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Poloxamer-Based In Situ Nasal Gel of Naratriptan Hydrochloride Deformable Vesicles for Brain Targeting

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Abstract

Migraine is the chronic neurological disorder identified by recurrent moderate to severe headache. Research was highlighted to formulate target drug delivery to treat migraine via the olfactory lobe through the intranasal route using ethosomal thermoreversible gel. Ethosomes were prepared by thin film hydration method using 32 factorial design. The prepared ethosomes were evaluated for percent drug loading, vesicle size, zeta potential, and polydispersity index, whereas nanoethosomal in situ gels were assessed for their pH, viscosity, mucoadhesive strength, and in vitro drug release. Ex vivo drug permeation was evaluated using nasal mucosa of sheep. The data produced from the experimental design indicated NE6 (soya lecithin 3%:ethanol 50%) as the optimized ethosome formulation, whereas NG3 (carbol 934-0.3%) and NG6 (PVP K30-0.3%) were recorded as the optimized in situ gel formulations. In vitro and ex vivo drug release demonstrated almost 100% release after 24 h for optimized formulations. In conclusion, drug-loaded in situ mucoadhesive gels could release the drug for longer duration of time which can improve the bioavailability providing new dimension to the treatment of migraine.

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Abbreviations

NH:

Naratriptan hydrochloride

NE6:

Optimized batch of ethosomes

NG3:

Carbol 934-0.3%

NG6:

PVP K30-0.3%

PVP K30:

Polyvinylpyrrolidone K30

5-HT:

5-Hydroxytryptamine

PBS:

Phosphate-buffered saline

UV-vis:

Ultraviolet-visible spectroscopy

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Acknowledgments

The authors wish to thank the Management, Srinath College of Pharmacy, Aurangabad (M.S.), India for providing required facilities to carry out the research work. We would also like to thank Orchid Chemicals and Pharmaceuticals Ltd., Chennai, India for providing free sample of NH.

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Authors and Affiliations

  1. Department of Pharmaceutics, Srinath College of Pharmacy, Bajaj Nagar, Aurangabad, Maharashtra, 431136, India

    Santosh Shelke, Manoj Damale, Rashmi Chouthe, Prabhakar Panzade & Deepak Kulkarni

  2. Department of Pharmaceutics, Government College of Pharmacy, Osmanpura, Aurangabad, Maharashtra, 431005, India

    Inayat Pathan

  3. Department of Pharmaceutics, Parul Institute of Pharmacy, Faculty of Pharmacy, Parul University, Vadodara, Gujarat, 391760, India

    Gajanan Shinde

  4. Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra, 431004, India

    Gaurav Agrawal

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  1. Santosh Shelke
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Correspondence to Santosh Shelke.

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Shelke, S., Pathan, I., Shinde, G. et al. Poloxamer-Based In Situ Nasal Gel of Naratriptan Hydrochloride Deformable Vesicles for Brain Targeting. BioNanoSci. 10, 633–648 (2020). https://doi.org/10.1007/s12668-020-00767-5

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