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Enhanced Oral Bioavailability of Isoformononetin Through Nanoemulsion: Development, Optimization, and Characterization

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Abstract

Background

Isoformononetin (IFN) is a methoxyl derivative of daidzein and has been stated as a potent osteogenic isoflavone. However, IFN has low oral bioavailability. Advancement in the technology has led to the development of newer drug carrier systems, featuring the delivery of drugs with low oral bioavailability to advance their clinical application.

Methods

The IFN nanoemulsion (IFN-NE) was developed and optimized using the design of the experiment tool and technique approaches.

Results

The optimized IFN-NE has a particle size of 174.65 ± 1.63 nm, PDI of 0.244 ± 0.004, and zeta potential of − 30.69 ± 4.99 mV, respectively. The TEM images of optimized IFN-NE showed the spherical globular size of the nanoemulsion. The entrapment efficiency showed higher entrapment of IFN in the NE (96.04 ± 1.28%). The compatibility of IFN with excipients was confirmed by physical state characterization such as FTIR and DSC, illustrating no interaction. Optimized IFN-NE formulation was stable at different temperature conditions. In comparison to a free drug suspension, IFN-NE showed sustained drug release over a 24-h period of time. Additionally, in situ, single-pass intestinal perfusion (SPIP) results displayed significant enhancement of IFN permeability through the intestine of rats from IFN-NE when compared to free IFN.

Conclusions

Pharmacokinetics results revealed the enhanced relative oral bioavailability of IFN-NE compared to IFN suspension using female Sprague–Dawley (SD) rats as animal models. The developed IFN-NE can be a promising candidate to overcome the low oral bioavailability of IFN.

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Data Availability

Data will be available from corresponding author with a significant request.

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Acknowledgements

The authors are very thankful to the Director, CSIR-Central Drug Research Institute, Lucknow, U.P., India, for the constant encouragement and financial support. All the authors are also thankful to the SAIF division, CSIR-CDRI, Luckow, for providing the FTIR facility. The authors also acknowledge the Department of Science and Technology (DST), New Delhi, India, for providing financial support in the form of the DST-Inspire fellowship to DC and PKY. CDRI communication number is 10740.

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Author notes

  1. Nazneen Sultana and Divya Chauhan equally contributed to this work.

Authors and Affiliations

  1. Division of Pharmaceutics & Pharmacokinetics, CSIR-Central Drug Research Institute, Uttar Pradesh, Lucknow-226031, India

    Nazneen Sultana, Divya Chauhan, Pavan K. Yadav, Manish K. Chourasia & Jiaur R. Gayen

  2. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad- 201002, India

    Divya Chauhan, Pavan K. Yadav, Manish K. Chourasia & Jiaur R. Gayen

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  1. Nazneen Sultana
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  2. Divya Chauhan
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Contributions

NS, DC, and JRG hypothesized and designed the research plan; NS, DC, and PKY did the experiments required and analyzed the data. MKC and JRG supervised the study and reviewed and edited the final manuscript.

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Correspondence to Jiaur R. Gayen.

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Sultana, N., Chauhan, D., Yadav, P.K. et al. Enhanced Oral Bioavailability of Isoformononetin Through Nanoemulsion: Development, Optimization, and Characterization. J Pharm Innov 19, 8 (2024). https://doi.org/10.1007/s12247-024-09821-1

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