International Journal of Pharmaceutics 2015-04-30

Formulation and characterization of ORMOSIL particles loaded with budesonide for local colonic delivery.

Vesna Petrovska-Jovanovska, Nikola Geskovski, Maja Simonoska Crcarevska, Oya Memed, Gjorgji Petruševski, Marina Chachorovska, Marija Petrusevska, Ana Poceva-Panovska, Kristina Mladenovska, Sonja Ugarkovic, Marija Glavas-Dodov

文献索引：Int. J. Pharm. 484(1-2) , 75-84, (2015)

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摘要

In this study, hybrid silica xerogel particles were developed as carriers of budesonide (BDS) for efficient local treatment of inflammatory bowel diseases (IBD). Organically modified silica particles (ORMOSILs) were prepared by co-condensation of 3-aminopropyltriethoxysilane (APTES) and tetraethyl orthosilicate (TEOS) by an ambient temperature acid catalysed sol-gel process followed by spray-drying. Formulation for preparation of BDS-loaded particles was optimized and their physicochemical parameters and drug release profiles were evaluated in vitro. Optimal formulation had a small particle size (mean diameter of 1.45±0.02μm) with unimodal narrow size distribution and high encapsulation efficiency (98.0 ± 1.85%). Due to the positive surface charge originated from amino group of APTES, ORMOSILs showed excessive mucoadhesiveness in comparison to native TEOS particles. The drug release decreased with increasing pH from 2.0 to 7.4. In order to avoid undesirable erroneous performance in the upper GI tract, particles were additionally coated with Eudragit(®) FS 30D, as a barrier to the drug release at pH range from 2.0 to 7.0. After Eudragit(®) FS 30D coating, the release of BDS in acidic media was sustained, while no significant differences in drug release were observed at pH 7.4. In conclusion, pH-responsive ORMOSILs showed great potential for efficient BDS delivery to the colon region.Copyright © 2015 Elsevier B.V. All rights reserved.