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

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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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Author information

Authors and Affiliations

  1. Mechanical Engineering Department, School of Computing and Engineering, University of Missouri-Kansas City, Kansas City, MO, 64110, USA

    Mahsa Yazdani

  2. School of Chemical Engineering, College of Engineering, University of Tehran, 14176, Tehran, Iran

    Mahsa Yazdani & Omid Tavakoli

  3. Biomaterials Group, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, 1417614411, Tehran, Iran

    Mehdi Khoobi, Elham Gholibegloo & Shabnam Farkhondeh

  4. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, 14176-53955, Tehran, Iran

    Mehdi Khoobi

  5. Division of Pharmacotherapy and Experimental Therapeutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA

    Yi Shuan Wu

  6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, 14174, Tehran, Iran

    Mohammad Ali Faramarzi

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  1. Mahsa Yazdani
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  2. Omid Tavakoli
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  3. Mehdi Khoobi
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  4. Yi Shuan Wu
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  7. Shabnam Farkhondeh
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Contributions

MY: Methodology, Validation, Formal analysis, Investigation, Resources, Data Curation, Writing—Original Draft, Writing—Review & Editing, Visualization. OT: Project administration, Supervision, Conceptualization. MK: Conceptualization, Validation, Supervision. YSW: Writing—Review & Editing, Visualization. MAF: Resources. EG: Supervision, Investigation. SF: Investigation.

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Correspondence to Omid Tavakoli.

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Yazdani, M., Tavakoli, O., Khoobi, M. et al. Beta-carotene/cyclodextrin-based inclusion complex: improved loading, solubility, stability, and cytotoxicity. J Incl Phenom Macrocycl Chem 102, 55–64 (2022). https://doi.org/10.1007/s10847-021-01100-7

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