Martins Susana, Sarmento Bruno, Ferreira Domingos C, Souto Eliana B
Department of Pharmaceutical Technology, Faculty of Pharmacy University of Porto, Porto, Portugal.
Int J Nanomedicine. 2007;2(4):595-607.
This paper highlights the importance of lipid-based colloidal carriers and their pharmaceutical implications in the delivery of peptides and proteins for oral and parenteral administration. There are several examples of biomacromolecules used nowadays in the therapeutics, which are promising candidates to be delivered by means of liposomes and lipid nanoparticles, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). Several production procedures can be applied to achieve a high association efficiency between the bioactives and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. Generally, this can lead to improved bioavailability, or in case of oral administration a more consistent temporal profile of absorption from the gastrointestinal tract. Advantages and drawbacks of such colloidal carriers are also pointed out. This article describes strategies used for formulation of peptides and proteins, methods used for assessment of association efficiency and practical considerations regarding the toxicological concerns.
本文强调了基于脂质的胶体载体及其在肽和蛋白质口服及肠胃外给药中的药学意义。目前在治疗学中使用的生物大分子有多个实例,它们有望通过脂质体和脂质纳米颗粒(如固体脂质纳米颗粒(SLN)和纳米结构脂质载体(NLC))进行递送。根据生物活性物质和载体的物理化学性质以及所应用的生产工艺,可以采用多种生产程序来实现生物活性物质与载体之间的高结合效率。一般来说,这可以提高生物利用度,或者在口服给药的情况下,使胃肠道吸收的时间曲线更加一致。还指出了此类胶体载体的优缺点。本文描述了用于肽和蛋白质制剂的策略、评估结合效率的方法以及有关毒理学问题的实际考虑因素。