Journal
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY
Volume 139, Issue 2, Pages 1151-1159Publisher
SPRINGER
DOI: 10.1007/s10973-019-08544-7
Keywords
Solid lipid microparticles; Cetyl palmitate; 5-aminosalicylic acid; DSC; WAXS; FTIR
Funding
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico -CNPq [443238/2014-6, 470388/2014-5]
- Portuguese Science and Technology Foundation, Ministry of Science and Education (FCT/MEC) [M-ERA-NET/0004/2015]
- FEDER under the Partnership Agreement PT2020
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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(R)) as surfactant, dimethyl sulphoxide, and acetone stabilized with Arlacel(R). 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.
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