Hoshi University, Department of Drug Delivery Research, Ebara, Shinagawa-ku, Tokyo, Japan.
Expert Opin Drug Deliv. 2011 Nov;8(11):1469-79. doi: 10.1517/17425247.2011.615829. Epub 2011 Sep 6.
Recently, pharmacotherapy has advanced extensively, but there are still many refractory diseases which cannot be solved fully by existing therapeutic agents. Therefore, alternative medicine and health foods are now attracting much attention, for example, lactoferrin (LF): a multifunctional glycoprotein. As LF is non-toxic and low-cost, its application in healthcare and therapeutics is expected to be widespread.
In this review, LF's general basic features are described. The interaction of LF with its receptors activates the immune system, including cytokine production and balance. In particular, the immune activation of orally administered LF is considered as a new strategy for the treatment of refractory diseases, such as inflammatory bowel disease, virus infection and tumor metastasis. Also mentioned are the problems associated with the use of LF. As LF is degraded rapidly in the body due to enzymatic hydrolysis, high amounts or frequent dosing is required; an appropriate delivery system may improve these problems and increase its efficiency.
Chemical modifications, such as PEGylation, can enhance the stability of LF in the body, resulting in increased efficacy. Also, liposomes and enteric or microparticulate formulations can promote the function of LF in oral administration due to target site delivery and protection of LF from enzymatic hydrolysis. These delivery systems are expected to improve the utility of LF.
近年来,药物治疗有了很大的进展,但仍有许多难治性疾病无法通过现有治疗药物完全解决。因此,替代医学和保健品现在引起了广泛关注,例如乳铁蛋白(LF):一种多功能糖蛋白。由于 LF 无毒且成本低,预计其在保健和治疗中的应用将很广泛。
本文描述了 LF 的一般基本特征。LF 与其受体的相互作用激活了免疫系统,包括细胞因子的产生和平衡。特别是,口服 LF 的免疫激活被认为是治疗难治性疾病(如炎症性肠病、病毒感染和肿瘤转移)的一种新策略。还提到了与 LF 使用相关的问题。由于 LF 在体内因酶解而迅速降解,因此需要大量或频繁给药;适当的给药系统可以改善这些问题并提高其效率。
化学修饰,如聚乙二醇化,可以提高 LF 在体内的稳定性,从而提高疗效。此外,由于靶向递药和保护 LF 免受酶解,脂质体和肠溶或微粒制剂可以促进 LF 在口服给药中的作用。这些给药系统有望提高 LF 的实用性。