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Spray-Dried Mucoadhesive Re-dispersible Gargle of Chlorhexidine for Improved Response Against Throat Infection: Formulation Development, In Vitro and In Vivo Evaluation

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  • Advancements in Amorphous Solid Dispersions to Improve Bioavailability
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Abstract

Drug delivery to the buccal mucosa is one of the most convenient ways to treat common mouth problems. Here, we propose a spray-dried re-dispersible mucoadhesive controlled release gargle formulation to improve the efficacy of chlorhexidine. The present investigation portrays an approach to get stable and free-flowing spray-dried porous aggregates of chlorhexidine-loaded sodium alginate nanoparticles. The ionic gelation technique aided with the chlorhexidine’s positive surface charge–based crosslinking, followed by spray drying of the nanoparticle’s dispersion in the presence of lactose- and leucine-yielded nano-aggregates with good flow properties and with a size range of about 120–350 nm. Provided with the high entrapment efficiency (87%), the particles showed sustained drug release behaviors over a duration of 10 h, where 87% of the released drug got permeated within 12 h. The antimicrobial activity of the prepared formulation was tested on S. aureus, provided with a higher zone of growth inhibition than the marketed formulation. Aided with an appropriate mucoadhesive strength, this product exhibited extended retention of nanoparticles in the throat region, as shown by in vivo imaging results. In conclusion, the technology, provided with high drug retention and extended effect, could be a potential candidate for treating several types of throat infections.

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Acknowledgements

The authors acknowledge the Researchers Supporting Project number (RSPD2024R708), King Saud University, Riyadh, Saudi Arabia, for funding this research work. The authors also acknowledge the financial support of the Department of Biotechnology (DBT), Govt. India.

Funding

The research was funded by the DBT Builder project with order no. (BT/INF/22/SP45078/2022).

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Authors and Affiliations

Authors

Contributions

Vineet Kumar Rai: data collection, experimental work, compilation, and manuscript writing. Amresh Kumar: data collection and experimental work. Deepak Pradhan: proof reading, software and language editing. Jitu Halder: data analysis, language editing and critical analysis. Tushar Kanti Rajwar: compilation, manuscript writing. Manoj Kumar Sarangi: data collection, experimentation and statistics. Priyanka Dash: animal experimentation and proof reading. Chandan Dash: software analysis, data collection, and proof reading. Salim Manoharadas: data analysis, language editing, and funding support. Biswakanth Kar: animal experiment and data interpretation. Goutam Ghosh: conceptualization of the topics and critical analysis. Goutam Rath: conceptualization of the topic and design of the table of content, supervision, data analysis, and paper writing, editing, and proof reading.

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Correspondence to Goutam Rath.

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The animal protocol used in this study was approved by the Institutional Animal Ethical Committee (IAEC) bearing Regd. No IAEC/SPS/SOA/122/2022.

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Rai, V.K., Kumar, A., Pradhan, D. et al. Spray-Dried Mucoadhesive Re-dispersible Gargle of Chlorhexidine for Improved Response Against Throat Infection: Formulation Development, In Vitro and In Vivo Evaluation. AAPS PharmSciTech 25, 31 (2024). https://doi.org/10.1208/s12249-024-02750-9

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