Montenegro-Nicolini Miguel, Morales Javier O
Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santos Dumont 964, 4to piso, Of# 09, Independencia, Santiago, 8380494, Chile.
Instituto de Salud Pública de Chile, Santiago, 7780050, Chile.
AAPS PharmSciTech. 2017 Jan 1;18(1):3-14. doi: 10.1208/s12249-016-0525-z. Epub 2016 Apr 15.
The main route of administration for drug products is the oral route, yet biologics are initially developed as injectables due to their limited stability through the gastrointestinal tract and solubility issues. In order to avoid injections, a myriad of investigations on alternative administration routes that can bypass enzymatic degradation and the first-pass effect are found in the literature. As an alternative site for biologics absorption, the buccal route presents with a number of advantages. The buccal mucosa is a barrier, providing protection to underlying tissue, but is more permeable than other alternative routes such as the skin. Buccal films are polymeric matrices designed to be mucoadhesive properties and usually formulated with permeability enhancers to improve bioavailability. Conventionally, buccal films for biologics are manufactured by solvent casting, yet recent developments have shown the potential of hot melt extrusion, and most recently ink jet printing as promising strategies. This review aims at depicting the field of biologics-loaded mucoadhesive films as buccal drug delivery systems. In light of the literature available, the buccal epithelium is a promising route for biologics administration, which is reflected in clinical trials currently in progress, looking forward to register and commercialize the first biologic product formulated as a buccal film.
药品的主要给药途径是口服途径，但生物制品最初是作为注射剂开发的，因为它们在胃肠道中的稳定性有限且存在溶解性问题。为了避免注射，文献中发现了大量关于可绕过酶降解和首过效应的替代给药途径的研究。作为生物制品吸收的替代部位，颊部途径具有许多优点。颊黏膜是一种屏障，可为下方组织提供保护，但比皮肤等其他替代途径更具渗透性。颊膜是设计具有黏膜黏附特性的聚合物基质，通常配制有渗透促进剂以提高生物利用度。传统上，用于生物制品的颊膜是通过溶剂浇铸制造的，但最近的进展表明热熔挤出以及最近的喷墨打印作为有前景的策略具有潜力。本综述旨在描述作为颊部给药系统的载有生物制品的黏膜黏附膜领域。根据现有文献，颊上皮是生物制品给药的一个有前景的途径，这在目前正在进行的临床试验中得到了体现，期待首个制成颊膜的生物制品上市注册并商业化。
