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Updated: Apr 12, 2026
08:38
Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
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A Novel Slowly Self-Emulsifying Drug Delivery System: Prolonged Systemic Exposure of Tacrolimus With Reduced Risks of
Kohei Yamada1, Keiya Sonobe1, Akihisa Miura1
1Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Biopharmaceutics & Drug Disposition
|April 10, 2026
Summary
A new slowly self-emulsifying drug delivery system (SL-SEDDS) for tacrolimus (TAC) offers prolonged systemic exposure and reduced kidney toxicity. This innovative formulation controls drug absorption for safer and more effective tacrolimus medication.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Tacrolimus (TAC) is a vital immunosuppressant with a narrow therapeutic index.
- Nephrotoxicity is a significant dose-limiting side effect of tacrolimus therapy.
- Standard self-emulsifying drug delivery systems (SEDDS) can lead to rapid drug absorption and potential toxicity.
Purpose of the Study:
- To design and characterize a novel slowly self-emulsifying drug delivery system (SL-SEDDS) for tacrolimus (TAC).
- To evaluate the potential of SL-SEDDS to achieve long-lasting systemic exposure of TAC.
- To assess the impact of SL-SEDDS on reducing TAC-induced nephrotoxicity.
Main Methods:
- Tacrolimus-loaded SEDDS were prepared and then semi-solidified with Geleol to create SL-SEDDS.
- Physicochemical and biopharmaceutical properties, including dissolution profiles in simulated gastric and intestinal fluids, were evaluated.
- Pharmacokinetic studies in rats were conducted to compare bioavailability, maximum plasma concentration, and mean residence time.
- Nephrotoxicity was assessed in a rat model by measuring blood urea nitrogen levels after administration.
Main Results:
- SL-SEDDS demonstrated slower and sustained drug release compared to conventional SEDDS, dependent on Geleol content.
- SL-SEDDS achieved similar oral bioavailability to SEDDS but with a 32% reduction in maximum plasma concentration.
- Mean residence time was significantly prolonged with SL-SEDDS.
- SL-SEDDS treatment attenuated blood urea nitrogen elevation by 33% in a rat model of acute kidney injury, indicating reduced nephrotoxicity.
Conclusions:
- SL-SEDDS is a promising formulation for controlling the oral absorption of tacrolimus.
- This novel drug delivery system can enhance the safety profile of tacrolimus by reducing nephrotoxicity.
- SL-SEDDS offers a potential strategy for achieving effective and safer tacrolimus-based therapies.
Keywords:
nephrotoxicitypharmacokinetic controlslowly self‐emulsifying drug delivery systemtacrolimusMore Related Videos
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