Enhanced Solubility and Biological Activity of Dexibuprofen-Loaded Silica-Based Ternary Solid Dispersions

Abstract

The current study was designed to formulate ternary solid dispersions (TSDs) of dexibuprofen (Dex) by solvent evaporation to augment the solubility and dissolution profile, in turn providing gastric protection and effective anti-inflammatory activity. Initially, nine formulations (S1 to S9) of binary solid dispersions (BSDs) were developed. Formulation S1 comprising a 1:1 weight ratio of Dex and Syloid 244FP® was chosen as the optimum BSD formulation due to its better solubility profile. Afterward, 20 TSD formulations were developed using the optimum BSD. The formulation containing Syloid 244FP® with 40% Gelucire 48/16® (S18) and Poloxamer 188® (S23) successfully enhanced the solubility by 28.23 and 38.02 times, respectively, in pH 6.8, while dissolution was increased by 1.99- and 2.01-fold during the first 5 min as compared to pure drug. The in vivo gastroprotective study in rats suggested that the average gastric lesion index was in the order of pure Dex (8.33 ± 2.02) > S1 (7 ± 1.32) > S18 (2.17 ± 1.61) > S23 (1.83 ± 1.04) > control (0). The in vivo anti-inflammatory study in rats revealed that the percentage inhibition of swelling was in the order of S23 (71.47 ± 2.16) > S18 (64.8 ± 3.79) > S1 (54.14 ± 6.78) > pure drug (18.43 ± 2.21) > control (1.18 ± 0.64) after 6 h. ELISA results further confirmed the anti-inflammatory potential of the developed formulation, where low levels of IL-6 and TNF alpha were reported for animals treated with S23. Therefore, S23 could be considered an effective formulation that not only enhanced the solubility and bioavailability but also reduced the gastric irritation of Dex.

Edible‐algae base composite film containing gelatin for food packaging from macroalgae, Gracilaroid (Gracilaria fisheri)

“…3 The main material used for this purpose is polysaccharides (such as alginate, chitosan, dextran and starch), proteins (plants such as corn zein and animal), lipids (carnauba wax and candelilla wax), 4,[7][8][9][10][11][12][13] solvent [deep eutectic solvent (DES)] 14 and dispersion (dexbuprofen-loaded silica). 15 Trends in chitosan as a primary biopolymer for functional films and manufacture of coatings for food and natural products were shown as new concepts in film formulations for food packaging together with polysaccharide, proteins and lipids such as oligodextran/chitosan blend films. 10,11,16 Research trends to propose new types of polysaccharides or other materials such as DES for use as materials for bio-degradable films such as smart films have been found.…”

“…EFs can be used as a pouch or sachet, particularly for energy drinks and meal replacement shakes, which, when added to cold or hot liquids, dissolve and release the contents, allowing customers ease of use, portion control and removal of solid waste 3 . The main material used for this purpose is polysaccharides (such as alginate, chitosan, dextran and starch), proteins (plants such as corn zein and animal), lipids (carnauba wax and candelilla wax), 4,7‐13 solvent [deep eutectic solvent (DES)] 14 and dispersion (dexbuprofen‐loaded silica) 15 . Trends in chitosan as a primary biopolymer for functional films and manufacture of coatings for food and natural products were shown as new concepts in film formulations for food packaging together with polysaccharide, proteins and lipids such as oligodextran/chitosan blend films 10,11,16 .…”