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Liposomal delivery systems for intestinal lymphatic drug transport

View Article: PubMed Central - PubMed

ABSTRACT

Intestinal lymphatic drug delivery has been widely studied because drugs can bypass the first-pass metabolism in the liver via the lymphatic route, which increases oral bioavailability. Various lipid-based nanoparticles have been used to deliver hydrophobic drugs to the lymphatic pathway. This review focuses on the liposomal delivery systems used for intestinal lymphatic drug transport. Liposomal formulations have attracted particular attention because they can stimulate the production of chylomicrons and the incorporated drugs readily associate with enterocyte-derived chylomicrons, enhancing lymphatic drug transport. We believe that a full understanding of their contribution to intestinal drug translocation will lead to effective oral delivery with liposomal formulations.

No MeSH data available.


Two pathways (portal vein versus lymph) of oral drug transport to systemic circulation
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Fig1: Two pathways (portal vein versus lymph) of oral drug transport to systemic circulation

Mentions: There are many ways to deliver drugs into the body, including oral, pulmonary, subcutaneous, intravenous, transdermal, and nasal. Among them, oral drug delivery is particularly useful because it is convenient and comfortable for patients and thus is associated with a high rate of compliance. In other words, patients prefer drugs to be administered in oral form. However, orally administered drugs typically show low bioavailability due to their degradation by enzymes in the gastrointestinal (GI) tract, the difficulty of absorbing them in the small intestine, and the first-pass metabolism in the liver [1]. After oral administration, the drugs pass through the small intestine and enter the portal vein or intestinal lymphatic system (Fig. 1). Two main factors control the route that drugs take: molecular mass and solubility [2, 3]. Soluble, small drugs are preferentially transported via the portal vein. These drugs immediately accumulate in the liver and are then metabolized by enzymes, which lowers the drug concentration in the bloodstream. An alternative route for delivering drugs to the systemic circulation is the intestinal lymphatic pathway. Lipophilic drugs are known to be transported via the lymphatic system. The intestinal lymphatic pathway can bypass first-pass metabolism in the liver, thus increasing drug bioavailability. Furthermore, the co-administration of drugs with lipids can enhance their lymphatic transport [4]. In a postprandial state, lipid–drug conjugates and lipid-based nanoparticles have been widely studied for the delivery of lipophilic drugs via the lymphatic pathway. In this article, we highlight liposomal formulations developed to facilitate the lymphatic transport of loaded lipophilic drugs.Fig. 1


Liposomal delivery systems for intestinal lymphatic drug transport
Two pathways (portal vein versus lymph) of oral drug transport to systemic circulation
© Copyright Policy - OpenAccess
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC5120490&req=5

Fig1: Two pathways (portal vein versus lymph) of oral drug transport to systemic circulation
Mentions: There are many ways to deliver drugs into the body, including oral, pulmonary, subcutaneous, intravenous, transdermal, and nasal. Among them, oral drug delivery is particularly useful because it is convenient and comfortable for patients and thus is associated with a high rate of compliance. In other words, patients prefer drugs to be administered in oral form. However, orally administered drugs typically show low bioavailability due to their degradation by enzymes in the gastrointestinal (GI) tract, the difficulty of absorbing them in the small intestine, and the first-pass metabolism in the liver [1]. After oral administration, the drugs pass through the small intestine and enter the portal vein or intestinal lymphatic system (Fig. 1). Two main factors control the route that drugs take: molecular mass and solubility [2, 3]. Soluble, small drugs are preferentially transported via the portal vein. These drugs immediately accumulate in the liver and are then metabolized by enzymes, which lowers the drug concentration in the bloodstream. An alternative route for delivering drugs to the systemic circulation is the intestinal lymphatic pathway. Lipophilic drugs are known to be transported via the lymphatic system. The intestinal lymphatic pathway can bypass first-pass metabolism in the liver, thus increasing drug bioavailability. Furthermore, the co-administration of drugs with lipids can enhance their lymphatic transport [4]. In a postprandial state, lipid–drug conjugates and lipid-based nanoparticles have been widely studied for the delivery of lipophilic drugs via the lymphatic pathway. In this article, we highlight liposomal formulations developed to facilitate the lymphatic transport of loaded lipophilic drugs.Fig. 1

View Article: PubMed Central - PubMed

ABSTRACT

Intestinal lymphatic drug delivery has been widely studied because drugs can bypass the first-pass metabolism in the liver via the lymphatic route, which increases oral bioavailability. Various lipid-based nanoparticles have been used to deliver hydrophobic drugs to the lymphatic pathway. This review focuses on the liposomal delivery systems used for intestinal lymphatic drug transport. Liposomal formulations have attracted particular attention because they can stimulate the production of chylomicrons and the incorporated drugs readily associate with enterocyte-derived chylomicrons, enhancing lymphatic drug transport. We believe that a full understanding of their contribution to intestinal drug translocation will lead to effective oral delivery with liposomal formulations.

No MeSH data available.