负载大麻二酚的纳米脂质载体增强其对小肠的生物可及性

L. Grifoni, G. Vanti, A. Bilia
{"title":"负载大麻二酚的纳米脂质载体增强其对小肠的生物可及性","authors":"L. Grifoni, G. Vanti, A. Bilia","doi":"10.3390/nutraceuticals3020016","DOIUrl":null,"url":null,"abstract":"The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.","PeriodicalId":93800,"journal":{"name":"Nutraceuticals","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine\",\"authors\":\"L. Grifoni, G. Vanti, A. Bilia\",\"doi\":\"10.3390/nutraceuticals3020016\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.\",\"PeriodicalId\":93800,\"journal\":{\"name\":\"Nutraceuticals\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-04-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nutraceuticals\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3390/nutraceuticals3020016\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nutraceuticals","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/nutraceuticals3020016","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 1

摘要

本研究的目的是研究非精神活性大麻二酚(CBD)在新型纳米结构脂质载体(NLC)中的负载特性,评估其在胃肠模拟生理介质中的生物可及性。CBD的水溶性很低,在模拟生理条件下和酸性介质中也很不稳定,这导致生物利用度非常低,低于6%。配制含有CBD(10 mg/mL)、Compritol 888 ATO、Lauroglycol 90、Labrafil 2125、Tween 20和Poloxamer 188的NLCs。这使得它们适合口服给药,因为其尺寸小于200 nm,多分散指数为0.152,ζ-电位为−39.21±1.89 mV。回收率和包封率分别为100%和93%。在模拟胃液(SGF)中孵育两小时后,NLCs保持不变,保护CBD免受酸性介质的影响。事实上,据报道,CBD在37°C pH=7.4的介质中也不稳定,但我们的研究证明,在肠液存在的情况下,NLC被消化并形成乳液,可以保护和保存CBD的化学结构,6小时后发现的100%回收率证实了这一点。因此,CBD负载的NLCs是一种很有前途的口服制剂,可以优化小肠的生物可及性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Nanostructured Lipid Carriers Loaded with Cannabidiol Enhance Its Bioaccessibility to the Small Intestine
The purpose of this study was to investigate the loading properties of the non-psychoactive cannabidiol (CBD) in a new nanostructured lipid carrier (NLC), evaluating its bioaccessibility in gastric and intestinal simulated physiological media. CBD has a low water solubility, as well as high instability in simulated physiological conditions and in the acidic media, which results in a very low bioavailability—less than 6%. NLCs containing CBD (10 mg/mL), Compritol 888 ATO, Lauroglycol 90, Labrafil 2125, Tween 20, and Poloxamer 188 were formulated. This resulted in them being suitable for oral administration because the size was less than 200 nm, polydispersity index 0.152, and ζ-potential −39.21 ± 1.89 mV. Recovery and encapsulation efficiency were 100% and 93%, respectively. After two hours of incubation in simulated gastric fluid (SGF), NLCs remained unchanged, protecting CBD from acidic medium. Indeed, CBD is also reported to be not stable in media with pH = 7.4 at 37 °C, but our studies evidenced that in the presence of the intestinal fluid, the NLC was digested and formed an emulsion, which can protect and preserve the CBD chemical structure, as confirmed by the 100% recovery found after six hours. Accordingly, CBD-loaded NLCs are a promising oral formulation that optimize bioaccessibility in the small intestine.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信