Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexateopen access
- Kim, Dong Shik; Cho, Jung Hyun; Park, Jong Hyuck; Kim, Jung Suk; Song, Eon Soo; Kwon, Jaewook; Giri, Bhupendra Raj; Jin, Sung Giu; Kim, Kyeong Soo; Choi, Han-Gon; Kim, Dong Wuk
- Issue Date
- DOVE MEDICAL PRESS LTD
- methotrexate; solid SMEDDS; solubility; bioavailability; photostability
- INTERNATIONAL JOURNAL OF NANOMEDICINE, v.14, pp.4949 - 4959
- Journal Title
- INTERNATIONAL JOURNAL OF NANOMEDICINE
- Start Page
- End Page
- Purpose: The objective of this study was to exploit a novel methotrexate (MTX)-loaded solid self-microemulsifying drug delivery system (SMEDDS) with enhanced bioavailability and photostability. Materials and methods: The optimized liquid SMEDDS was composed of castor oil, Tween (R) 80, and Plurol (R) diisostearique at a voluminous ratio of 27:63:10. The solid SMEDDS was formulated by spray drying liquid SMEDDS with the solid carrier (calcium silicate). Particle size analyzer, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared (FTIR) spectroscopy experiments characterized the physiochemical properties of the MTX-loaded solid SMEDDS. These properties include a z-average diameter of emulsion around 127 nm and the amorphous form of the solid SMEDDS. Furthermore, their solubility, dissolution, and pharmacokinetics in Sprague-Dawley rats were analyzed in comparison with the MTX powder. Results: The final dissolution rate and required time for complete release of solid SMEDDS were 1.9-fold higher and 10 min shorter, respectively, than those of MTX powder. Pharmacokinetic analysis demonstrated 2.04- and 3.41-fold increments in AUC and C-max, respectively in comparison to MTX powder. The AUC and C-max were significantly increased in solid SMEDDS. Finally, the photostability studies revealed the substantially enhanced photostability of the MTX-loaded SMEDDS under the forced degradation and confirmatory conditions. Conclusion: This solid SMEDDS formulation could be an outstanding candidate for improving the oral bioavailability and photostability of MTX.
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- 생명과학대학 > Department of Pharmaceutical Engineering > Journal Articles
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