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Application of Lipid Blend-Based Nanoparticulate Scaffold for Oral Delivery of Antihypertensive Drug: Implication on Process Variables and In Vivo Absorption Assessment

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Abstract

Purpose

The aim of the present study was to formulate and optimize lipid blend-based olmesartan medoxomil (OLM) loaded nanoparticulate scaffolds (NLCs) for enhanced oral bioavailability.

Method

The OLM-NLCs were formulated using dependent variables in different concentrations of solid lipid, liquid lipid, surfactant, and co-surfactant by using melt emulsification combined with ultrasonication technique. The formulations were experimentally optimized using a three-factor, three-level statistical design approach. The formulated OLM-NLCs were evaluated for various pharmaceutical quality evaluation parameters and further optimized formulation (OLM-NLCopt) was assessed for release kinetics, thermal behavior, and in vivo absorption assessment.

Result

The optimized formulation (OLM-NLCopt) showed particle size (138.7 nm), PDI (0.18), and entrapment efficiency (83.65%). The comparative in vitro release study revealed OLM-NLCopt showed significantly higher (p < 0.05) drug release compare to OLM-susp. The in vivo study showed the OLM-NLCopt indicated nearly 3-fold improvement in oral bioavailability vis-a-vis OLM-susp in mice model.

Conclusion

The results of the release study and pharmacokinetic study suggest the potential of OLM-NLCs for improved oral delivery.

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Acknowledgements

The authors would like to thank Ranbaxy, Gurgaon, India, for providing OLM as a gift sample.

Source of Funding

The authors have not received any funding for the research work.

Author information

Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard (Deemed University), M. B. Road, New Delhi, 110062, India

    Manzar Hasnain, Mohd. Aqil & Yasmin Sultana

  2. Department of Pharmaceutics, Glocal School of Pharmacy, Glocal University, Saharanpur, Uttar Pradesh, 247121, India

    Syed Sarim Imam

  3. Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia

    Abdul Ahad

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  1. Manzar Hasnain
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  2. Syed Sarim Imam
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  3. Mohd. Aqil
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  4. Abdul Ahad
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  5. Yasmin Sultana
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Corresponding author

Correspondence to Mohd. Aqil.

Ethics declarations

All the experiments reported in this manuscript comply with the current laws of the country in which they were performed. All institutional and national guidelines for the care and use of laboratory animals were followed.

Conflict of Interest

All authors declare no conflicts interest.

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Hasnain, M., Imam, S.S., Aqil, M. et al. Application of Lipid Blend-Based Nanoparticulate Scaffold for Oral Delivery of Antihypertensive Drug: Implication on Process Variables and In Vivo Absorption Assessment. J Pharm Innov 13, 341–352 (2018). https://doi.org/10.1007/s12247-018-9329-x

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  • DOI: https://doi.org/10.1007/s12247-018-9329-x

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