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Co-Amorphous Based Supersaturated Urea-Losartan Potassium Transdermal Formulation For Hypertension
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| Author:
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NANHI NANDINI, AFRASIM MOIN, ROHINI BHATTACHARYA, MEENAKSHI S, SIDDARAMAIAH, SATHISHBABU P, NITHIN K S, D V GOWDA
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| Abstract:
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The present study aims to develop and evaluate a co-amorphous-based supersaturated transdermal formulation of a drug and enhance skin permeation with co-formers' help. Both Losartan potassium(LP) and urea(UR) were used as a model drug and co-former. Supersaturated solutions of Losartan Potassium and urea were prepared at different molar ratios in polyethylene glycol 400 (PEG400). All the formulations showed precipitations upon storage at 25?C except Losartan Potassium-Urea 1:8 molar ratios, which remained supersaturated. Fourier Transform Infrared (FTIR) study and Differential Scanning Colorimetry (DSC) studies confirmed no interactions between drugs and co-formers. Due to low glass transition temperature (Tg), physical mixtures of Losartan Potassium and Urea exhibited reduced melting points, and co-amorphous form was developed in a supercooled liquid state. Thermal analysis showed that the combination of Losartan Potassium-Urea induced co-melting and the co-amorphous structure showed a high crystallization tendency. After 45 days, 1:8 ratios of supersaturated formulations of Losartan Potassium-Urea showed the inhibition effect on recrystallization. The Proton Nuclear Magnetic Resonance(1H-NMR) study, the interaction between the Losartan Potassium-Urea in the supersaturated formulation, prevents the interaction between Losartan Potassium-Losartan Potassium or Urea-Polyethylene glycol 400 and also precipitation of Losartan Potassium from the formulation. From the In vitro skin permeation study, Losartan Potassium exhibited more skin permeation from the co-amorphous supersaturated formulation.
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| Keyword:
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Co-Amorphous, Supersaturation, Transdermal Drug Delivery, Losartan Potassium,Urea.
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| EOI:
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-
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.01.403
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| Download:
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