Design of chitosan colon delivery micro/nano particles for an Achillea millefolium extract with antiproliferative activity against colorectal cancer cells.

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Title: Design of chitosan colon delivery micro/nano particles for an Achillea millefolium extract with antiproliferative activity against colorectal cancer cells.
Authors: Siles-Sánchez, María de las Nieves1 (AUTHOR), Fernández-Jalao, Irene1 (AUTHOR), Jaime De Pablo, Laura1 (AUTHOR), Santoyo, Susana1 (AUTHOR) susana.santoyo@uam.es
Source: Drug Delivery. Dec2024, Vol. 31 Issue 1, p1-11. 11p.
Subject Terms: *COMMON yarrow, *PHENOLS, *MOLECULAR weights, *COLORECTAL cancer, *YARROW, *CHLOROGENIC acid, *SPRAY drying, *GELATION
Abstract: In this study, chitosan low molecular weight (LCH) and chitosan medium molecular weight (MCH) were employed to encapsulate a yarrow extract rich in chlorogenic acid and dicaffeoylquinic acids (DCQAs) that showed antiproliferative activity against colon adenocarcinoma cells. The design of CH micro/nanoparticles to increase the extract colon delivery was carried out by using two different techniques: ionic gelation and spray drying. Ionic gelation nanoparticles obtained were smaller and presented higher yields values than spray-drying microparticles, but spray-drying microparticles showed the best performance in terms of encapsulation efficiency (EE) (> 94%), also allowing the inclusion of a higher quantity of extract. Spray-drying microparticles designed using LCH with an LCH:extract ratio of 6:1 (1.25 mg/mL) showed a mean diameter of 1.31 ± 0.21 µm and EE values > 93%, for all phenolic compounds studied. The release profile of phenolic compounds included in this formulation, at gastrointestinal pHs (2 and 7.4), showed for most of them a small initial release, followed by an increase at 1 h, with a constant release up to 3 h. Chlorogenic acid presented the higher release values at 3 h (56.91% at pH 2; 44.45% at pH 7.4). DCQAs release at 3 h ranged between 9.01- 40.73%, being higher for 1,5- and 3,4-DCQAs. After gastrointestinal digestion, 67.65% of chlorogenic and most DCQAs remained encapsulated. Therefore, spray-drying microparticles can be proposed as a promising vehicle to increase the colon delivery of yarrow phenolics compounds (mainly chlorogenic acid and DCQAs) previously described as potential agents against colorectal cancer. [ABSTRACT FROM AUTHOR]
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Items – Name: Title
  Label: Title
  Group: Ti
  Data: Design of chitosan colon delivery micro/nano particles for an Achillea millefolium extract with antiproliferative activity against colorectal cancer cells.
– Name: Author
  Label: Authors
  Group: Au
  Data: <searchLink fieldCode="AR" term="%22Siles-Sánchez%2C+María+de+las+Nieves%22">Siles-Sánchez, María de las Nieves</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Fernández-Jalao%2C+Irene%22">Fernández-Jalao, Irene</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Jaime+De+Pablo%2C+Laura%22">Jaime De Pablo, Laura</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Santoyo%2C+Susana%22">Santoyo, Susana</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> susana.santoyo@uam.es</i>
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  Data: <searchLink fieldCode="JN" term="%22Drug+Delivery%22">Drug Delivery</searchLink>. Dec2024, Vol. 31 Issue 1, p1-11. 11p.
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  Data: *<searchLink fieldCode="DE" term="%22COMMON+yarrow%22">COMMON yarrow</searchLink><br />*<searchLink fieldCode="DE" term="%22PHENOLS%22">PHENOLS</searchLink><br />*<searchLink fieldCode="DE" term="%22MOLECULAR+weights%22">MOLECULAR weights</searchLink><br />*<searchLink fieldCode="DE" term="%22COLORECTAL+cancer%22">COLORECTAL cancer</searchLink><br />*<searchLink fieldCode="DE" term="%22YARROW%22">YARROW</searchLink><br />*<searchLink fieldCode="DE" term="%22CHLOROGENIC+acid%22">CHLOROGENIC acid</searchLink><br />*<searchLink fieldCode="DE" term="%22SPRAY+drying%22">SPRAY drying</searchLink><br />*<searchLink fieldCode="DE" term="%22GELATION%22">GELATION</searchLink>
– Name: Abstract
  Label: Abstract
  Group: Ab
  Data: In this study, chitosan low molecular weight (LCH) and chitosan medium molecular weight (MCH) were employed to encapsulate a yarrow extract rich in chlorogenic acid and dicaffeoylquinic acids (DCQAs) that showed antiproliferative activity against colon adenocarcinoma cells. The design of CH micro/nanoparticles to increase the extract colon delivery was carried out by using two different techniques: ionic gelation and spray drying. Ionic gelation nanoparticles obtained were smaller and presented higher yields values than spray-drying microparticles, but spray-drying microparticles showed the best performance in terms of encapsulation efficiency (EE) (> 94%), also allowing the inclusion of a higher quantity of extract. Spray-drying microparticles designed using LCH with an LCH:extract ratio of 6:1 (1.25 mg/mL) showed a mean diameter of 1.31 ± 0.21 µm and EE values > 93%, for all phenolic compounds studied. The release profile of phenolic compounds included in this formulation, at gastrointestinal pHs (2 and 7.4), showed for most of them a small initial release, followed by an increase at 1 h, with a constant release up to 3 h. Chlorogenic acid presented the higher release values at 3 h (56.91% at pH 2; 44.45% at pH 7.4). DCQAs release at 3 h ranged between 9.01- 40.73%, being higher for 1,5- and 3,4-DCQAs. After gastrointestinal digestion, 67.65% of chlorogenic and most DCQAs remained encapsulated. Therefore, spray-drying microparticles can be proposed as a promising vehicle to increase the colon delivery of yarrow phenolics compounds (mainly chlorogenic acid and DCQAs) previously described as potential agents against colorectal cancer. [ABSTRACT FROM AUTHOR]
– Name: AbstractSuppliedCopyright
  Label:
  Group: Ab
  Data: <i>Copyright of Drug Delivery is the property of Taylor & Francis Ltd and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
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      – Type: doi
        Value: 10.1080/10717544.2024.2372285
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      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        PageCount: 11
        StartPage: 1
    Subjects:
      – SubjectFull: COMMON yarrow
        Type: general
      – SubjectFull: PHENOLS
        Type: general
      – SubjectFull: MOLECULAR weights
        Type: general
      – SubjectFull: COLORECTAL cancer
        Type: general
      – SubjectFull: YARROW
        Type: general
      – SubjectFull: CHLOROGENIC acid
        Type: general
      – SubjectFull: SPRAY drying
        Type: general
      – SubjectFull: GELATION
        Type: general
    Titles:
      – TitleFull: Design of chitosan colon delivery micro/nano particles for an Achillea millefolium extract with antiproliferative activity against colorectal cancer cells.
        Type: main
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          Name:
            NameFull: Siles-Sánchez, María de las Nieves
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            NameFull: Fernández-Jalao, Irene
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            NameFull: Jaime De Pablo, Laura
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            NameFull: Santoyo, Susana
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            – D: 01
              M: 12
              Text: Dec2024
              Type: published
              Y: 2024
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            – TitleFull: Drug Delivery
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