Self-microemulsifying Drug Delivery System of Eprosartan Mesylate: Design, Characterization, In vitro and Ex vivo evaluation
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Author:
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SABITRI BINDHANI, SNEHAMAYEE MOHAPATRA, RAJAT KUMAR KAR
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Abstract:
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The present investigation was aimed to design a self microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate for enhancing its bioavailability by scaling up its intestinal permeability. Preliminary screening was carried out to select oil, surfactant, and cosurfactant and an array of nine SMEDDS was prepared on using oil, surfactant, and cosurfactant. Pseudo ternary phase diagrams were constructed to identify the emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOSmix. The formulated SMEDDS of eprosartan mesylate was evaluated for thermodynamic stability, dispersibility study, robustness to dilution study, percent transmittance, cloud point determination, globule size and zeta potential, drug content analysis, FTIR study, in vitro dissolution study, in vitro diffusion study, ex vivo intestinal permeation study. Four batches were found stable after thermodynamic stability. Based on the comparative study, OF9 was optimized due to higher drug content (90.54±0.26), minimum droplet size (132.9 nm), highest in vitro drug release (98.57%), higher in vitro drug diffusion (93.71%) and ex vivo permeation study (74.25%). The bioavailability of eprosartan mesylate can be overcome by SMEDDS. The results prove the potential of SMEDDS as a means of enhancing the release performance of eprosartan mesylate leading to an increase of oral bioavailability and thus the therapeutic efficacy of eprosartan mesylate.
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Keyword:
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Eprosartan Mesylate, Bioavailability, Self microemulsifying drug delivery system (SMEDDS), Ex vivo drug permeation, poorly soluble drug.
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EOI:
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-
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DOI:
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https://doi.org/10.31838/ijpr/2020.SP1.287
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