Targeting of herbal bioactives through folate receptors: a novel concept to enhance intracellular drug delivery in cancer therapy
Abstract
Targeted drug delivery through folate receptor (FR) has emerged as a most biocompatible, target oriented, and non-immunogenic cargoes for the delivery of anticancer drugs. FRs are highly overexpressed in many tumor cells (like ovarian, lung, breast, kidney, brain, endometrial, and colon cancer), and targeting them through conjugates bearing specific ligand with encapsulated nanodrug moiety is undoubtedly, a promising approach toward tumor targeting. Folate, being an endogenous ligand, can be exploited well to affect various cellular events occurring during the progress of tumor, in a more natural and definite way. Thus, the aim of the review lies in summarizing the advancements taken place in the drug delivery system of different therapeutics through FRs and to refine its role as an endogenous ligand, in targeting of synthetic as well as natural bioactives. The review also provides an update on the patents received on the folate-based drug delivery system.
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Folic acid can highly specifically bind to FR, promoting internalization of folate-targeted NPs into cytoplasm through receptor-mediated endocytosis.
“Folic acid can highly specifically bind to FR, which promote the internalization of folate-targeted NPs into the cytoplasm through receptor-mediated endocytosis.”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [266]
Compared with antibodies, folic acid has higher tumor permeability, higher self-stability, relatively low toxicity, and is highly economical.
“Besides, in ligand-modified active targeted drug delivery systems, compared with antibodies, folic acid has the following characteristics: 1) higher tumor permeability; 2) higher self-stability, including in acidic, alkaline and solvent ; 3) Relatively low toxicity; 4) Highly economical.266”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [266]
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References 84 · Cited by 27
- Authors
- Gupta, A., Kaur, C. D., Saraf, S., & Saraf, S.
- Affiliations
- Pandit Ravishankar Shukla University (IN)
- Corresponding author
- Saraf, Swarnlata
- Venue
- Journal of Receptors and Signal Transduction
- Publisher
- Informa UK Limited
- Published
- 2017-01-17
- Volume
- 37
- Issue
- 3
- Pages
- 314-323
- ISSN
- 1079-9893 (ISSN-L)
- 1532-4281
- OpenAlex
- W2577026405
- Cited by
- 27
- References
- 84
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 1 · 2023: 1 · 2022: 3 · 2021: 2 · 2020: 4 · 2019: 3 · 2018: 5 · 2017: 2
- FWCI
- 0.28
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Receptors and Signal Transduction (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Health Sciences › Medicine › Rheumatology › Folate and B Vitamins Research
- Keywords
- folate receptor, folate receptor targeting, targeted drug delivery, intracellular drug delivery, anticancer agents
- MeSH terms
- Antineoplastic Agents, Folic Acid, Humans, Ligands, Neoplasms, Plants, Medicinal, Receptors, Cell Surface, Drug Delivery Systems, Folate Receptor 1, Molecular Targeted Therapy
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