Overcoming the intestinal barrier: A look into targeting approaches for improved oral drug delivery systems.,Journal of Controlled Release

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Overcoming the intestinal barrier: A look into targeting approaches for improved oral drug delivery systems.
Journal of Controlled Release ( IF 10.5 ) Pub Date : 2020-04-08 , DOI: 10.1016/j.jconrel.2020.04.006
Yining Xu ₁ , Neha Shrestha ₁ , Véronique Préat ₁ , Ana Beloqui ₁

Affiliation

Oral drug administration is one of the most preferred and simplest routes among both patients and formulation scientists. Nevertheless, orally delivery of some of the most widely used therapeutic agents (e.g., anticancer drugs, peptides, proteins and vaccines) is still a major challenge due to the limited oral bioavailability associated with them. The poor oral bioavailability of such drugs is attributed to one or many factors, such as poor aqueous solubility, poor permeability, and enzymatic degradation. Various technological strategies (such as permeation enhancers, prodrugs and nanocarriers) have been developed to enhance the bioavailability of these drugs after oral administration. Among the different approaches, advanced and innovative drug delivery systems, especially targeting-based strategies, have garnered tremendous attention. Furthermore, the presence of numerous types of cells and solute carrier transporters throughout the gastrointestinal tract represents numerous potential targeting sites for successful oral delivery that have not yet been exploited for their full potential. This review describes different targeting strategies towards different targeting sites in the gastrointestinal tract. Additionally, exciting improvements in oral drug delivery systems with different targeting strategies (e.g., M cells for oral vaccination and L cells for type 2 diabetes mellitus) are also discussed.

中文翻译：

克服肠道障碍：旨在研究改善口服药物递送系统的靶向方法。

口服药物给药是患者和制剂科学家中最优选和最简单的途径之一。然而，由于与它们相关的有限的口服生物利用度，一些最广泛使用的治疗剂（例如，抗癌药，肽，蛋白质和疫苗）的口服递送仍然是主要的挑战。这类药物的口服生物利用度差归因于一种或多种因素，例如水溶性差，渗透性差和酶促降解。已经开发出各种技术策略（例如渗透促进剂，前药和纳米载体）以增强口服给药后这些药物的生物利用度。在不同的方法中，先进和创新的药物输送系统，尤其是基于目标的策略，已经引起了极大的关注。此外，遍及整个胃肠道的多种类型的细胞和溶质载体转运蛋白的存在代表了许多成功口服给药的潜在靶向位点，尚未充分发挥其全部潜能。这篇综述描述了针对胃肠道中不同靶向部位的不同靶向策略。另外，还讨论了具有不同靶向策略的口服药物输送系统的令人兴奋的改进（例如，用于口服疫苗的M细胞和用于2型糖尿病的L细胞）。这篇综述描述了针对胃肠道中不同靶向部位的不同靶向策略。另外，还讨论了具有不同靶向策略的口服药物输送系统的令人兴奋的改进（例如，用于口服疫苗的M细胞和用于2型糖尿病的L细胞）。这篇综述描述了针对胃肠道中不同靶向部位的不同靶向策略。另外，还讨论了具有不同靶向策略的口服药物输送系统的令人兴奋的改进（例如，用于口服疫苗的M细胞和用于2型糖尿病的L细胞）。

更新日期：2020-04-08

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