2019
DOI: 10.3390/pharmaceutics11080381
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Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications

Abstract: 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 desig… Show more

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Cited by 81 publications
(59 citation statements)
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References 162 publications
(165 reference statements)
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“…The functionalization of the liposomes surface with different ligands, such as peptides, monoclonal antibodies, aptamers, growth factors, sensitively ameliorates the specificity of the liposome interaction with target sites (targeted drug delivery) [176,177]. Folate receptor (FR) is one of the most commonly employed tumor-associated antigens that can bind (with high affinity) with folic acid (FA) and its conjugates and is able to ingest the bound molecules inside the targeted cells via the endocytic pathway [178]. Folate ligands have been largely employed for the delivery, to FR-overexpressed cells, of different anticancer drugs (including Doxorubricin, Methotrexate, Vincristine, Paclitaxel), up to large macromolecules containing DNA, which proved to be highly effective as targeted drug delivery system [178].…”
Section: Lipidsmentioning
confidence: 99%
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“…The functionalization of the liposomes surface with different ligands, such as peptides, monoclonal antibodies, aptamers, growth factors, sensitively ameliorates the specificity of the liposome interaction with target sites (targeted drug delivery) [176,177]. Folate receptor (FR) is one of the most commonly employed tumor-associated antigens that can bind (with high affinity) with folic acid (FA) and its conjugates and is able to ingest the bound molecules inside the targeted cells via the endocytic pathway [178]. Folate ligands have been largely employed for the delivery, to FR-overexpressed cells, of different anticancer drugs (including Doxorubricin, Methotrexate, Vincristine, Paclitaxel), up to large macromolecules containing DNA, which proved to be highly effective as targeted drug delivery system [178].…”
Section: Lipidsmentioning
confidence: 99%
“…Folate receptor (FR) is one of the most commonly employed tumor-associated antigens that can bind (with high affinity) with folic acid (FA) and its conjugates and is able to ingest the bound molecules inside the targeted cells via the endocytic pathway [178]. Folate ligands have been largely employed for the delivery, to FR-overexpressed cells, of different anticancer drugs (including Doxorubricin, Methotrexate, Vincristine, Paclitaxel), up to large macromolecules containing DNA, which proved to be highly effective as targeted drug delivery system [178]. For example, folate-conjugated liposomes evidenced an efficient internalization (though FR-α-mediated endocytosis) in H1299 cells.…”
Section: Lipidsmentioning
confidence: 99%
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“…The delivery of cargo in non-targeted liposomes is mediated by the EPR effect [205]. Nevertheless, in the last years, targeted liposomal formulations have been described and particularly folate-conjugated liposomes that involves the attachment of folic acid with phospholipids, cholesterol or peptides before liposomal formulation synthesis has been developed (for a review see [206]). The most common application of liposomes in gene delivery is to carry DNA into the cells [22].…”
Section: Lipid Basedmentioning
confidence: 99%
“…FA can be easily internalized in a nondestructive manner into cancerous cells via endocytic pathway that facilitates delivery of folate-conjugated anticancer drug payloads into cells in the same receptormediated process called a Trojan horse strategy (9)(10)(11). To date, treatments that involve folate-targeted approaches were extensively studied in context of variety of therapeutic cargos, including chemotherapeutic agents, imaging agents, oligonucleotides and DNA molecules (12). One of the widely used chemotherapeutic agent is doxorubicin, a topoisomerase inhibitor that interaction with DNA leads to growth suppression of cancer cells (13).…”
Section: Introductionmentioning
confidence: 99%