4.5 Article

Lymphatic transport system to circumvent hepatic metabolism for oral delivery of lipid-based nanocarriers

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ELSEVIER
DOI: 10.1016/j.jddst.2021.102934

关键词

Lipid-based nanocarriers; Hepatic first-pass metabolism; Lymphatic transport; Presystemic metabolism; Oral delivery of nanoparticles; Research models

资金

  1. Department of Science and Technology, Ministry of Science and Technology, Government of India [IFA18-ENG266, DST/INSPIRE/04/2018/000991]

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The oral route of administration for lipid-based nanocarriers is crucial for improving the bioavailability of drugs with low bioavailability. Through lymphatic transport, these drug delivery systems can enhance oral bioavailability and therapeutic activity. Avoiding first-pass metabolism can lead to significant improvements in oral bioavailability. Further research, including detailed clinical studies, is needed to explore the safety and efficacy of various lipid-based nanocarriers.
The oral route of administration for lipid-based nanocarriers is of immense importance for the drugs having low bioavailability because of extensive first-pass metabolism. These drug delivery systems have reportedly improved oral bioavailability via lymphatic transport. The solubility issues of a drug are addressed by directly encapsu-lating them into the lipid. Subsequently, various lipid-based nanocarriers have enhanced the therapeutic activity of drugs via lymphatic transport with negligible side effects. Animal studies have depicted significant improvement in the oral bioavailability of drugs by avoiding first-pass metabolism. A detailed clinical study for large animals is needed to investigate the safety and efficacy of various lipid-based nanocarriers. In this review, we have described the potential and pertinence of the oral route of administration for lipid-based nanocarriers. The importance of lymphatic transport systems as a liver bypass transport system is also described herein. Various carriers such as liposomes, nanostructured lipid carriers, lipid-drug conjugate, etc. are discussed in brief with recent examples. The transport of lipids and absorption of drugs across the lymphatic pathway and various factors associated with nanocarriers affecting the lymph node targeting are also highlighted. Various in vivo and in vitro research models along with a brief focus on in silico prediction of the lymphatic transfer are described. The insights on future perspectives with an emphasis on the translational barriers may help the researchers working in this area.

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