Folic Acid Decorated Zeolitic Imidazolate Framework (ZIF-8) Loaded with Baicalin as a Nano-Drug Delivery System for Breast Cancer Therapy

Abstract

Background Baicalin (BAN) has attracted widespread attention due to its low-toxicity and efficient antitumor activity, but its poor water solubility and low bioavailability severely limit its clinical application. Development of a targeted drug delivery system is a good strategy to improve the antitumor activity of baicalin. Methods We prepared a BAN nano-drug delivery system PEG-FA@ZIF-8@BAN with a zeolite imidazole framework-8 (ZIF-8) as a carrier, which can achieve the response of folate receptor (FR). We characterized this system in terms of morphology, particle size, zeta-potential, infrared (IR), ultraviolet (UV), x-ray diffraction (XRD), and Brunel-Emmett-Teller (BET), and examined the in vitro cytotoxicity and cellular uptake properties of PEG-FA@ZIF-8@BAN using MCF-7 cells. Lastly, we established a 4T1 tumor-bearing mouse model and evaluated its in vivo anti-mammary cancer activity. Results The PEG-FA@ZIF-8@BAN nano-delivery system had good dispersion with a BAN loading efficiency of 41.45 ± 1.43%, hydrated particle size of 176 ± 8.1 nm, Zeta-potential of −23.83 ± 1.1 mV, and slow and massive drug release in an acidic environment (pH 5.0), whereas release was 11.03% in a neutral environment (pH 7.4). In vitro studies showed that PEG-FA@ZIF-8@BAN could significantly enhance the killing effect of BAN on MCF-7 cells, and the folic acid-mediated targeting could lead to better uptake of nanoparticles by tumor cells and thus better killing of cancer cells. In vivo studies also showed that PEG-FA@ZIF-8@BAN significantly increased the inhibition of the proliferation of solid breast cancer tumors ( p < 0.01 or p < 0.001). Conclusion The PEG-FA@ZIF-8@BAN nano-drug delivery system significantly enhanced the anti-breast cancer effect of baicalin both in vivo and in vitro, providing a more promising drug delivery system for the clinical applications and tumor management.

Baicalin regulates stem cells as a creative point in the treatment of climacteric syndrome

“…Further research is warranted on the in vivo transformation of the two and the combined regulation of stem cells. Furthermore, Baicalin has poor water solubility and a limited bioavailability ( Mi et al, 2021 ), limiting its future clinical applicability. To increase medication usage, dosage formulations such as cyclodextrin inclusion and hydrogel are currently being explored ( Li et al, 2018 ; Wang et al, 2022 ).…”

Highly Biocompatible Apigenin-Loaded Silk Fibroin Nanospheres: Preparation, Characterization, and Anti-Breast-Cancer Activity

“…As for breast cancer patients who are clinically diagnosed with cancer spread or recurrence, especially those in an advanced stage, chemotherapy is usually used to significantly prolong the survival time of patients [ 3 ]. Unfortunately, chemotherapy is usually associated with adverse effects such as side effects and drug resistance as well as long treatment cycles and high treatment costs [ 4 ]. Compared with other medications, plant-derived compounds and secondary metabolites have low side effects and are attractive drugs for breast cancer treatment [ 5 ].…”

Combined Biomimetic MOF-RVG15 Nanoformulation Efficient Over BBB for Effective Anti-Glioblastoma in Mice Model

“… 43 This pH-sensitive degradation makes ZIF-8 nanoparticles a promising nanodrug delivery system for tumor treatment. 44–47 …”

“…43 This pH-sensitive degradation makes ZIF-8 nanoparticles a promising nanodrug delivery system for tumor treatment. [44][45][46][47] Docetaxel (DTX) is a broad-spectrum antineoplastic drug, derived from paclitaxel, which was developed by Planck Le Rhone. As a first-line strategy against various types of cancers, DTX is used clinically for the treatment of breast, ovarian, non-small cell lung, and prostate cancers.…”