O'Driscoll Caitriona M
Department of Pharmaceutics and Pharmaceutical Technology, University of Dublin, Trinity College, Ireland.
Eur J Pharm Sci. 2002 Jun;15(5):405-15. doi: 10.1016/s0928-0987(02)00051-9.
The current state of the art of intestinal lymphatic transport is given by reviewing the more recent publications, which have utilized lipid-based vehicles. The results published often show variable trends depending on, the design of the vehicle, the components used, the physicochemical properties of the drug, the animal model and experimental techniques, these variables often make direct comparisons difficult. Traditionally intestinal lymphatic delivery has been expressed as a percentage of the dose transported in the lymph. Using this parameter results obtained to date, with lipid-based vehicles, are somewhat disappointing maximising at approximately 20-30%, for highly lipophilic compounds including DDT and halofantrine (Hf). Recent data, monitoring Hf, in a fed versus fasted dog study, have shown that a higher degree of lymphatic transport is possible (>50% dose) in the postprandial state, this study should result in stimulating renewed interest in the potential of achieving significant levels of lymphatic targeting. Although some relevant features controlling lymphatic transport have been identified over the years a deeper appreciation of all the mechanisms, which is vital for therapeutic exploitation of lymphatic transport, is still unrealized. This review analyses the success and limitations of a formulation approach using lipid-based vehicles and highlights potential areas for further research.
通过回顾最近利用脂质载体的出版物，介绍了肠道淋巴转运的当前技术水平。发表的结果往往显示出不同的趋势，这取决于载体的设计、所用的成分、药物的物理化学性质、动物模型和实验技术，这些变量常常使直接比较变得困难。传统上，肠道淋巴递送是以淋巴中转运剂量的百分比来表示的。使用这个参数，迄今为止用脂质载体获得的结果有些令人失望，对于包括滴滴涕和卤泛群（Hf）在内的高度亲脂性化合物，最大转运率约为20%-30%。最近在一项喂食与禁食犬类研究中监测卤泛群的数据表明，在餐后状态下，更高程度的淋巴转运是可能的（>50%剂量），这项研究应该会激发人们对实现显著水平淋巴靶向潜力的新兴趣。尽管多年来已经确定了一些控制淋巴转运的相关特征，但对于所有机制的更深入理解（这对于淋巴转运的治疗应用至关重要）仍未实现。本综述分析了使用脂质载体的制剂方法的成功与局限性，并强调了进一步研究的潜在领域。
