Effects of lipid class and lipid vehicle volume on the intestinal lymphatic transport of DDT
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Structured edible lipid-based particle systems for oral drug-delivery
2022, Biotechnology AdvancesNatural sesame oil is superior to pre-digested lipid formulations and purified triglycerides in promoting the intestinal lymphatic transport and systemic bioavailability of cannabidiol
2021, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :It has been reported previously that lipid-based formulations can increase the intraluminal solubility of lipophilic drugs and enhance the drug absorption. Moreover, oral administration of highly lipophilic drugs in lipid-based formulations containing long-chain triglycerides or long-chain fatty acids results in intestinal lymphatic transport and therefore avoids hepatic first-pass metabolism [9,35]. CBD is a highly lipophilic drug which has high affinity to both rat and human chylomicrons and extensive intestinal lymphatic transport when administered orally with a long-chain triglyceride vehicle (sesame oil) [16,17].
A Retrospective Biopharmaceutical Analysis of >800 Approved Oral Drug Products: Are Drug Properties of Solid Dispersions and Lipid-Based Formulations Distinctive?
2020, Journal of Pharmaceutical SciencesCitation Excerpt :The “spring and parachute” analogy applies here to the generation and prolongation of supersaturation where the “spring” involves the self-emulsifying properties of the LBF, incorporating the solubilised active substance 33, while “parachute” refers to formulation additives which increase stability, reducing drug precipitation in vivo34 (Fig. 2). LBFs are also biopharmaceutically advantageous regarding impact on intestinal permeability,35 metabolism36 and lymphatic transport.37,38 Additionally, from a pharmaceutical manufacture standpoint, once acceptable manufacturing equipment is in place, large scale manufacture of LBFs is relatively low risk and less technologically demanding which can usually be completed on a smaller scale than other delivery technologies.15,39
Evaluating hexabromocyclododecane (HBCD) toxicokinetics in humans and rodents by physiologically based pharmacokinetic modeling
2019, Food and Chemical ToxicologyPromoting intestinal lymphatic transport targets a liver-X receptor (LXR) agonist (WAY-252,623) to lymphocytes and enhances immunomodulation
2019, Journal of Controlled ReleaseCitation Excerpt :WAY-252,623 is a highly lipophilic drug candidate with physicochemical properties that are consistent with the potential to be transported from the intestine via the lymph following oral delivery. Charman and Stella initially proposed that intestinal lymphatic transport following oral delivery is likely to be substantial for highly lipophilic drugs (Log D > 5, lipid solubility >50 mg/mL) that associate with intestinal lipoproteins [34]. This suggestion was made based on the realisation that the flow rate of blood through the intestinal blood capillaries and portal vein is substantially higher (~500-fold) than the flow rate of lymph through the intestinal lymphatics, and that 1% of lymph fluid consists of lipid.
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Present address: Sterling-Winthrop Research Institute, Rensselaer, NY 12144, U.S.A.