Abstract
Objective: Hesperidin is flavonoid glycosides that proven to have therapeutic activity to any desease, one of them is colon disease; but, its low solubility (< 100 mg/L) makes small absosption inside the body so it needs delivery system that could deliver hesperidin to the therapy target. The objective of this research is to get optimum formula from hydrogel with polimer pectin-chitosan combination that can control in vitro hesperidin release.Method: Optimum hydrogel formula determination using Design Expert 7.0.0 with factorial method design, resulted in formula plans with pectin-chitosan consentration comparison of (P3% : C1%), (P3% : C2%), (P5% : C1%), (P5% : C2%) respectively.Result: Optimum formula with pectin : chitosan concentration comparison (5% : 1%) has entrapment efficiency about 96.658%; k(/hour) swelling index at pH 5.0, 6.8, and 7.4, about 34.917, 15.766, and 8.146 respectively; drug release at pH 5.0, 6.8, and a medium contained 2% mouse’s caecum about 0.461, 20.116, and 52.955% respectively; and the mucoadhesive strength about 0.184 N/cm2.Conclusion: The combination of pectin-chitosan polymer in hydrogel muchoadhesive matrix can control hesperidin in vitro release with the drug release value at the highest concentration of pectin in medium contained 2% mouse’s saecum that could release drug about 56%. Hesperidin hydrogel release mechanism follows Higuchi kinetic.
Highlights
IntroductionControlled drug delivery system is one of a method to control drug release in order to increase drug effectiveness; and commonly applied to the active substance with low solubility, one of them is hesperidin
The combination of pectin-chitosan polymer was observed in several physicochemical traits, which are entrapment efficiency, swelling index, mucoadhesive strength and drug release
Highest mucoadhesive strength was achieved by formula 4, which has the highest chitosanpectin concentration
Summary
Controlled drug delivery system is one of a method to control drug release in order to increase drug effectiveness; and commonly applied to the active substance with low solubility, one of them is hesperidin. Pectin is one of the hydrogel constituent polymer commonly used to deliver drugs to the colon. Other research showed that hydrogel beads of pectin-zein protects indomethacin from upper gastrointestinal tract conditions and its release was controlled by pectin degradation with pectinase; pectin is highly soluble in water, which leads to the development of another polymer with low solubility in water, to produce a strong and effective gel for carrying drug which is entrapped in gastric fluid and small intestine [9,10]. One of the polymers that can be used to overcome this problem is chitosan, which its carboxylic group binds ionically with the chitosan amine group [11]
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