Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin
Cardiovascular diseases are caused by hypercholesterolemia. Astaxanthin (AST) has been reported to exhibit antioxidant and anti-inflammatory properties. However, its bioavailability is poor because of low solubility and instability. In order to improve the bioavailability of AST, we developed an int...
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American Chemical Society
2024
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| Online Access: | http://psasir.upm.edu.my/id/eprint/120121/ https://pubs.acs.org/doi/10.1021/acs.jafc.3c08697 |
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| author | Liu, Aiyang He, Mengxue Liu, Chunhuan Ye, Zhan Tan, Chin-Ping Liu, Yanjun Gong, Jiajia Lei, Jingnan He, Yuan Zhu, Shuang Zhao, Jialiang Xu, Yong-Jiang Liu, Yuanfa |
| author_facet | Liu, Aiyang He, Mengxue Liu, Chunhuan Ye, Zhan Tan, Chin-Ping Liu, Yanjun Gong, Jiajia Lei, Jingnan He, Yuan Zhu, Shuang Zhao, Jialiang Xu, Yong-Jiang Liu, Yuanfa |
| author_sort | Liu, Aiyang |
| building | UPM Library |
| collection | Institutional Repository |
| content_provider | Universiti Putra Malaysia |
| content_source | UPM Institutional Repository |
| continent | Asia |
| country | Malaysia |
| description | Cardiovascular diseases are caused by hypercholesterolemia. Astaxanthin (AST) has been reported to exhibit antioxidant and anti-inflammatory properties. However, its bioavailability is poor because of low solubility and instability. In order to improve the bioavailability of AST, we developed an intestinal-responsive composite carrier termed as “liposomes in micropheres” incorporating N-succinyl-chitosan (NSC)-poly(ethylene glycol) (PEG) liposomes that functionalized by neonatal Fc receptors (FcRn) into hydrogels of sodium alginate (SA) and carboxymethyl chitosan (CMCS). In the AST NSC/HSA-PEG liposomes@SA/CMCS microspheres, the AST’s encapsulation efficiency (EE) was 96.26% (w/w) and its loading capacity (LC) was 6.47% (w/w). AST NSC/HSA-PEG liposomes had stability in the gastric conditions and achieved long-term release of AST in intestinal conditions. Then, AST NSC/HSA-PEG liposomes@SA/CMCS bind to intestinal epithelial cell targets by the neonatal Fc receptor. In vitro permeation studies show that there was a 4-fold increase of AST NSC/HSA-PEG liposomes@SA/CMCS in AST permeation across the intestinal epithelium. Subsequent in vivo experiments demonstrated that the composite carrier exhibited a remarkable mucoadhesive capacity, allowing for extended intestinal retention of up to 12 h, and it displayed deep penetration through the mucus layer, efficiently entering the intestinal villi epithelial cells, and enhancing the absorption of AST and its bioavailability in vivo. And oral administration of AST NSC/HSA-PEG liposomes@SA/CMCS could effectively prevent hypercholesterolemia caused by a high-fat, high-cholesterol diet (HFHCD). These advancements highlight the potential of NSC/HSA-PEG liposomes@SA/CMCS composite carriers for targeted and oral uptake of hydrophobic bioactives. |
| format | Article |
| id | my.upm.eprints-120121 |
| institution | Universiti Putra Malaysia |
| publishDate | 2024 |
| publisher | American Chemical Society |
| record_format | eprints |
| spelling | my.upm.eprints-1201212025-10-30T03:40:21Z http://psasir.upm.edu.my/id/eprint/120121/ Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin Liu, Aiyang He, Mengxue Liu, Chunhuan Ye, Zhan Tan, Chin-Ping Liu, Yanjun Gong, Jiajia Lei, Jingnan He, Yuan Zhu, Shuang Zhao, Jialiang Xu, Yong-Jiang Liu, Yuanfa Cardiovascular diseases are caused by hypercholesterolemia. Astaxanthin (AST) has been reported to exhibit antioxidant and anti-inflammatory properties. However, its bioavailability is poor because of low solubility and instability. In order to improve the bioavailability of AST, we developed an intestinal-responsive composite carrier termed as “liposomes in micropheres” incorporating N-succinyl-chitosan (NSC)-poly(ethylene glycol) (PEG) liposomes that functionalized by neonatal Fc receptors (FcRn) into hydrogels of sodium alginate (SA) and carboxymethyl chitosan (CMCS). In the AST NSC/HSA-PEG liposomes@SA/CMCS microspheres, the AST’s encapsulation efficiency (EE) was 96.26% (w/w) and its loading capacity (LC) was 6.47% (w/w). AST NSC/HSA-PEG liposomes had stability in the gastric conditions and achieved long-term release of AST in intestinal conditions. Then, AST NSC/HSA-PEG liposomes@SA/CMCS bind to intestinal epithelial cell targets by the neonatal Fc receptor. In vitro permeation studies show that there was a 4-fold increase of AST NSC/HSA-PEG liposomes@SA/CMCS in AST permeation across the intestinal epithelium. Subsequent in vivo experiments demonstrated that the composite carrier exhibited a remarkable mucoadhesive capacity, allowing for extended intestinal retention of up to 12 h, and it displayed deep penetration through the mucus layer, efficiently entering the intestinal villi epithelial cells, and enhancing the absorption of AST and its bioavailability in vivo. And oral administration of AST NSC/HSA-PEG liposomes@SA/CMCS could effectively prevent hypercholesterolemia caused by a high-fat, high-cholesterol diet (HFHCD). These advancements highlight the potential of NSC/HSA-PEG liposomes@SA/CMCS composite carriers for targeted and oral uptake of hydrophobic bioactives. American Chemical Society 2024-03-13 Article PeerReviewed Liu, Aiyang and He, Mengxue and Liu, Chunhuan and Ye, Zhan and Tan, Chin-Ping and Liu, Yanjun and Gong, Jiajia and Lei, Jingnan and He, Yuan and Zhu, Shuang and Zhao, Jialiang and Xu, Yong-Jiang and Liu, Yuanfa (2024) Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin. Journal of Agricultural and Food Chemistry, 72 (12). pp. 6118-6132. ISSN 0021-8561; eISSN: 1520-5118 https://pubs.acs.org/doi/10.1021/acs.jafc.3c08697 10.1021/acs.jafc.3c08697 |
| spellingShingle | Liu, Aiyang He, Mengxue Liu, Chunhuan Ye, Zhan Tan, Chin-Ping Liu, Yanjun Gong, Jiajia Lei, Jingnan He, Yuan Zhu, Shuang Zhao, Jialiang Xu, Yong-Jiang Liu, Yuanfa Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title | Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title_full | Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title_fullStr | Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title_full_unstemmed | Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title_short | Prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| title_sort | prevention of hypercholesterolemia with “liposomes in microspheres” composite carriers: a promising approach for intestinal-targeted oral delivery of astaxanthin |
| url | http://psasir.upm.edu.my/id/eprint/120121/ https://pubs.acs.org/doi/10.1021/acs.jafc.3c08697 |
| url_provider | http://psasir.upm.edu.my/ |