Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.
Adv Drug Deliv Rev. 2012 May 1;64(6):531-9. doi: 10.1016/j.addr.2011.12.014. Epub 2012 Jan 4.
During the past few decades, the novel biotherapeutic agents such as peptides and proteins have been contributed to the treatment of several diseases. However, their oral absorption is significantly limited due to their poor delivery through the intestinal mucosa. Therefore, the feasible approaches are needed for improving the oral bioavailability of biodrugs. Recently, cell-penetrating peptides (CPPs) such as HIV-1 Tat, penetratin and oligoarginine are considered as a useful tool for the intracellular delivery of therapeutic macromolecules. Hence, it was expected that the ability of CPPs may be applicable to enhance the absorption of biodrugs through intestinal epithelial membrane. CPPs are likely to become powerful tools for overcoming the low permeability of therapeutic peptides and proteins through the intestinal membrane, the major barrier to their oral delivery. Further advantage of this promising strategy is that this successful intestinal absorption could be achieved by more convenient methodology, coadministration of CPP with drugs via intermolecular interaction among them. Hereafter, the further establishment of delivery system based on CPPs is required to realize the development of the oral forms of therapeutic peptides and proteins. The aim here is to introduce our vision focusing on oral biodrug delivery by the use of CPPs as potential peptide carrier in order to provide new information in the design and development of new oral delivery systems for novel biotherapeutics.
在过去几十年中，新型生物治疗剂如肽和蛋白质已被用于治疗多种疾病。然而，由于它们在肠道黏膜中的传递较差，其口服吸收受到显著限制。因此，需要寻找可行的方法来提高生物药物的口服生物利用度。最近，细胞穿透肽（CPPs）如 HIV-1 Tat、 penetratin 和寡精氨酸被认为是用于治疗性大分子细胞内传递的有用工具。因此，人们期望 CPPs 的能力可适用于通过肠上皮细胞膜增强生物药物的吸收。CPPs 可能成为克服治疗性肽和蛋白质通过肠膜（口服递送的主要障碍）低渗透性的强大工具。该有前途策略的另一个优点是，通过 CPP 与药物之间的分子间相互作用，以更方便的方法将 CPP 与药物共同给药，可实现药物在肠道中的成功吸收。此后，需要进一步建立基于 CPP 的递送系统，以实现治疗性肽和蛋白质口服剂型的开发。本文旨在介绍我们的愿景，即通过使用 CPP 作为潜在的肽载体，专注于口服生物药物递送，为新型生物治疗剂的新型口服递送系统的设计和开发提供新的信息。
