Abstract
Allantoin (ALL) is a phytochemical possessing an impressive array of biological activities. Nonetheless, developing a nanostructured delivery system targeted to augment the gastric antiulcerogenic activity of ALL has not been so far investigated. Consequently, in this survey, ALL-loaded chitosan/sodium tripolyphosphate nanoparticles (ALL-loaded CS/STPP NPs) were prepared by ionotropic gelation technique and thoroughly characterized. A full 24 factorial design was adopted using four independently controlled parameters (ICPs). Comprehensive characterization, in vitro evaluations as well as antiulcerogenic activity study against ethanol-induced gastric ulcer in rats of the optimized NPs formula were conducted. The optimized NPs formula, (CS (1.5% w/v), STPP (0.3% w/v), CS:STPP volume ratio (5:1), ALL amount (13 mg)), was the most convenient one with drug content of 6.26 mg, drug entrapment efficiency % of 48.12%, particle size of 508.3 nm, polydispersity index 0.29 and ζ-potential of + 35.70 mV. It displayed a sustained in vitro release profile and mucoadhesive strength of 45.55%. ALL-loaded CS/STPP NPs (F-9) provoked remarkable antiulcerogenic activity against ethanol-induced gastric ulceration in rats, which was accentuated by histopathological, immunohistochemical (IHC) and biochemical studies. In conclusion, the prepared ALL-loaded CS/STPP NPs could be presented to the phytomedicine field as an auspicious oral delivery system for gastric ulceration management.
Highlights
Allantoin (ALL) is a phytochemical possessing an impressive array of biological activities
ALL-loaded CS/sodium tripolyphosphate (STPP) NPs were successfully prepared by ionotropic gelation method
Administration of ALL-loaded CS/STPP NPs, in the doses of 30 mg/kg (NanoAL group) and 60 mg/kg (NanoAH group), proved the most superiority as antiulcerogenic activity (AA) in enhancing the AA parameters; where the total UA was 4.725 ± 3.55 and 2.99 ± 1.32, respectively, and AI was 0.23 ± 0.13 and 0.211 ± 0.11, respectively, grossing a protection index (PI) of 97% for both, compared to a PI of 81.33% for ALL group (60 mg/kg). These findings proved the success of the CS/STPP carrier system as AA system by significantly reducing the damage of ethanol on the gastric mucosa compared to ulcer group, and its ability to reach the same AA effect by reducing the medicated portion (ALL) to a half of the dose
Summary
Allantoin (ALL) is a phytochemical possessing an impressive array of biological activities. Developing a nanostructured delivery system targeted to augment the gastric antiulcerogenic activity of ALL has not been so far investigated In this survey, ALL-loaded chitosan/ sodium tripolyphosphate nanoparticles (ALL-loaded CS/STPP NPs) were prepared by ionotropic gelation technique and thoroughly characterized. Ionotropic gelation method, an easy and attractive physical cross-linking process, is a cost-effective technique adopted to prepare chitosan nanoparticles (CS-NPs) This technique depends on ionic interactions arise from electrostatic attraction between two groups of opposite charge namely; positive amino groups (–NH3+) of CS as well as negative phosphate groups of sodium tripolyphosphate (STPP). It possesses wound healing and tissue regeneration activities, besides renowned anti-oxidant, anti-inflammatory, pain reducing and gastroprotective effects that have been proved using a diversity of in vitro assay methods, in vivo animal models as well as clinical studies[7,8,9,10,11,12]
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