Beta-Carotene/Cyclodextrin-Based Inclusion Complex: Improved Loading, Solubility, Stability, and Cytotoxicity Publisher



Yazdani M^{1, 2} ; Tavakoli O² ; Khoobi M^{3, 4} ; Wu YS⁵ ; Faramarzi MA⁶ ; Gholibegloo E³ ; Farkhondeh S³
Source: Journal of Inclusion Phenomena and Macrocyclic Chemistry Published:2022

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. © 2021, The Author(s), under exclusive licence to Springer Nature B.V.