Active Targeted Nanoformulations via Folate Receptors: State of the Art and Future Perspectives

Cristina Martín-Sabroso1,2, Ana Isabel Torres-Suárez1,2, Mario Alonso-González1

  • 1Department of Pharmaceutics and Food Technology, School of Pharmacy, Complutense University, 28040 Madrid, Spain.

Pharmaceutics
|January 21, 2022
PubMed

Insights

Folate receptors (FRs) are overexpressed in cancer and inflammatory diseases, making them a promising therapeutic target. Targeting FRs with ligands or nanocarriers offers improved drug delivery and reduced toxicity for these conditions.

Area of Science:

  • Biomedical Science
  • Drug Delivery
  • Nanotechnology

Background:

  • Folate receptors (FRs) exhibit low expression in normal tissues but are overexpressed in cancer cells and activated macrophages.
  • This overexpression presents a therapeutic opportunity for targeted drug delivery in pathological conditions.

Purpose of the Study:

  • To analyze the use of folate receptors (FRs) as a target for novel therapeutic strategies.
  • To explore nanoformulations for targeted drug delivery and imaging in cancer and inflammatory diseases.

Main Methods:

  • Review of strategies for folate receptor targeting, including high-affinity ligands (folic acid, monoclonal antibodies) and ligand-decorated nanocarriers.
  • Analysis of nanoformulations for therapeutic and imaging applications targeting FRs.

Main Results:

  • Folate receptor targeting enables selective drug delivery to cancer cells and activated macrophages.
  • Nanoformulations enhance therapeutic efficacy and reduce systemic toxicity of treatments.
  • Targeted approaches show potential for both therapeutic intervention and diagnostic imaging.

Conclusions:

  • Folate receptor targeting is a viable strategy for developing advanced therapeutics for cancer and inflammatory diseases.
  • Nanoformulations offer a promising platform for FR-targeted drug delivery and imaging, improving treatment outcomes.

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.9K
Microorganisms in Medicine and Therapeutics01:29

Microorganisms in Medicine and Therapeutics

Microorganisms play a fundamental role in vaccine development, gene therapy, and therapeutic production. Their biological properties are harnessed to advance medicine and public health. Beyond immunization, microorganisms contribute to gut health, antibiotic synthesis, and genetic disease treatment.Live Attenuated and Inactivated VaccinesLive attenuated vaccines, such as the measles, mumps, and rubella (MMR) vaccine, utilize weakened forms of pathogens to closely resemble natural infections.
450
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
7.8K
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
1.8K
Signal Transduction: Overview01:26

Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...
9.7K
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.2K