Development and In vitro Evaluation of Nifedipine Gel Formulations for Anorectal Applications

Author(s): Nuray Bagci, Zerrin Sezgin Bayindir, Ozge Inal, Nurten Altanlar, Nilufer Yuksel*

Journal Name: Current Drug Delivery

Volume 17 , Issue 2 , 2020

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Graphical Abstract:


Objective: Current study focuses on the formulation and characterization of lipophilic and hydrophilic gel formulations of nifedipine to treat anal fissure via anodermal application.

Methods: Lipophilic gels were prepared with Aerosil grades as gelling agents in bulk oils. Polyethylene glycols, hydroxypropyl methylcellulose, and Carbopol® 974P were used as gelling agents in water and propylene glycol for forming hydrophilic gels. The effect of repeated Freeze-Thaw Cycles (FT-C) on microstructures of the gels was investigated by examining viscosity, rheology and textural properties. Aerosil 200 containing lipophilic gels exhibited thixotropic behavior with plastic flow properties and higher viscosities.

Result: Accordingly, their compressibility and adhesiveness increased. FT-C caused notable changes in microstructures and textural properties of the lipophilic gels excluding the formulation containing Aerosil 200-in-isopropyl myristate. Among the hydrophilic gels, the viscosity of Carbopol® 974P gels increased depending on the amount of polymer, triethanolamine and water; these gels featured plastic flow without thixotropic behavior. Their compressibility and adhesiveness were higher than other gel formulations with stable post-FT-C characteristics. The higher flux values of nifedipine were observed from water containing Carbopol® 974P gel.

Conclusion: The results of the stability tests showed that the Carbopol® 974P gel had a longer shelf life than the Aerosil 200-in-isopropyl myristate gel.

Keywords: Nifedipine, anal fissure, anorectal gel, texture analysis, rheology, freeze-thaw cycle.

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Year: 2020
Page: [126 - 139]
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DOI: 10.2174/1567201817666200102125242
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