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Fabrication of hesperidin self-micro-emulsifying nutraceutical delivery system embedded in sodium alginate beads to elicit gastric stability

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Abstract

Poor bioavailability of hesperidin (HES) due to its gastric instability and low aqueous solubility limits its clinical application. The objective of presented work was to incorporate self-microemulsifying drug delivery system of HES (SMEDDS-HES) into alginate beads. The alginate beads were characterized for their size and morphology by using motic microscopy and scanning electron microscopy. The selected beads formulation (BF 7) revealed particle size (1.3 ± 0.117 mm), entrapment efficiency (87.4 ± 2.2%), circularity (0.9987), aspect ratio (0.9950), and swelling index (81.75 ± 2.14%). The encapsulation of HES in beads was assured by Fourier transform infrared spectroscopy study. The in vitro drug release kinetic of beads was performed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The results revealed negligible release of HES (3.52 ± 0.8%) from beads in SGF after 2 h, and in SIF (after 8 h), the beads showed burst release (72.52 ± 3.5%) of HES. Antidiabetic and histopathological studies on experimental rat revealed promising hypoglycemic activity of beads which sought for its ability to protect HES in the stomach. The shelf life of optimized bead formulation was estimated 1079 days suggesting excellent stability of HES after encapsulation. Finally, developed beads formulation was considered a promising approach in oral delivery of HES.

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Acknowledgment

We sincerely thank the Gattefosse Pvt. Ltd for providing a gratis sample of oil and surfactant, and STIC (Sophisticated Test and Instrumentation Center), Cochin, India, to analyze samples.

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Authors and Affiliations

  1. Department of Pharmaceutical Quality Assurance, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dist, Dhule, 425 405, India

    Pankaj V. Dangre, Poorva P. Dusad & Shailesh S. Chalikwar

  2. Department of Pharmacology, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dist, Dhule, 425 405, India

    Alok D. Singh

  3. Department of Pharmacognosy, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dist, Dhule, 425 405, India

    Sanjay J. Surana

  4. Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, 11201, USA

    Kaushalendra K. Chaturvedi

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  1. Pankaj V. Dangre
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Correspondence to Shailesh S. Chalikwar.

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Dangre, P.V., Dusad, P.P., Singh, A.D. et al. Fabrication of hesperidin self-micro-emulsifying nutraceutical delivery system embedded in sodium alginate beads to elicit gastric stability. Polym. Bull. 79, 605–626 (2022). https://doi.org/10.1007/s00289-020-03507-7

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  • DOI: https://doi.org/10.1007/s00289-020-03507-7

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