Alginate-based hybrid aerogel microparticles for mucosal drug delivery

Journal
European journal of pharmaceutics and biopharmaceutics  
Volume
107
Start Page
160
End Page
170
Citation
European Journal of Pharmaceutics and Biopharmaceutics (107): 160-170 (2016-10-01)
Publisher DOI
10.1016/j.ejpb.2016.07.003
Scopus ID
2-s2.0-84978101100
Publisher
Elsevier
The application of biopolymer aerogels as drug delivery systems (DDS) has gained increased interest during the last decade since these structures have large surface area and accessible pores allowing for high drug loadings. Being biocompatible, biodegradable and presenting low toxicity, polysaccharide-based aerogels are an attractive carrier to be applied in pharmaceutical industry. Moreover, some polysaccharides (e.g. alginate and chitosan) present mucoadhesive properties, an important feature for mucosal drug delivery. This feature allows to extend the contact of DDS with biological membranes, thereby increasing the absorption of drugs through the mucosa. Alginate-based hybrid aerogels in the form of microparticles (<50 μm) were investigated in this work as carriers for mucosal administration of drugs. Low methoxyl pectin and κ-carrageenan were co-gelled with alginate and further dried with supercritical CO2 (sc-CO2). Spherical mesoporous aerogel microparticles were obtained for alginate, hybrid alginate/pectin and alginate/κ-carrageenan aerogels, presenting high specific surface area (370–548 m2 g−1) and mucoadhesive properties. The microparticles were loaded with ketoprofen via adsorption from its solution in sc-CO2, and with quercetin via supercritical anti-solvent precipitation. Loading of ketoprofen was in the range between 17 and 22 wt% whereas quercetin demonstrated loadings of 3.1–5.4 wt%. Both the drugs were present in amorphous state. Loading procedure allowed the preservation of antioxidant activity of quercetin. Release of both drugs from alginate/κ-carrageenan aerogel was slightly faster compared to alginate/pectin. The results indicate that alginate-based aerogel microparticles can be viewed as promising matrices for mucosal drug delivery applications.
Subjects
Alginate
Carrageenan
Hybrid aerogels
Microparticles
Pectin
Supercritical fluid technology
DDC Class
600: Technik
More Funding Information
Supported by Fundação para a Ciência e Tecnologia (FCT) through grant PEst-OE/EQB/LA0004/2011 and DFG (project SM 82/8-3). V. S. S. Gonçalves is grateful for the financial support from FCT through the grant SFRH/BD/77350/2011 and transnational cooperation project FCT-DAAD (57050501). iNOVA4Health – UID/Multi/04462/2013, a program financially supported by Fundação para a Ciência e Tecnologia/Ministério da Educação e Ciência, through national funds and co-funded by FEDER under the PT2020 Partnership Agreement is acknowledged.