Faculdade de Farmácia, Universidade Federal de Goiás, Av. Universitária esq. com 1ª Avenida, Setor Universitário, 74605-220, Goiânia, GO, Brazil.
AAPS PharmSciTech. 2013 Sep;14(3):1227-35. doi: 10.1208/s12249-013-0012-8. Epub 2013 Aug 9.
Pectin is a heteropolysaccharide which has been investigated for the development of colon-specific drug delivery systems. Polymers have been associated with pectin to reduce its aqueous solubility and improve the performance of drug delivery systems. Pectin-casein interaction is widely known in food research, but it has not been fully considered by pharmaceutical scientists. Thus, this study investigated the potential of casein-pectin microparticles as a drug delivery system and clarified the impact of cross-linking and drying methods on the in vitro release of indomethacin (IND) or acetaminophen (PCT) from microparticles. Microparticles were prepared by coacervation and dried by spray or spouted bed methods. Drug recovery, in vitro drug release, size, morphology, and the thermal and diffractometric properties of dried microparticles were determined. Spray-dried non-cross-linked microparticles were able to prolong IND release, and pectin was still degraded by pectinolytic enzymes. On the other hand, glutaraldehyde cross-linking prevented the enzymatic breakdown of pectin without improving IND release. Spouted bed drying reduced IND recovery from all microparticles when compared with spray drying, thus the successful spouted bed drying of microparticles depends on the chemical characteristics of both the drug and the polymer. Release data from PCT microparticles suggested that the microparticle formulation should be improved to bring about a more efficient delivery of water-soluble drugs. In conclusion, casein-pectin microparticles show great potential as a drug delivery system because casein reduces the water solubility of pectin. The drying method and cross-linking process had significant effects on the in vitro performance of these microparticles.
果胶是一种杂多糖，已被研究用于开发结肠特异性药物传递系统。聚合物与果胶结合可以降低其水溶性并改善药物传递系统的性能。果胶-酪蛋白相互作用在食品研究中广为人知，但在药物科学领域尚未得到充分考虑。因此，本研究探讨了酪蛋白-果胶微球作为药物传递系统的潜力，并阐明了交联和干燥方法对吲哚美辛（IND）或扑热息痛（PCT）从微球中体外释放的影响。微球通过共凝聚法制备，并通过喷雾或喷动床干燥方法进行干燥。测定了药物回收率、体外药物释放、粒径、形态以及干燥微球的热学和衍射特性。喷雾干燥未交联的微球能够延长 IND 的释放，并且果胶仍然被果胶酶降解。另一方面，戊二醛交联虽然阻止了果胶的酶解，但并没有改善 IND 的释放。与喷雾干燥相比，喷动床干燥会降低所有微球中 IND 的回收率，因此成功地对微球进行喷动床干燥取决于药物和聚合物的化学特性。PCT 微球的释放数据表明，应该改进微球配方以实现更有效的水溶性药物传递。总之，酪蛋白-果胶微球作为药物传递系统具有很大的潜力，因为酪蛋白降低了果胶的水溶性。干燥方法和交联过程对这些微球的体外性能有显著影响。
