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Purpose
To provide a comprehensive and up-to-date overview focusing on the extent of lymphatic transport of drugs following intestinal absorption and to summarize available data on the impact of molecular weight, lipophilicity, formulation and prandial state.
Methods
Literature was searched for
in vivo
studies quantifying extent of lymphatic transport of drugs after enteral dosing. Pharmacokinetic data were extracted and summarized. Influence of molecular weight, log P, formulation and prandial state was analyzed using relative bioavailability via lymph (F
RL
) as the parameter for comparison. The methods and animal models used in the studies were also summarized.
Results
Pharmacokinetic data on lymphatic transport were available for 103 drugs. Significantly higher F
RL
[median (IQR)] was observed in advanced lipid based formulations [54.4% (52.0)] and oil solutions [38.9% (60.8)] compared to simple formulations [2.0% (27.1)],
p
< 0.0001 and
p
= 0.004, respectively. Advanced lipid based formulations also provided substantial F
RL
in drugs with log P < 5, which was not observed in simple formulations and oil solutions. No relation was found between F
RL
and molecular weight. There were 10 distinct methods used for
in vivo
testing of lymphatic transport after intestinal absorption so far.
Conclusion
Advanced lipid based formulations provide superior ability to increase lymphatic absorption in drugs of various molecular weights and in drugs with moderate to low lipophilicity.