Abstract
Purpose: To prepare metformin HCl-loaded alginate (AL) and alginate-chitosan (AL-CS) beads for oral application and to evaluate their in vitro characteristics and in vivo activities.Methods: AL and AL-CS beads were prepared using ionotropic gelation. The beads were evaluated for particle size, surface morphology, drug encapsulation efficiency (EE) and in vitro drug release. The antidiabetic effects of the beads were evaluated in diabetic Sprague Dawley rats.Results: The mean particle sizes of AL and AL-CS beads in wet state ranged from 1714 ± 140 to 1850 ± 103 μm. The EE % of AL and AL-CS beads were 33.58 ± 1.56 and 24.11 ± 1.72, respectively, with sustained in vitro drug release of about 93 to 96 % within 8 days in phosphate buffer (PB). Optimized metformin HCl-loaded AL and AL-CS beads showed significant hypoglycaemic effects in diabetic rats over a prolonged period (about 12 h) after oral administration compared to the pure drug (p < 0.05).Conclusion: Metformin HCl-loaded AL and AL-CS beads for oral application may be useful in prolonging the hypoglycaemic effect of metformin. This is capable of increasing patients’ compliance to the medication.Keywords: Alginate, Beads, Chitosan, Metformin, Diabetes, In vivo study
Highlights
Metformin hydrochloride is a biguanide derivative widely used for the treatment of Type 2 diabetes, and prescribed for about 120 million people worldwide [1,2,3,4]
The present study focuses on the development and in vitro characterization of metformin HClloaded AL beads and AL-CS beads
Regardless of the release medium, about 25 – 40 % of the loaded metformin HCL was released from the beads during the initial burst release (60 min)
Summary
Metformin hydrochloride is a biguanide derivative widely used for the treatment of Type 2 diabetes, and prescribed for about 120 million people worldwide [1,2,3,4]. More effective beads for the controlled release of drugs can be prepared using the combination of chitosan and alginate. The present study focuses on the development and in vitro characterization of metformin HClloaded AL beads and AL-CS beads It focuses on in vivo evaluation of the hypoglycaemic activities of the bead formulations in streptozotocin (STZ) and nicotinamide-induced diabetic rats. Metformin HCl-loaded AL and AL-CS beads were prepared by ionotropic gelation technique. The blood samples of diabetic rats (n = 8) collected from the tail veins were centrifuged (10,000 rpm, 10 min) and the supernatant was frozen until assayed for fasting serum insulin level using rat insulin enzyme immunoassay kit (SPI-BIO Bertin Pharma, France). Diabetic rats were divided randomly into five different groups (Group IIGroup VI).The pure drug and the formulations of blank and metformin HCl-loaded beads were administered orally through a flexible plastic tube after an overnight fast. P < 0.05 was taken as indicative of statistical significance
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