Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions

Cyclolinopeptides (CLs) have anti-inflammatory, anti-osteoporosis, and anti-tumor effects, however, low water and oil solubility greatly limit their application. Herein, CLs-loaded β-cyclodextrin (β-CD) emulsions were prepared with different oil phases. The in vitro digestibility, cellular absorptio...

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Main Authors: Liu, Zhongbo, Lee, Yee Ying, Tan, Chin Ping, Wang, Yong, Qiu, Chaoying
Format: Article
Language:English
Published: Elsevier Ltd 2025
Online Access:http://psasir.upm.edu.my/id/eprint/118709/
http://psasir.upm.edu.my/id/eprint/118709/1/118709.pdf
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author Liu, Zhongbo
Lee, Yee Ying
Tan, Chin Ping
Wang, Yong
Qiu, Chaoying
author_facet Liu, Zhongbo
Lee, Yee Ying
Tan, Chin Ping
Wang, Yong
Qiu, Chaoying
author_sort Liu, Zhongbo
building UPM Institutional Repository
collection Online Access
description Cyclolinopeptides (CLs) have anti-inflammatory, anti-osteoporosis, and anti-tumor effects, however, low water and oil solubility greatly limit their application. Herein, CLs-loaded β-cyclodextrin (β-CD) emulsions were prepared with different oil phases. The in vitro digestibility, cellular absorption, and anti-inflammatory effects were evaluated. Camellia oil diacylglycerol (CO DAG) showed enhanced dissolving ability for CLs due to high polarity. β-CD formed inclusion complexes with DAG through hydrogen bond and the emulsions showed smaller size and higher physical stability with 50 % (w/w) oil. The in vitro digestibility of the DAG emulsion was increased and the CLs' bioavailability was 13.6–fold higher than CLs in oil. The CLs–loaded Pickering emulsion digesta exhibited a higher nitric oxides (NO) inhibition rate (58.62 %) and Caco-2 cell penetration (3.09 × 10−6 cm/s). Therefore, emulsion formulated with β-cyclodextrin and DAG can effectively improve the solubility and bioavailability of CLs, which has significant potential for application in functional foods and pharmaceutical industry.
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spelling upm-1187092025-07-22T07:17:35Z http://psasir.upm.edu.my/id/eprint/118709/ Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions Liu, Zhongbo Lee, Yee Ying Tan, Chin Ping Wang, Yong Qiu, Chaoying Cyclolinopeptides (CLs) have anti-inflammatory, anti-osteoporosis, and anti-tumor effects, however, low water and oil solubility greatly limit their application. Herein, CLs-loaded β-cyclodextrin (β-CD) emulsions were prepared with different oil phases. The in vitro digestibility, cellular absorption, and anti-inflammatory effects were evaluated. Camellia oil diacylglycerol (CO DAG) showed enhanced dissolving ability for CLs due to high polarity. β-CD formed inclusion complexes with DAG through hydrogen bond and the emulsions showed smaller size and higher physical stability with 50 % (w/w) oil. The in vitro digestibility of the DAG emulsion was increased and the CLs' bioavailability was 13.6–fold higher than CLs in oil. The CLs–loaded Pickering emulsion digesta exhibited a higher nitric oxides (NO) inhibition rate (58.62 %) and Caco-2 cell penetration (3.09 × 10−6 cm/s). Therefore, emulsion formulated with β-cyclodextrin and DAG can effectively improve the solubility and bioavailability of CLs, which has significant potential for application in functional foods and pharmaceutical industry. Elsevier Ltd 2025-02-01 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/118709/1/118709.pdf Liu, Zhongbo and Lee, Yee Ying and Tan, Chin Ping and Wang, Yong and Qiu, Chaoying (2025) Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions. Food Chemistry, 464. art. no. 141553. pp. 1-12. ISSN 0308-8146; eISSN: 1873-7072 https://linkinghub.elsevier.com/retrieve/pii/S0308814624032035 10.1016/j.foodchem.2024.141553
spellingShingle Liu, Zhongbo
Lee, Yee Ying
Tan, Chin Ping
Wang, Yong
Qiu, Chaoying
Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title_full Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title_fullStr Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title_full_unstemmed Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title_short Improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin Pickering emulsions
title_sort improved solubility and bioavailability of cyclolinopeptides by diacylglycerol in the β-cyclodextrin pickering emulsions
url http://psasir.upm.edu.my/id/eprint/118709/
http://psasir.upm.edu.my/id/eprint/118709/
http://psasir.upm.edu.my/id/eprint/118709/
http://psasir.upm.edu.my/id/eprint/118709/1/118709.pdf