Folate conjugated albumin as a targeted nanocarrier for the delivery of fisetin: in silico and in vitro biological studies
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Date
2024-02
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Abstract
Fisetin (FST), a natural flavonoid compound derived from various fruits and vegetables, including apple,
strawberry, and onion, demonstrates potential for a wide range of pharmaceutical applications, including
potential anticancer properties. However, challenges such as low bioavailability, poor aqueous solubility,
and limited permeability restrict the use of FST in the pharmaceutical sector. Nowadays, targeted
nanomedicines have garnered attention to overcome limitations associated with phytochemicals, including
FST. In the present study, we have designed and successfully prepared folate-targeted FST nanoparticles
(FFNPs). Characterization through DLS and FE-SEM revealed the successful preparation of monodisperse
(PDI: 0.117), nanoscale-sized (150 nm), and spherical nanoparticles. Physicochemical characterization
including FTIR, XRD, DSC, and TGA analysis, confirmed the encapsulation of the FST within the Folic acid
(FA) – conjugated nanoparticles (CNPs) and revealed its amorphous nature. Molecular docking analysis
revealed the strong binding affinity and specific amino acid interactions involved in the BSA–FST–FA
complex, suggesting the potential synergistic effect of FST and FA in enhancing the therapeutic activity of
the FFANPs. Cytotoxic assessments by the MTT assay, migration assay, AO-EtBr staining assay, colony
formation assay, and cellular uptake study demonstrated enhanced anticancer efficacy, apoptosis
induction, and enhanced uptake of FFNPs compared to pure FST. These findings propose prepared FFNPs
as a promising targeted drug delivery nanocarrier for effective FST delivery in cancer therapy.