Molecular weight effects of low acyl gellan gum on antioxidant capacity and rheological properties.

The current study investigated the antioxidant capacity of enzymatically cleaved low acyl gellan gum (LA-GAGR) fragments, named midi-GAGR (MWv : 1.2 × 105  Da) and mini-GAGR (MWv : 2.5 × 104  Da). Three different methods-hydroxide assay, superoxide assay, and DPPH assay-were used to measure the antioxidant capacity of the low acyl gellan gum fragments. Both mini-GAGR and midi-GAGR showed similar antioxidant capacities, 27.1% and 25.6%, respectively, for hydroxide radicals, whereas ascorbic acid showed 9.8%. For superoxide radicals, the fragments scavenged 41.7% (mini) and 35.6% (midi) of free radicals compared to 10.6% removal by ascorbic acid. Mini- and midi-GAGR displayed modest scavenging capabilities with DPPH radicals (8.5% and 6.6%, respectively) as compared to ascorbic acid (96.3%). Both midi- and mini-GAGR showed less gel-like behaviors than LA-GAGR. Midi-GAGR was observed to have a transition from liquid to gel at 63 rad/s. PRACTICAL APPLICATION: The results in the manuscript are helpful when gellan gum and its derivatives are directly applied to food processing as a dietary fiber supplement or a stabilizer for functional beverages. The antioxidant capacity results can be used to promote the functionality of gellan gum as a food additive and for controlling cell adhesion and growth on gellan gum scaffolds. The rheology results will be useful for synthesis of scaffolds for bone tissue generation and facilitating clinical treatments when gellan gum is injected as an adsorbent or a filler for treating bone fractures. In the pharmaceutical industry, they are useful when controlling the therapeutic effects of drug delivery systems.

Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate.

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® 80, and Plurol® 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 Cmax, respectively in comparison to MTX powder. The AUC and Cmax 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.

Comparison of solvent-wetted and kneaded l-sulpiride-loaded solid dispersions: Powder characterization and in vivo evaluation.

The purpose of this study was to compare the powder properties, solubility, dissolution and oral absorption of solvent-wetted (SWSD) and kneaded (KNSD) l-sulpiride-loaded solid dispersions. The SWSD and KNSD were prepared with silicon dioxide, sodium laurylsulfate and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) using a spray dryer and high shear mixer, respectively. Their powder properties, solubility, dissolution and oral absorption were assessed compared to l-sulpiride powder. The drug in SWSD was in the amorphous state; however, in KNSD, it existed in the crystalline state. The SWSD with a drug/sodium laurylsulphate/TPGS/silicon dioxide ratio of 5/1/2/12 gave the higher drug solubility and dissolution compared to the KNSD with the same composition. The oral absorption of drug in the SWSD was 1.4 fold higher than the KNSD and 3.0 fold higher than the l-sulpiride powder (p<0.05) owing to better solubility and reduced crystallinity. Furthermore, the SWSD at the half dose was bioequivalent of commercial l-sulpiride-loaded product in rats. Thus, the SWSD with more improved oral absorption would be recommended as an alternative for the l-sulpiride-loaded oral administration.