AI Article Synopsis
- Sirolimus (SRL) faces challenges as an immunosuppressant due to its low water solubility and narrow therapeutic window, but a self-microemulsifying drug delivery system (SMEDDS) improves its solubility.
- By optimizing the SMEDDS formulation, notably adding 0.20% citric acid, SRL's stability under harsh conditions (high temperature, humidity, and light) was enhanced.
- The final product, SMEDDS absorbed by microcrystalline cellulose mixed with hydroxypropyl methylcellulose to create tablets, achieved a sustained release of SRL over 12 hours, showing promise for water-insoluble drugs.
Article Abstract
The application of sirolimus (SRL) as immunosuppressive agent is hampered by its poor water solubility and narrow therapeutic range. The self-microemulsifying drug delivery system (SMEDDS) succeeded in improving the solubility of SRL in our previous work. In this study, the formulation of the SMEDDS was further optimized by investigating the influence of the excipients including the media, antioxidant and organic acid. It was demonstrated that addition of 0.20% of citric acid in SMEDDS most efficiently promoted the stability of SRL under high temperature (40±2°C), high humidity (relative humidity 90±5%) or strong light irradiation (4500±500lx). SMEDDS absorbed by microcrystalline cellulose (MCC) was mixed with hydroxypropyl methylcellulose (HPMC) to prepare tablets. The optimal formulation composed of 15% of HPMC 100 LV with hardness of 120N, which had a sustained release of 12h. Results of X-ray powder diffraction and differential scanning calorimetry demonstrated that SRL in the tablets was in amorphous or molecularly dispersed state. The SMEDDS-tablets presented as promising substrates for water insoluble drugs with enhanced stability and extended release.
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| http://dx.doi.org/10.1016/j.ijpharm.2016.09.035 | DOI Listing |
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