DOI: 10.3390/polym18212667 ISSN: 2073-4360

Physicochemical and Release Characteristics of Andrographolide Liquisolid Systems Fabricated Based on Microcrystalline Cellulose, Magnesium Aluminometasilicate, and Their Blends

Napaphak Jaipakdee, Peera Tabboon, Pinpair Ekkanjanakorn, Kattiya Sonchiangkham, Thaned Pongjanyakul, Ekapol Limpongsa

This study aimed to investigate physicochemical properties and release characteristics of andrographolide liquisolid systems developed using microcrystalline cellulose (MCC), magnesium aluminometasilicate (NEU), and their combinations (MCC:NEU) as carriers. Polyoxyl 15 hydroxystearate combined with N-methyl-2-pyrrolidone as a non-volatile liquid vehicle facilitated AG solubility, leading to the transformation into non-crystalline AG in the liquisolid powder, as demonstrated via PXRD. NEU-based liquisolid powder exhibited a greater liquid-loading factor than that of MCC (0.925 vs. 0.202). Liquid-loading factor of MCC:NEU exhibited a notable improvement, resulting in an increase in AG loading from 1.63% to 4.20% as the NEU content increased from 0% to 75%. MCC:NEU-based liquisolid powders exhibited greater AG release and tabletability than MCC-based powders. Five prepared AG liquisolid tablets based on liquisolid powder, sodium starch glycolate (4%), and magnesium stearate (1%) had acceptable tablet properties and AG content uniformity. MCC-based liquisolid tablets showed a modest improvement in AG release with a release efficiency of 44.6 ± 2.5%, while NEU-based tablets had a release efficiency of 8.7 ± 0.7%. MCC:NEU-based AG liquisolid tablets exhibited increased disintegration time and thus significantly suppressed AG release. This suggests that a justification for the design of MCC:NEU liquisolid tablets with prompt disintegration is essential for achieving superior AG release.

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