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Development of Morin-Loaded Nanoemulsions Containing Various Polymers; Role of Polymers in Formulation Properties and Bioavailability

AAPS PharmSciTech volume 21, Article number: 150 (2020) Cite this article

Abstract

Emulsions for oral delivery are not suitable for sustained drug absorption because such preparations diffuse rapidly in the gastrointestinal (GI) tract after oral administration. In order to generate sustained drug absorption and increase oral bioavailability, various polymers were added to a morin (MO) nanoemulsion to improve retention in the GI tract and alter the surface properties of oil droplets in the nanoemulsion. The influence of these polymers on the formulation properties was investigated. The area under the blood concentration–time curve (AUC) and the mean residence time (MRT) after oral administration of the nanoemulsions were measured, and the influence of the polymers on bioavailability was investigated. Chitosan (Chi) addition MO nanoemulsion (MO-Chi nanoemulsion) showed the highest AUC and MRT. MO-Chi nanoemulsion increased retention in the GI tract because of the relatively higher viscosity and high affinity between mucin and Chi covering the oil droplets. Furthermore, MO-Chi nanoemulsion could maintain the drug in oil droplets by suppression of drug release through the polymer hydration layer, and sustained drug release achieved continuous drug absorption. Nanoemulsions with sodium carboxymethylcellulose and poly-γ-glutamic acid potassium salt showed the next highest AUC and MRT after MO-Chi nanoemulsion. From these results, it was suggested that by increasing the viscosity of the nanoemulsion, there was high affinity between the added polymer and mucin, and sustained drug release was useful for enhancing the bioavailability of the polymer-containing nanoemulsions.

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Funding

The authors received funding from Mitsubishi Chemical Corporation, Tokyo, Japan.

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Affiliations

  1. Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo, 142-8501, Japan

    Yuri Ikeuchi-Takahashi, Shingo Murata, Wataru Murata & Hiraku Onishi

  2. Osaka R&D Center, Mitsubishi Chemical Corporation, Ibaraki, Osaka, Japan

    Ayaka Kobayashi & Chizuko Ishihara

Authors
  1. Yuri Ikeuchi-Takahashi
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  2. Shingo Murata
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  3. Wataru Murata
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  4. Ayaka Kobayashi
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  5. Chizuko Ishihara
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  6. Hiraku Onishi
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Correspondence to Yuri Ikeuchi-Takahashi.

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Ikeuchi-Takahashi, Y., Murata, S., Murata, W. et al. Development of Morin-Loaded Nanoemulsions Containing Various Polymers; Role of Polymers in Formulation Properties and Bioavailability. AAPS PharmSciTech 21, 150 (2020). https://doi.org/10.1208/s12249-020-01670-8

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  • DOI: https://doi.org/10.1208/s12249-020-01670-8

KEY WORDS

  • polymer-containing nanoemulsion
  • morin
  • bioavailability
  • sustained drug release
  • viscosity