Abstract
Glibenclamide (GL)-loaded microcapsules (MC) and transdermal patches (TDP) were formulated and in vitro and in vivo parameters compared to find out the best route of drug administration. The formulation TDP1 having a drug–polymer ratio 1:1 showed comparatively higher GL release and better permeation across mice skin (p < 0.05). From the comparative study, it was concluded that the transdermal system of GL produced better improvement compared to oral microcapsule administration (p < 0.05). The transdermal system exhibited comparatively slow and continuous supply of GL at a desired rate to systemic circulation avoiding metabolism, which improved day-to-day glycemic control in diabetic subjects. Transdermal system of GL exhibited better control of hyperglycemia and prolonged plasma half-life by transdermal systems (9.6 ± 1.2 h) in comparison with oral microcapsule (5.84 ± 2.1 h), indicating that the drug, when administered by transdermal systems, will remain in the body for a longer period. From the glucose tolerance test, transdermal route effectively maintained the normoglycemic levels in contrast to the oral group (MC1), which produced remarkable hypoglycemia ranging from −12.6 ± 2.1% to −18 ± 2.3%. The significantly high (p < 0.05) area under the curve values observed with transdermal system (1,346.2 ± 92.3 ng ml−1 h−1) also indicate increased bioavailability of the drug from these systems compared to the oral route (829.8 ± 76.4 ng ml−1 h−1).
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Acknowledgments
This work was supported by the Siksha-O-Anusandhan University, India. The authors would like to thank Zydus Cadila Pharmaceuticals Ltd., Gujarat, India for providing the gift sample of glibenclamide for the study.
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Mishra, M.K., Ray, D. & Barik, B.B. Microcapsules and Transdermal Patch: A Comparative Approach for Improved Delivery of Antidiabetic Drug. AAPS PharmSciTech 10, 928–934 (2009). https://doi.org/10.1208/s12249-009-9289-z
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DOI: https://doi.org/10.1208/s12249-009-9289-z