Oral bioavailability enhancement of glibenclamide by self-emulsifying drug delivery systems (SEDDS)

Anup Naha, Harsha Srivastava, Sivakumar Kannan

Research output: Contribution to journalArticle

Abstract

The present work was aimed to improve the oral bioavailability of glibenclamide by developing self-emulsifying drug delivery system (SEDDS). Solubility of glibenclamide was determined in oils, surfactant, and cosurfactant. Pseudoternary phase diagrams were constructed to obtain self-nanoemulsi-fying region. SEDDS were evaluated for thermodynamic stability, droplet size, in vitro dissolution, in vivo pharmacokinetic, and stability studies. Sunflower oil (3.46 ± 0.32 mg/100 mg), Tween 80 (3.75 ± 0.37 mg/100 mg) and PEG 600 (2.98 ± 0.44 mg/100 mg) were selected as oil, surfactant, and cosurfactant, respectively. Surfactant and cosurfactant mix (Smix) of 3:1, 2:1, and 1:1 showed a larger nanoemulsification region and Ba3 (Smix 3:1) showed minimum emulsion globule size of 122.9 nm with PDI of 0.549 and exhibited highest cumulative drug release (97.6 ± 1.8), as compared to pure glibenclamide (31.2 ± 2.2) and marketed tablet (90.3 ± 2.1). Cmax of Ba3 (10.01 ± 2.14 µg/mL) was significantly higher than pure drug (7.13 ± 1.16 µg/mL) and marketed tablet (9.02 ± 2.23 µg/mL) and AUC of Ba3 (140.39 ± 10.14 µg.h/mL) was found to be significantly higher than pure glibenclamide (100.12 ± 11.45 µg.h/mL), indicating an improvement in the bioavailability of glibenclamide from SEDDS formulation as compared to pure drug.

Original languageEnglish
Pages (from-to)1319-1326
Number of pages8
JournalLatin American Journal of Pharmacy
Volume38
Issue number7
Publication statusPublished - 01-01-2019

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Glyburide
Drug Delivery Systems
Biological Availability
Surface-Active Agents
Tablets
Oils
Polysorbates
Emulsions
Thermodynamics
Pharmaceutical Preparations
Solubility
Area Under Curve
Pharmacokinetics

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery

Cite this

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abstract = "The present work was aimed to improve the oral bioavailability of glibenclamide by developing self-emulsifying drug delivery system (SEDDS). Solubility of glibenclamide was determined in oils, surfactant, and cosurfactant. Pseudoternary phase diagrams were constructed to obtain self-nanoemulsi-fying region. SEDDS were evaluated for thermodynamic stability, droplet size, in vitro dissolution, in vivo pharmacokinetic, and stability studies. Sunflower oil (3.46 ± 0.32 mg/100 mg), Tween 80 (3.75 ± 0.37 mg/100 mg) and PEG 600 (2.98 ± 0.44 mg/100 mg) were selected as oil, surfactant, and cosurfactant, respectively. Surfactant and cosurfactant mix (Smix) of 3:1, 2:1, and 1:1 showed a larger nanoemulsification region and Ba3 (Smix 3:1) showed minimum emulsion globule size of 122.9 nm with PDI of 0.549 and exhibited highest cumulative drug release (97.6 ± 1.8), as compared to pure glibenclamide (31.2 ± 2.2) and marketed tablet (90.3 ± 2.1). Cmax of Ba3 (10.01 ± 2.14 µg/mL) was significantly higher than pure drug (7.13 ± 1.16 µg/mL) and marketed tablet (9.02 ± 2.23 µg/mL) and AUC of Ba3 (140.39 ± 10.14 µg.h/mL) was found to be significantly higher than pure glibenclamide (100.12 ± 11.45 µg.h/mL), indicating an improvement in the bioavailability of glibenclamide from SEDDS formulation as compared to pure drug.",
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Oral bioavailability enhancement of glibenclamide by self-emulsifying drug delivery systems (SEDDS). / Naha, Anup; Srivastava, Harsha; Kannan, Sivakumar.

In: Latin American Journal of Pharmacy, Vol. 38, No. 7, 01.01.2019, p. 1319-1326.

Research output: Contribution to journalArticle

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AU - Srivastava, Harsha

AU - Kannan, Sivakumar

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