Document Details
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Document Type |
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Thesis |
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Document Title |
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Improved glimepiride buccal transmucosal delivery through optimized combined nanostructured formulation تحسين إنطلاق عقار الجليميبرايد عبر الأغشية المخاطية للفم من خلال صياغة مثلي مجمعة متناهية الصغر |
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Subject |
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faculty of Pharmacy |
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Document Language |
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Arabic |
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Abstract |
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Glimepiride (GMD) is a 3rd generation Sulfonylureas (SUs) which is an efficient and well-tolerated hypoglycemic agent, that delivers a significant option for the treatment of type 2 diabetes. GMD is a poorly water-soluble drug that leads to difficulties in pharmaceutical formulation and an unexpected absorption, which led to the need for a novel drug dosage form. Transmucosal route for delivery offers a unique characteristic by the introduction of drugs through the buccal mucosa. Consequently, avoid 1st pass metabolism effect and gastric destruction. In this work, GMD was formulated in a transmucosal buccal film through optimized nanostructured formulation. Nanostructured lipid carriers (NLCs) and micelles offer unique characteristics for GMD buccal film, enhancement of drug solubility, improvement of drug permeation, and hence its absorption through the buccal mucosa. Based on the Box-Behnken experimental design, we designed fifteen formulations that were assessed based on three factors: percentage of micelles relative to NLC (X1), percent concentration of Carbopol (X2), and percent concentration of permeation enhancer (X3). In response to these three factors, two response parameters were investigated, percent initial release after 1 hour (Y1) and the percentage of cumulative release after 6 hours (Y2).
All fifteen formulations and films were assessed for their size, thickness, stretching, drug content, and drug release. After reaching an optimized formula, the permeation of GMD from the prepared films was in favor of the micelles as an optimized formula.
The optimum levels for X1, X2, and X3 were found to be 99.92% of the micelles relative to NLCs, 0.05 the percentage of Carbopol( CRP), and 1.8% of the permeation enhancer respectively. Among the design points, maximum desirability was achieved at formulation (F6). The optimized formula was prepared, characterized for its size, zeta potential, thickness, stretching, content uniformity, and a fluorescent laser microscope study was done. The optimum GMD formula was prepared as bilayer film, loaded into the transmucosal buccal film, characterized for its mucoadhesive strength and permeation study. Ex-vivo permeation study observed values for Y1 and Y2 were about 21% and 95 %, respectively. The transport of the optimized formula as a unidirectional transmucosal film across buccal layers was investigated using a fluorescence laser microscope. Results revealed the successful delivery of the micelles formulation to deeper buccal mucus layers. According to these promising results, it is expected that the optimized formulation could enhance the absorption of GMD loaded into the nanocarrier system. |
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Supervisor |
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Dr. Osama Ahmed |
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Thesis Type |
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Master Thesis |
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Publishing Year |
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1442 AH
2021 AD |
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Added Date |
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Friday, August 13, 2021 |
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Researchers
| تهاني سعيد باصحيح | Basahih, Tahani Saeed | Researcher | Master | |
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