Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Int J Biol Macromol. 2018 Aug;115:483-493. doi: 10.1016/j.ijbiomac.2018.04.095. Epub 2018 Apr 19.
Polysaccharide-protein composites offer potential utility for the delivery of drugs. The objectives of this work were to investigate the molecular interactions between sodium alginate (SA) and sodium caseinate (SC) in dispersions and films and to characterize calcium alginate (CA) beads mixed with SC for the delivery of fluconazole (FZ) and clotrimazole (CZ). The results demonstrated that SA could interact with SC, which caused a viscosity synergism in the dispersions. Hydrogen bonding between the carboxyl or hydroxyl groups of SA and the amide groups of SC led to the formation of soluble complexes that could reinforce the CA beads prepared by calcium cross-linking. The SC-CA beads provided higher drug entrapment efficiency, lower water uptake and erosion, and slower drug release than for the CA beads. The loaded FZ was an amorphous form, but CZ crystals were embedded in the bead matrix due to the low water solubility of this drug. However, SC micellization could enhance the water solubility and efficacy of CZ against Candida albicans. This finding indicates that SA can interact with SC via hydrogen bonding to form complexes and that the anticandidal-loaded SC-CA beads can be used as drug delivery systems and drug reservoirs in tablets for oral candidiasis.
多糖-蛋白质复合材料在药物传递方面具有潜在的应用价值。本研究的目的是研究海藻酸钠（SA）和酪蛋白酸钠（SC）在分散体和薄膜中的分子相互作用，并对混合有 SC 的海藻酸钙（CA）珠粒用于氟康唑（FZ）和克霉唑（CZ）的传递进行表征。结果表明，SA 可以与 SC 相互作用，导致分散体中的粘度协同作用。SA 的羧基或羟基与 SC 的酰胺基团之间的氢键导致形成可增强通过钙离子交联制备的 CA 珠的可溶性复合物。与 CA 珠相比，SC-CA 珠具有更高的药物包封效率、更低的吸水率和侵蚀率以及更慢的药物释放。负载的 FZ 呈无定形态，但由于该药物的低水溶性，CZ 晶体嵌入珠粒基质中。然而，SC 的胶束化可以提高 CZ 的水溶性和抗白色念珠菌的功效。这一发现表明，SA 可以通过氢键与 SC 相互作用形成复合物，并且负载抗真菌药物的 SC-CA 珠粒可用作口腔念珠菌病片剂中的药物传递系统和药物库。
