经皮途径传递蛋白质药物。
Passive delivery of protein drugs through transdermal route.
机构信息
a Department of Pharmaceutical Sciences, Pharmaceutics Research Projects Laboratory , Dr. Hari Singh Gour Central University , Sagar , India.
b Institute of Pharmaceutical Research, GLA University , Mathura , India.
出版信息
Artif Cells Nanomed Biotechnol. 2018;46(sup1):472-487. doi: 10.1080/21691401.2018.1430695. Epub 2018 Jan 29.
Skin is the largest external organ in the human body but its use for therapeutic purposes has been minimal. Stratum corneum residing on the uppermost layer of the skin provides a tough barrier to transport the drugs across the skin. Very small group of drugs sharing Lipinski properties, i.e. drugs having molecular weight not larger than 500 Da, having high lipophilicity and optimum polarity are fortunate enough to be used on skin therapeutics. But, at a time where modern therapeutics is slowly shifting from use of small molecular drugs towards the use of macromolecular therapeutic agents such as peptides, proteins and nucleotides in origin, skin therapeutics need to be evolved accordingly to cater the delivery of these agents. Physical technologies like iontophoresis, laser ablation, micro-needles and ultrasound, etc. have been introduced to enhance skin permeability. But their success is limited due to their complex working mechanisms and involvement of certain irreversible skin damage in some or other way. This review therefore explores the delivery strategies for transport of mainly peptide and protein drugs that do not involve any injuries (non-invasive) to the skin termed as passive delivery techniques. Chemical enhancers, nanocarriers, certain biological peptides and miscellaneous approaches like prodrugs are also thoroughly reviewed for their applications in protein delivery.
皮肤是人体最大的外部器官,但它在治疗中的应用却很少。位于皮肤最上层的角质层为药物穿过皮肤提供了一个坚固的屏障。极少数具有 Lipinski 性质的药物,即分子量不超过 500Da、具有高亲脂性和最佳极性的药物,有幸被用于皮肤治疗。但是,在现代治疗学正逐渐从使用小分子药物转向使用源自肽、蛋白质和核苷酸等大分子治疗剂的时代,皮肤治疗学需要相应地发展,以满足这些制剂的输送需求。已经引入了物理技术,如离子电渗、激光烧蚀、微针和超声波等,以增强皮肤通透性。但由于它们复杂的工作机制以及在某种程度上涉及某些不可逆转的皮肤损伤,它们的成功受到限制。因此,本综述探讨了主要用于输送肽和蛋白质药物的输送策略,这些药物不会对皮肤造成任何损伤(非侵入性),称为被动输送技术。还对化学增强剂、纳米载体、某些生物肽以及前药等各种方法进行了深入综述,以了解它们在蛋白质输送中的应用。