Food and Drug Department, Viale Delle Scienze 27/a, University of Parma , Parma, Italy.
Expert Opin Drug Deliv. 2020 Oct;17(10):1345-1359. doi: 10.1080/17425247.2020.1789585. Epub 2020 Oct 16.
The oral route still represents the most popular way of administering drugs; nowadays oral administration faces new challenges, in particular with regards to the delivery of APIs that are poorly absorbed and sensitive to degradation such as macromolecules and biotechnological drugs. Nanoparticles are promising tools for the efficient delivery of these drugs to the gastrointestinal tract. Approaches and techniques for the formulation of drugs, with particular focus on the preparation of polysaccharide nanoparticles obtained by non-covalent interactions. Polysaccharide-based nanoparticulate systems offer the opportunity to address some of the issues posed by biotechnological drugs, as well as by small molecules, with problems of stability/intestinal absorption, by exploiting the capability of the polymer to establish non-covalent bonds with functional groups in the chemical structure of the API. This area of research will continue to grow, provided that these drug delivery technologies will efficaciously be translated into systems that can be manufactured on a large scale under GMP conditions. Industrial scale-up represents the biggest obstacle to overcome in view of the transformation of very promising results obtained on lab scale into medicinal products. To do that, an effort toward the simplification of the process and technologies is necessary.
口服途径仍然是给药的最常见方式；如今，口服给药面临新的挑战，特别是对于那些吸收不良且易降解的 API（如大分子和生物技术药物）的递送。纳米颗粒是将这些药物高效递送至胃肠道的有前途的工具。本文介绍了药物制剂的方法和技术，特别关注通过非共价相互作用制备多糖纳米粒子。基于多糖的纳米颗粒系统为解决生物技术药物以及小分子药物的一些问题提供了机会，这些问题包括稳定性/肠道吸收问题，可以利用聚合物与 API 化学结构中的官能团建立非共价键的能力。只要这些药物递送技术能够有效地转化为能够在 GMP 条件下大规模制造的系统，这一研究领域将继续发展。工业放大是将实验室规模获得的非常有前景的结果转化为药物的最大障碍。为此，有必要努力简化工艺和技术。
