New folate receptor targeted nano liposomes for delivery of 5-fluorouracil to cancer cells: Strong implication for enhanced potency and safety

Handali, Somayeh; Moghimipour, Eskandar; Kouchak, Maryam; Ramezani, Zahra; Amini, Mohsen; Angali, Kambiz Ahmadi; Saremy, Sadegh; Dorkoosh, Farid Abedin; Rezaeian, Mohsen

doi:10.1016/j.lfs.2019.04.030

Cited by 54 publications

(19 citation statements)

References 49 publications

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“…Folic acid (FA) is a member of the vitamin B family and is found widely in green leafy vegetables [18]. Studies have found that both free folate and folate conjugates can enter cells through folate receptor-mediated endocytosis [19,20]. Overexpression of the folate receptor has been found on the surface of most malignant tumors, but few exist on the surface of normal cells [21].…”

Section: Introductionmentioning

confidence: 99%

Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

et al. 2019

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Nano anti-cancer drug carriers loaded with antineoplastic drugs can achieve targeted drug delivery, which enriches drugs at tumor sites and reduces the toxic side effects in normal tissues. Mesoporous silica nanoparticles (MSN) are good nano drug carriers, as they have large specific surface areas, adjustable pore sizes, easily modifiable surfaces, and good biocompatibility. In this work, polyethyleneimine (PEI) grafted MSN were modified with folic acid (FA) as an active target molecule using chemical methods. The product was characterized by SEM, TEM, Zetasizer nano, FTIR, and an N2 adsorption and desorption test. MSN-PEI-FA are porous nano particles with an average particle size of approximately 100 nm. In addition, the loading rate and release behavior of MSN-PEI-FA were studied with curcumin as a model drug. The results show that when loading curcumin to MSN-PEI-FA at 7 mg and 0.1 g, respectively, the encapsulation efficiency was 90% and the cumulative release rate reached more than 50% within 120 h at pH = 5. This drug delivery system is suitable for loading fat-soluble antineoplastic drugs for sustained release and pH sensitive delivery.

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Section: Introductionmentioning

confidence: 99%

Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

et al. 2019

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“…Moreover, FA modification can further enhance the retention of liposomes in the tumor and facilitate its uptake via FR-mediated endocytosis, enabling the drug to target FR-overexpressed tumors more precisely and efficiently [74]. Until now, two types of folate conjugation to the phospholipids have been used: (a) uncleavable folate conjugation [75,76,77,78,79,80], and (b) cleavable folate conjugation [81].…”

Section: Design and Fabrication Of Folate-conjugated Liposomesmentioning

confidence: 99%

Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications

2019

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The folate receptor (FR) is a tumor-associated antigen that can bind with folic acid (FA) and its conjugates with high affinity and ingests the bound molecules inside the cell via the endocytic mechanism. A wide variety of payloads can be delivered to FR-overexpressed cells using folate as the ligand, ranging from small drug molecules to large DNA-containing macromolecules. A broad range of folate attached liposomes have been proven to be highly effective as the targeted delivery system. For the rational design of folate-targeted liposomes, an intense conceptual understanding combining chemical and biomedical points of view is necessary because of the interdisciplinary nature of the field. The fabrication of the folate-conjugated liposomes basically involves the attachment of FA with phospholipids, cholesterol or peptides before liposomal formulation. The present review aims to provide detailed information about the design and fabrication of folate-conjugated liposomes using FA attached uncleavable/cleavable phospholipids, cholesterol or peptides. Advances in the area of folate-targeted liposomes and their biomedical applications have also been discussed.

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“…The excellent biocompatibility and safety of this FA receptor-targeting strategy were verified by hemolytic assays and histological examinations. In a similar study, S. Handali et al confirmed that the in vitro cytotoxicity (tested by MTT assay) of an FA-coated liposomal 5-fluorouracil formulation was much higher than those of conventional liposomes and free 5-fluorouracil against various CRC cell lines (e.g., HT29, Caco2, and CT26 cells) [ 34 , 142 ]. The targeted liposomes were also found to induce necrosis in vitro in HT29 cells.…”

Section: Deliverable Targets For Crc Treatmentmentioning

confidence: 91%

“…For example, FA receptors and transporters are overexpressed in many types of cancers, including CRC. Therefore FA-coated liposomes are expected to exhibit increased uptake by cancer cells with overexpressed folate receptors [ 141 , 142 ]. E. Moghimipour et al showed that, in CT26 cells, FA-decorated liposomal 5-fluorouracil exhibited enhanced cellular uptake of the encapsulated 5-fluorouracil compared to free 5-fluorouracil, with a three-fold decrease in the IC 50 (12.02 versus 39.81 µM, respectively) and 25-fold higher ROS production (62,271.28 versus 2369.55 a.u., respectively, as shown by fluorescence intensity) [ 69 ].…”

Section: Deliverable Targets For Crc Treatmentmentioning

confidence: 99%

Lipid-Based Drug Delivery Nanoplatforms for Colorectal Cancer Therapy

Yang

Merlin

2020

Nanomaterials

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Colorectal cancer (CRC) is a prevalent disease worldwide, and patients at late stages of CRC often suffer from a high mortality rate after surgery. Adjuvant chemotherapeutics (ACs) have been extensively developed to improve the survival rate of such patients, but conventionally formulated ACs inevitably distribute toxic chemotherapeutic drugs to healthy organs and thus often trigger severe side effects. CRC cells may also develop drug resistance following repeat dosing of conventional ACs, limiting their effectiveness. Given these limitations, researchers have sought to use targeted drug delivery systems (DDSs), specifically the nanotechnology-based DDSs, to deliver the ACs. As lipid-based nanoplatforms have shown the potential to improve the efficacy and safety of various cytotoxic drugs (such as paclitaxel and vincristine) in the clinical treatment of gastric cancer and leukemia, the preclinical progress of lipid-based nanoplatforms has attracted increasing interest. The lipid-based nanoplatforms might be the most promising DDSs to succeed in entering a clinical trial for CRC treatment. This review will briefly examine the history of preclinical research on lipid-based nanoplatforms, summarize the current progress, and discuss the challenges and prospects of using such approaches in the treatment of CRC.

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New folate receptor targeted nano liposomes for delivery of 5-fluorouracil to cancer cells: Strong implication for enhanced potency and safety

Cited by 54 publications

References 49 publications

Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications

Lipid-Based Drug Delivery Nanoplatforms for Colorectal Cancer Therapy

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