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Formulation and evaluation of thermoreversible, mucoadhesive in situ intranasal gel of rizatriptan benzoate

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Abstract

The present study was aimed to formulate and evaluate in situ thermoreversible intranasal gel of an antimigraine drug rizatriptan benzoate. The poloxamer 407 and carbopol 934 were used as thermoreversible and mucoadhesive polymers respectively. The gels were prepared with cold method. The phase transition temperature was determined with visual method. The gels were evaluated for their pH, mucoadhesive strength, in vitro release and ex vivo drug permeation through goat nasal mucosa. The histopathological study of the nasal mucosa was carried out to check for its damage during drug permeation. The 18 % w/v poloxamer solution was found to be showing phase transition at physiologic conditions (34–35 °C). As the percentage of carbopol 934 was increased from 0.1 to 0.5 % w/v the gelling temperature was found to be decreased. All formulations were showing mucoadhesive strength above 4,000 dynes/cm2. Drug permeation studies have indicated that the drug permeation rate can be increased by using carbopol 934 above 0.3 % w/v concentration. The histopathological evaluation of nasal mucosa after drug permeation study has not shown any evidence of damage. Thus in situ thermoreversible mucoadhesive gel of rizatriptan benzoate can be a promising approach to treat migraine.

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Acknowledgments

Authors are thankful to the KLE University, Belgaum for providing financial grant and Dr. Prabhakar Kore Basic Science Research Centre, Belgaum for providing research facilities to carry out this research work. Authors extend acknowledgement to Cipla Pvt Ltd, Mumbai for providing rizatriptan benzoate as gift sample.

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Correspondence to Amolkumar Kempwade.

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Kempwade, A., Taranalli, A. Formulation and evaluation of thermoreversible, mucoadhesive in situ intranasal gel of rizatriptan benzoate. J Sol-Gel Sci Technol 72, 43–48 (2014). https://doi.org/10.1007/s10971-014-3422-5

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  • DOI: https://doi.org/10.1007/s10971-014-3422-5

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