Beta-carotene/cyclodextrin-based inclusion complex: improved loading, solubility, stability, and cytotoxicity

IF 2.3 4区化学 Q2 Agricultural and Biological Sciences Journal of Inclusion Phenomena and Macrocyclic Chemistry Pub Date : 2021-08-25 DOI:10.1007/s10847-021-01100-7

Mahsa Yazdani, Omid Tavakoli, Mehdi Khoobi, Yi Shuan Wu, Mohammad Ali Faramarzi, Elham Gholibegloo, Shabnam Farkhondeh

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引用次数: 21

Abstract

Beta-carotene (BC) is a vitamin A precursor and has potential anticancer benefits, but the delivery of BC is hindered by its low solubility and storage instability. To overcome these challenges, this study investigated the use of fabricated cyclodextrin-based nanosponges (CDNS) using different ratios of two cross-linkers, epiclon (EPI) and hexamethylene diisocyanate (HMDI) to form inclusion complex with BC. The ratios of crosslinkers to βCD for two most optimaly encapsulated CDNSs-BC were determined to be 2:1 for EPI and 4:1 for HMDI with loading efficiency of 61.46% and 59.61%, respectively. The charachterization tests were carefully done for two optimal CDNSs. Encapsulation significantly improved the solubility by ~ 10 folds, 30-day storage stability by 40% compared to BCs. The in vitro release of the two encapsulated products showed no burst release. The MTT assay revealed a variable increase in cytotoxic effect in both normal and cancer cells compared to free BC. Overall, the CDNSs appear to be promising carriers for the delivery of BCs.

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β -胡萝卜素/环糊精包合物:改善负载，溶解度，稳定性和细胞毒性

β -胡萝卜素(BC)是一种维生素a前体，具有潜在的抗癌作用，但BC的低溶解度和储存不稳定阻碍了其输送。为了克服这些挑战，本研究研究了使用制备的环糊精基纳米海绵(CDNS)，使用不同比例的两种交联剂，epiclon (EPI)和hex亚甲基二异氰酸酯(HMDI)与BC形成包合物。结果表明，两种包封最优的CDNSs-BC交联剂与βCD的比例分别为:EPI为2:1,HMDI为4:1，其负载效率分别为61.46%和59.61%。对两种最佳cdns进行了仔细的表征试验。与bc相比，包封后的溶解度提高了10倍，30天的储存稳定性提高了40%。两种囊化产物的体外释放均无爆裂释放。MTT试验显示，与游离BC相比，正常细胞和癌细胞的细胞毒性作用都有所增加。总的来说，cdss似乎是交付bc的有希望的运营商。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Inclusion Phenomena and Macrocyclic Chemistry 化学-化学综合

CiteScore

3.30

自引率

8.70%

发文量

审稿时长

3-8 weeks

期刊介绍： The Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.