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Solid Sirolimus Self-microemulsifying Drug Delivery System: Development and Evaluation of Tablets with Sustained
Chun Tao1, Xu Wen1,2, Qian Zhang2
1Department of Pharmacy, Fuzong Clinical Medical College of Fujian Medical University (Fuzhou General Hospital), Fuzhou 350025, PR China.
Iranian Journal of Pharmaceutical Research : IJPR
|March 19, 2020
Summary
This study developed novel sirolimus (SRL) tablets using self-microemulsifying drug delivery systems (SMEDDS) for sustained release. These SMEDDS tablets offer improved safety and pharmacokinetic profiles compared to conventional formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Sirolimus (SRL) exhibits a narrow therapeutic range, limiting its clinical use as an immunosuppressant.
- Enhancing SRL solubility and controlling its release are crucial for improving safety and efficacy.
Purpose of the Study:
- To develop sustained-release sirolimus (SRL) tablets using a self-microemulsifying drug delivery system (SMEDDS).
- To optimize the formulation and investigate the in vitro and in vivo performance of SRL-SMEDDS tablets.
Main Methods:
- SRL solubility was enhanced using SMEDDS, adsorbed onto microcrystalline cellulose (MCC).
- Sustained release was achieved by incorporating hydroxypropyl methylcellulose (HPMC) into tablets, with formulation optimization via single factor and orthogonal designs.
- In vitro release profiles were studied under various conditions, and release kinetics were determined.
- Pharmacokinetic studies were conducted in beagle dogs.
Main Results:
- The optimal tablet formulation contained 10% HPMC 100lv and 5% HPMC K4M.
- In vitro studies indicated HPMC erosion as the release mechanism.
- Pharmacokinetic analysis in beagle dogs demonstrated bioequivalence to commercial tablets, with a lower Cmax and larger Tmax, suggesting reduced peak-dose toxicity.
Conclusions:
- SRL-SMEDDS tablets represent a promising drug delivery system for achieving sustained release of sirolimus.
- This approach enhances SRL solubility and provides a favorable pharmacokinetic profile for improved clinical application.
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