CBQF - Centro de Biotecnologia e Química Fina - Laboratório Associado, Escola Superior de Biotecnologia, Universidade Católica Portuguesa/Porto, Rua Arquiteto Lobão Vital Apartado 2511, 4202-401 Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra 1317, 4585-116 Gandra-PRD, Portugal.
CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra 1317, 4585-116 Gandra-PRD, Portugal; REQUIMTE, Department of Chemical Sciences - Applied Chemistry Lab, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal.
J Control Release. 2015 Aug 10;211:63-73. doi: 10.1016/j.jconrel.2015.05.258. Epub 2015 May 13.
Therapeutic proteins and peptides demonstrate unique, peerless, pharmacological characteristics such as high specificity to receptors and superior biological mimicking of physiological mechanisms, resulting in a better therapeutic index compared to conventional chemical-derived drugs. However, proteins also present inherent bioavailability limitations. Thus, this paper proposes several effective tools to improve protein/peptide drugs stability, permeability and pharmacokinetics with special emphasis on oral polymeric films as oral delivery platforms. Indeed, oral films present inherent characteristics that can greatly enhance biological performance of proteins and peptides and patient compliance along with other advantages that are critically discussed in this review. A rational choice of excipients addressed in and manufacture processes are also focused. In addition, possible toxicity issues to be overtaken and critical analysis regarding current market tendencies respecting oral films and protein/peptides along with future prospects are disclosed.
治疗性蛋白和肽具有独特的、无与伦比的药理学特性，如对受体的高度特异性和对生理机制的优越生物模拟性，与传统的化学衍生药物相比，具有更好的治疗指数。然而，蛋白质也存在固有的生物利用度限制。因此，本文提出了几种有效的工具来提高蛋白质/肽类药物的稳定性、渗透性和药代动力学特性，特别强调了口服聚合物薄膜作为口服递药平台。事实上，口服薄膜具有内在的特性，可以极大地增强蛋白质和肽类的生物性能和患者的顺应性，以及本文中讨论的其他优点。本文还重点讨论了赋形剂的合理选择和制造工艺。此外，还揭示了可能出现的毒性问题，以及对口服薄膜和蛋白质/肽类药物的当前市场趋势的批判性分析和未来展望。
