Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide

Abstract

Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half-life of approximately 1h. Developing a controlled and prolonged release delivery system is required to maintain its therapeutic plasma concentration and to eliminate its adverse effects particularly hypoglycemia. The present study aimed to develop controlled release repaglinide loaded beads using sodium alginate and pectin with dual cross-linking for effective control of drug release. The prepared beads were characterized for size, percentage drug entrapment efficiency, in vitro drug release and the morphological examination using scanning electron microscope. For the comparative study, the release profile of a marketed conventional tablet of repaglinide (Prandin tablets 2mg, Novo Nordisk) was determined by the same procedure as followed for beads. The particle size of beads was in the range of 698±2.34-769±1.43μm. The drug entrapment efficiency varied between 55.24±4.61 to 82.29±3.42%. The FTIR results suggest that there was no interaction between repaglinide and excipients. The XRD and DSC results suggest partial molecular dispersion and amorphization of the drug throughout the system. These results suggest that repaglinide did not dissolve completely in the polymer composition and seems not to be involved in the cross-linking reaction. The percent drug release was decreased with higher polymer concentrations. In conclusion, the developed beads could enhance drug entrapment efficiency, prolong the drug release and enhance bioavailability for better control of diabetes.

In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

“…The hydrogel beads obtained at this stage were in the semisolid state. The hydrogel beads were collected and air-dried overnight at 30°C as explained by Awasthi and co-workers [37].…”

Development of a Simple Fe(II) Ion Colorimetric Sensor from the Immobilization of 1,10-Phenanthroline In Alginate/Pectin Film

“…The nature of alginate and pectin were known to be very hydrophilic since they consisted of many -OH and -COOH groups. The presence of divalent cations, such as Ca 2+ , replaced the Na + ions in the sodium alginate and caused the polymer chains of alginate/pectin to cross-link [18]. This process increased the mechanical strength of alginate/pectin film, reducing its dissolution in water; however, it still has the ability to swelling.…”

Pectin-Based Formulations for Controlled Release of an Ellagic Acid Salt with High Solubility Profile in Physiological Media

“…Pectins are widely used in food industries (food additive E440 according to International Numbering System for Food Additives (INS)) as gelling or thickening agents and in the pharmaceutical industry as bulking agents in drug production, in wound healing preparations, and in medical adhesives for oral drug delivery formulations (e.g., controlled release systems, gastro-retentive systems, colon-specific delivery systems, and mucoadhesive delivery systems). Beads prepared from sodium alginate and pectin with dual cross-linking were tested for effective control of release of the antidiabetic drug repaglinide [18]. Numerous applications have been reported that exploit the colon-specific delivery ability of pectins.…”