Synthesis, characterisation and photo-stability of a folate-modified β-cyclodextrin as a functional food additive.

A novel two-step synthetic route was developed and gave the mono-substituted derivative 6-deoxy-6-[(1-(2-amino)ethylamino)folate]-b-cyclodextrin (CDEnFA) with high yield (60 %). Elemental analysis, mass spectrometry, 1H and 13C NMR, FTIR and Raman spectroscopies demonstrated the successful synthesis of the γ isomer only with no evidence of the presence of other isomers or free folic acid. Electronic absorption spectroscopy was used to study the photochemical properties of CDEnFA and showed that in both the solid state and aqueous solution CDEnFA is considerably more photo-stable than free folic acid

In Vitro Evaluation of the Cytotoxicity of a Folate-modified β-cyclodextrin as a New Anti-cancer Drug Delivery System

Many chemotherapeutic drugs are therapeutically non-selective and do not distinguish between healthy cells and tumour cells which can result in severe side effects and toxicity. Drug delivery systems can be used to target specific cells and therefore may eliminate many of the side effects, increasing drug efficiency and efficacy, and controlling drug release. One possible strategy for targeted drug delivery is to use unique molecular markers such as folate receptors in cancer cells. In this work the cytotoxicity of a novel cyclodextrin-folate conjugate, 6-deoxy-6-[(1-(-2amino)ethylamino)folate-β-cyclodextrin (CDEnFA) was studied using the MTT assay and the MCF-7 (Breast), HeLa (Cervical), A549 (Lung cancer) and BEAS-2B (normal Lung) cell lines. The MTT assay showed that the drug delivery vehicle CDEnFA is not cytotoxic towards the cell lines studied even towards the normal BEAS-2B cell line and therefore it is expected that it is safe for medical use. The inclusion complex CDEnFA:MTX has superior cytotoxic activity towards all of the cancer cell lines studied compared to the drug MTX alone and CDEnFA:MTX is four times less cytotoxic than the drug towards the normal cell line. The observed toxicity is attributed solely to MTX since CDEnFA did not exhibit significant cytotoxicity. These results also suggest that the drug remains bioactive even after inclusion in the CD cavity. The cytotoxicity trend observed for CDEnFA:MTX in this study is MCF-7 (Breast) \u3e A549 (Lung) \u3e HeLa (Cervical) \u3e BEAS-2B (normal Lung)

Photochemical Studies of Nutraceuticals in the Presence of Cyclodextrins

The photostability studies of Folic acid and Menadione Sodium Bisulfite, also known as vitamin K3, were carried out in their aqueous solutions at room temperature. Solutions of Folic acid ( 4.8 x 10-5 M) and Menadione Sodium Bisulfite (4.0 x 10-4 M) were exposed to ultraviolet radiation at a wavelength of 365 nm. During exposure absorbance of both solutions was measured using a Perkin Elmer Lamda 900 UV/VIS/NIR Spectrometer. During the stability tests it was noted that addition of β Cyclodextrin (1:1 ratio) to aqueous solutions containing the vitamin slowed down the photodegradation process. The unique shape of Cyclodextrins allows whole or partial inclusion of nutrients inside their cavity. The obtained results suggests that the physical mixture of β-Cyclodextrin with Folic acid or vitamin K3 enhances the photostability of the nutrient

Folate-cyclodextrin Conjugate for Targeted Chemotherapy

A general disadvantage of chemotherapy is that the drugs cannot discriminate between fast-growing cancer cells and normal healthy cells which causes many side-effects such as hair loss. An ideal solution to current methods of chemotherapy would be the development of a carrier for an anticancer drug which would be able to transport the drug and therefore target only cancer cells and release the drug molecules inside the cells. In this work folic acid (FA) is attached to an aminoalkane derivative of b-cyclodextrin (CDEn) with a view to developing novel drug delivery systems for therapeutic purposes. Cytotoxisity of folate-conjugate (CDEnFA) is tested on folate over-expressing cell line (HeLa cells) and folate receptor deficient cell line (A549 cells). EC50 values compared to standard (Cisplatin)