Pérez Yolanda Alvarado, Urista Claudia Muro, Martínez Javier Illescas, Nava María Del Carmen Díaz, Rodríguez Francisco A Riera
Departamento de Ingeniería Química e Investigación, Instituto Tecnológico de Toluca, Apartado Postal 890, 52149 Metepec, MEX, Mexico.
Departamento de Ingeniería Química y Tecnología de Medio Ambiente, Universidad de Oviedo, Oviedo, 33006 Asturias, Spain.
Polymers (Basel). 2016 Jun 2;8(6):214. doi: 10.3390/polym8060214.
Currently, many sensitive molecules have been studied for effective oral administration. These substances are biologically active compounds that mainly suffer early degradation in the gastrointestinal tract (GIT) and physicochemical instability, inactivation and poor solubility and permeability. The sensibility of the biomolecules has limited their oral administration in the body and today is an important research topic to achieve desired effects in medicine field. Under this perspective, various enhancement approaches have been studied as alternatives to increase their oral bioavailability. Some of these strategies include functionalized polymers to provide specific useful benefits as protection to the intestinal tract by preventing its degradation by stomach enzymes, to increase their absorption, permeability, stability, and to make a proper release in the GIT. Due to specific chemical groups, shapes and sizes, morphologies, mechanical properties, and degradation, recent advances in functionalized polymers have opened the door to great possibilities to improve the physicochemical characteristics of these biopharmaceuticals. Today, many biomolecules are found in basic studies, preclinical steps, and others are late stage clinical development. This review summarizes the contribution of functionalized polymers to enhance oral bioavailability of sensitive molecules and their application status in medicine for different diseases. Future trends of these polymers and their possible uses to achieve different formulation goals for oral delivery are also covered in this manuscript.
目前,已经对许多敏感分子进行了有效口服给药方面的研究。这些物质是生物活性化合物,主要在胃肠道(GIT)中过早降解,并且存在物理化学不稳定性、失活以及溶解性和渗透性差的问题。生物分子的敏感性限制了它们在体内的口服给药,如今这是在医学领域实现预期效果的一个重要研究课题。从这个角度来看,已经研究了各种增强方法作为提高其口服生物利用度的替代方案。其中一些策略包括功能化聚合物,以提供特定的有益效果,例如通过防止胃酶降解来保护肠道,提高其吸收、渗透性、稳定性,并在胃肠道中实现适当释放。由于特定的化学基团、形状和尺寸、形态、机械性能以及降解情况,功能化聚合物的最新进展为改善这些生物药物的物理化学特性带来了巨大可能性。如今,许多生物分子处于基础研究、临床前阶段,其他一些则处于临床开发后期。本综述总结了功能化聚合物对提高敏感分子口服生物利用度的贡献及其在治疗不同疾病的医学中的应用现状。本文还涵盖了这些聚合物的未来趋势以及它们为实现口服给药的不同制剂目标的可能用途。