Maria Curie-Sklodowska University, Faculty of Chemistry, Department of Adsorption, 3M. Curie-Sklodowska Sq., Lublin 20-031, Poland.
Medical University of Lublin, Faculty of Pharmacy, Department of Applied Pharmacy, 1 Chodzki Str, Lublin 20-093, Poland.
Colloids Surf B Biointerfaces. 2016 Jun 1;142:30-37. doi: 10.1016/j.colsurfb.2016.02.041. Epub 2016 Feb 22.
The present study concerns the preparation of ternary composites via the in situ encapsulation of solid dispersion of diclofenac sodium within the acrylic polymer beads. The encapsulating species were produced through the hydrolysis and condensation of the silica precursors (tetraethoxysilane or ethyltriethoxysilane) introduced into the solid dispersion. The transformation of precursors occurred in the vapor phase of ammonia. A great advantage of the presented vapor-phase method is preventing the desorption of the highly soluble drug during gelation of silica precursors, which stands in contrast to the conventional sol-gel processes occurring in the solution. The conducted studies, involving the low temperature N2 sorption together with spectroscopic techniques, provide insight into the structural differences of drug loaded particles. They reveal that the formation of silica gel accompanies the conversion of the drug into its amorphous form. Finally, the desorption profiles of diclofenac sodium demonstrate that the deposition of silica gel successfully diminishes the degree of the initial drug desorption while significantly modifying its release rate.
本研究通过在丙烯酸聚合物珠粒内原位包封双氯芬酸钠的固体分散体来制备三元复合材料。包封物种是通过引入固体分散体中的硅烷前体(四乙氧基硅烷或乙基三乙氧基硅烷)的水解和缩合产生的。前体的转化发生在氨的气相中。所提出的气相方法的一个很大的优点是防止在硅烷前体凝胶化过程中高溶性药物的解吸,这与在溶液中发生的传统溶胶-凝胶过程形成对比。涉及低温 N2 吸附和光谱技术的研究提供了对载药颗粒结构差异的深入了解。它们表明,硅胶的形成伴随着药物向无定形形式的转化。最后,双氯芬酸钠的解吸曲线表明,硅胶的沉积成功地降低了初始药物解吸的程度,同时显著改变了其释放速率。