The ALGINATE MICROSPHERES CONTAINING CURCUMIN: PREPARATION, CHARACTERIZATION, AND IN VITRO HUMAN HAEMOGLOBIN GLYCOSYLATION ASSAY
Formulation development and glycosylation inhibition assay
Keywords:Alginate microspheres,, Hemoglobin,, Glycosylation,, Quercetin
Objective: The objective of the present study was to formulate, evaluate alginate microspheres of curcumin, and to investigate the inhibitory effect on glycosylated hemoglobin.
Methods: All formulations were prepared by an ionotropic gelation technique using sodium alginate as a polymer and calcium chloride as a crosslinker in varying concentrations. The formulation batches (F1–F6) were evaluated for physical properties such as compatibility studies, percentage entrapment efficiency (%EE), microsphere yield, particle size, and polydispersity index. In vitro, drug release was studied and surface morphology was characterized by scanning electron microscopy.
Results: The microspheres showed %EE, microsphere yield, particle size in the ranges of 44.86%–84.24%, 43.05%–81.4%, and 352–559 μm, respectively. In vitro, drug release and release kinetics showed that the developed curcumin microspheres system is a promising delivery system for controlled drug release. Scanning electron micrographs indicate porous and rough surface. The inhibitory properties of curcumin and microspheres (F4) on glycosylation formation were investigated in hemoglobin using quercetin as standard. The decreased in hemoglobin concentration after incubation of hemoglobin with a graded concentration of glucose over a specified time was used as an index for in vitro human hemoglobin glycosylation assay. Glycosylation inhibition was about 75% for standard quercetin, 60% for curcumin microspheres, and 38.74% for curcumin suspension occurred after 72 h.
Conclusion: From these results, it can be concluded that curcumin in microsphere formulation has better therapeutic potential and could prove to be useful in the development of antidiabetic formulation.
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