Please use this identifier to cite or link to this item: http://hdl.handle.net/1822/63342

TitleLoading of 5-aminosalicylic in solid lipid microparticles (SLM): Solubility screening of lipid excipients and physicochemical characterization
Author(s)Silveira, Elisânia F.
Rannier, Lucas
Nalone, Luciana
da Silva, Classius F.
Chaud, Marco V.
Barbosa, Raquel de M.
Junior, Ricardo L. C. A.
Costa, Luiz P. da
Souto, Eliana
Severino, Patrícia
KeywordsSolid lipid microparticles
Cetyl palmitate
5-aminosalicylic acid
DSC
WAXS
FTIR
Issue date2019
PublisherSpringer
JournalJournal of Thermal Analysis and Calorimetry
CitationSilveira, 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 (Lipoid®) as surfactant, dimethyl sulphoxide, and acetone stabilized with Arlacel®. 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.
TypeArticle
URIhttp://hdl.handle.net/1822/63342
DOI10.1007/s10973-019-08544-7
ISSN1388-6150
e-ISSN1588-2926
Publisher versionhttp://www.springer.com/chemistry/physical+chemistry/journal/10973
Peer-Reviewedyes
AccessRestricted access (UMinho)
Appears in Collections:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series

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