Department of Pharmacology and Immunotherapy, Veterinary Research Institute, Hudcova 70, Brno 621 00, Czech Republic.
Faculty of Pharmacy, Masaryk University, Brno 625 00, Czech Republic.
J Control Release. 2020 Aug 10;324:695-727. doi: 10.1016/j.jconrel.2020.05.045. Epub 2020 May 29.
Hydroxypropylmethylcellulose (HPMC), also known as Hypromellose, is a traditional pharmaceutical excipient widely exploited in oral sustained drug release matrix systems. The choice of numerous viscosity grades and molecular weights available from different manufacturers provides a great variability in its physical-chemical properties and is a basis for its broad successful application in pharmaceutical research, development, and manufacturing. The excellent mucoadhesive properties of HPMC predetermine its use in oromucosal delivery systems including mucoadhesive tablets and films. HPMC also possesses desirable properties for formulating amorphous solid dispersions increasing the oral bioavailability of poorly soluble drugs. Printability and electrospinnability of HPMC are promising features for its application in 3D printed drug products and nanofiber-based drug delivery systems. Nanoparticle-based formulations are extensively explored as antigen and protein carriers for the formulation of oral vaccines, and oral delivery of biologicals including insulin, respectively. HPMC, being a traditional pharmaceutical excipient, has an irreplaceable role in the development of new pharmaceutical technologies, and new drug products leading to continuous manufacturing processes, and personalized medicine. This review firstly provides information on the physical-chemical properties of HPMC and a comprehensive overview of its application in traditional oral drug formulations. Secondly, this review focuses on the application of HPMC in modern pharmaceutical technologies including spray drying, hot-melt extrusion, 3D printing, nanoprecipitation and electrospinning leading to the formulation of printlets, nanoparticle-, microparticle-, and nanofiber-based delivery systems for oral and oromucosal application. Hypromellose is an excellent excipient for formulation of classical dosage forms and advanced drug delivery systems. New methods of hypromellose processing include spray draying, hot-melt extrusion, 3D printing, and electrospinning.
羟丙甲纤维素（HPMC），也称为羟丙基甲基纤维素，是一种传统的药物赋形剂，广泛应用于口服缓控释药物释放基质系统。不同制造商提供的众多粘度等级和分子量的选择为其物理化学性质提供了很大的可变性，这是其在药物研究、开发和制造中的广泛成功应用的基础。HPMC 具有优异的粘膜粘附性能，决定了其在口腔粘膜给药系统中的应用，包括粘膜粘附片剂和薄膜。HPMC 还具有理想的性质，可用于制备无定形固体分散体，提高难溶性药物的口服生物利用度。HPMC 的可印刷性和可纺性是其在 3D 打印药物产品和基于纳米纤维的药物输送系统中应用的有前途的特性。基于纳米颗粒的制剂被广泛探索作为抗原和蛋白质载体，用于口服疫苗的制剂，以及生物制品的口服输送，包括胰岛素。HPMC 作为一种传统的药物赋形剂，在新的药物技术和新的药物产品的开发中发挥着不可替代的作用，这些技术和产品导致了连续制造过程和个性化医疗。本综述首先提供了 HPMC 的物理化学性质的信息，并全面概述了其在传统口服药物制剂中的应用。其次，本综述重点介绍了 HPMC 在现代药物技术中的应用，包括喷雾干燥、热熔挤出、3D 打印、纳米沉淀和电纺丝，从而形成用于口服和口腔粘膜应用的打印片、纳米颗粒、微粒和纳米纤维给药系统。羟丙甲纤维素是制剂经典剂型和先进药物输送系统的优良赋形剂。羟丙甲纤维素的新加工方法包括喷雾干燥、热熔挤出、3D 打印和电纺丝。
