Costa, Luiz P.; Souto, Eliana; Severino, Patrícia, Loading of 5-aminosalicylic in solid lipid microparticles (SLM): Solubility screening of lipid excipients and physicochemical characterization. Journal of Thermal Analysis and Calorimetry, 139(2), 1151-1159, 2019.|
|Abstract(s):||5-Aminosalicylic acid (5-ASA), the active moiety of sulphasalazine, is the most commonly used drug for treating patients with inflammatory bowel disease (IBD). Its bioavailability is low, i.e. 20--30\% upon oral administration and 10--35\\% by rectal administration. As the extent of 5-ASA absorption is very much dependent on the time-length, the drug is retained in the colon, a way to increase drug retention is the use of orally administered sustained released formulations. Solid lipid microparticles (SLM) are a viable option for site-specific targeted delivery in compressed tablets produced by direct compaction. In this study, we describe the development and characterization of 5-ASA-loaded SLM for sustained release. The solubility of 5-ASA in different types of solid lipids (e.g. cetyl palmitate, cetyl alcohol, and cetearyl alcohol) was evaluated to select the best lipid as the inert matrix-forming agent to control the release of the drug. SLM dispersions were prepared using the hot emulsification method employing the selected solid lipid, lecithin (LipoidÂ®) as surfactant, dimethyl sulphoxide, and acetone stabilized with ArlacelÂ®. The characterization was performed by differential scanning calorimetry, thermogravimetric analysis, wide-angle x-ray diffraction, Fourier transform infrared spectroscopy measurements, optical microscopy, and scanning electron microscopy. Results show that the best lipid for dissolving the 5-ASA was cetyl palmitate and that the melting process did not affect the chemical stability of the materials. The thermal analysis suggests that 5-ASA was successfully encapsulated with the microparticles, of spherical shape and uniform size distribution.|
|Access:||Restricted access (UMinho)|
|Appears in Collections:||CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series|
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