ArticlePharmaceutical research1995
Physicochemical, pharmacokinetic and pharmacodynamic evaluation of liposomal tacrolimus (FK 506) in rats.
Article in Pharmaceutical research, 1995. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
5 citing papers in PubMed, 28 citations in OpenAlex.
- Effect of stabilizer on the maximum degree and extent of supersaturation and oral absorption of tacrolimus made by ultra-rapid freezing.Pharmaceutical research · 2008Article
- Nano-liposomal dry powder inhaler of tacrolimus: preparation, characterization, and pulmonary pharmacokinetics.International journal of nanomedicine · 2007Article
- Mechanisms of clinically relevant drug interactions associated with tacrolimus.Clinical pharmacokinetics · 2002Review
- The pharmacokinetics of water-in-oil-in-water-type multiple emulsion of a new tacrolimus formulation.Lipids · 1997Article
- Clinical pharmacokinetics of tacrolimus.Clinical pharmacokinetics · 1995Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTacrolimus (FK 506) is a new potent immunosuppressant. Because of poor water solubility, the conventional intravenous dosage forms of FK 506 (C-FK 506) contain surfactants such as HCO-60 which may cause adverse effects. We sought a liposomal formulation of FK 506 (L-FK 506) containing endogenous phospholipids to target drug to the spleen, a major organ controlling the immune system.
methodsL-FK 506, consisting of 0.1 micron diameter vesicles of phosphatidylcholine and phosphatidylglycerol (molar ratio 9:1) and 7.5 mole% drug, was evaluated for in vitro stability. The intravenous disposition profile, spleen distribution, and immunosuppression of L-FK 506 was compared with that of C-FK 506 in the rat after single doses of 0.3 mg/kg.
resultsThe L-FK 506 showed good in vitro stability. L-FK 506 exhibited an increased volume of distribution at steady-state (Vss) (from 3.41 to 14.71 L/kg) and increased mean residence time (MRT) (from 2.83 to 16.07 hr). FK 506 concentrations in spleen were increased by 40% at 10 hr after administration of the liposomal formulation. The pharmacodynamics of L-FK 506, evaluated by the extent of inhibition of splenocyte proliferation, was comparable to that of C-FK 506.
conclusionsLiposomal FK 506 may be an improved dosage form for parenteral use.
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