Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropylcellulose pellets

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• 作者：Paolo Mannina ; Lorena Segale ; ^{lorena.segale@uniupo.it" class="auth_mail" title="E-mail the corresponding author} ; Lorella Giovannelli ; Andrea Foglio Bonda ; Franco Pattarino
• 关键词：Sodium alginate (PubChem CID 6850754) ; Hydroxypropylcellulose (PubChem CID 71306830) ; Pectin (PubChem CID 854) ; Ibuprofen (PubChem CID 114864) ; d-α-Tocopherol polyethylene glycol 1000 succinate (PubChem CID 71406)
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：29 February 2016
• 年：2016
• 卷：499
• 期：1-2
• 页码：74-80
• 全文大小：971 K

文摘

In this work, alginate, alginate–pectin and alginate–hydroxypropylcellulose pellets were produced by ionotropic gelation and characterized. Ibuprofen was selected as model drug; it was suspended in the polymeric solution in crystalline form or dissolved in a self-emulsifying phase and then dispersed into the polymeric solution. The self-emulsifying excipient platform composed of Labrasol (PEG-8 caprylic/capric glycerides) and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS), able to solubilize the drug was used to improve the technological and biopharmaceutical properties of the alginate pellets. The pellets had diameters between 1317 and 2026 μm and a high drug content (>51%). DSC analysis showed the amorphous state of drug in the pellets containing the self-emulsifying phase. All the systems restricted drug release in conditions simulating the gastric environment and made the drug completely available at a pH value typical for the intestine. Only alginate-HPC systems containing the drug solubilized into the self-emulsifying phase showed the ability to partially control the release of ibuprofen at neutral pH. The self-emulsifying excipient platform is a useful tool to improve technological and biopharmaceutical properties of alginate–HPC pellets.