弹性体
胶囊
材料科学
生物医学工程
药物输送
生物利用度
高分子
吸收(声学)
生物物理学
口服
聚合物
纳米技术
剂型
箔法
体内
小肠
化学
药理学
医学
生物化学
色谱法
复合材料
生物
生物技术
植物
作者
Jørgen Jørgensen,Lasse Højlund Eklund Thamdrup,Khorshid Kamguyan,Line Hagner Nielsen,Hanne Mørck Nielsen,Anja Boisen,Thomas Rades,Anette Müllertz
标识
DOI:10.1016/j.jconrel.2020.10.024
摘要
Delivering macromolecular drugs, e.g. peptides, to the systemic circulation by oral administration is challenging due to their degradation in the gastrointestinal tract and low transmucosal permeation. In this study, the concept of an oral delivery device utilizing an elastomeric material is presented with the potential of increasing the absorption of peptides, e.g. insulin. Absorption enhancement in the intestine is proposed as a result of self-unfolding of a polydimethylsiloxane foil upon release from enteric coated capsules. A pH-sensitive polymer coating prevents capsule disintegration until arrival in the small intestine where complete unfolding of the elastomeric foil ensures close contact with the intestinal mucosa. Foils with close-packed hexagonal compartments for optimal drug loading are produced by casting against a deep-etched silicon master. Complete unfolding of the foil upon capsule disintegration is verified in vitro and the insulin release profile of the final delivery device confirms insulin protection at gastric pH. In vivo performance is evaluated with the outcome of quantifiable plasma insulin concentrations in all rats receiving duodenal administration of the novel delivery device. By taking advantage of elastomeric material properties for drug delivery, this approach might serve as inspiration for further development of commercially viable biocompatible devices for oral delivery of macromolecules.
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