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Pharm Res. 2011 Jan;28(1):107-16. doi: 10.1007/s11095-010-0123-9. Epub 2010 Mar 31.
The purpose of this research was to examine the pharmacokinetics (PK) of drug uptake for microneedle-based intradermal (ID) delivery of several classes of protein drugs compared to standard subcutaneous (SC) administration.
Systemic absorption kinetics of various proteins were analyzed following microneedle-based ID delivery and standard injection methods in the swine model. Comparative PK data were determined using standard non-compartmental techniques based on blood serum levels.
Delivery of proteins using microneedles resulted in faster systemic availability, measured via t(max,) and increased maximal drug concentration, C(max,) over SC delivery for all proteins tested. Some agents also exhibited increased bioavailability for the ID route. Imaging studies using reporter dyes showed rapid lymphatic-mediated uptake.
Microneedle delivery is applicable to a wide variety of protein drugs and is capable of effective parenteral administration of therapeutic drug dosages. This delivery route alters absorption kinetics via targeting a tissue bed better perfused with lymphatic and blood vessels than the SC space. Microneedle delivery may afford various advantages, including a robust method to increase the absorption rate and bioavailability of proteins that have been challenging to deliver at therapeutic levels or with physiologically relevant profiles.
本研究旨在考察与标准皮下（SC）给药相比，基于微针的皮内（ID）给药对几类蛋白药物的药物摄取的药代动力学（PK）。
在猪模型中，通过基于微针的 ID 给药和标准注射方法分析各种蛋白质的全身吸收动力学。比较 PK 数据是使用基于血清水平的标准非房室技术确定的。
与 SC 给药相比，所有测试的蛋白质通过微针给药导致更快的全身可用性，通过 t(max,) 测量，并增加最大药物浓度 C(max,)。一些药物在 ID 途径下也表现出更高的生物利用度。使用报告染料的成像研究表明，快速的淋巴介导摄取。
微针给药适用于多种蛋白质药物，能够有效进行治疗性药物剂量的肠胃外给药。这种给药途径通过靶向具有更好的淋巴和血管灌注的组织床，改变了吸收动力学，而不是 SC 空间。微针给药可能具有多种优势，包括增加具有挑战性的治疗水平或具有生理相关特征的蛋白质的吸收速率和生物利用度的稳健方法。
