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Related Concept Videos

Drug Delivery: Overview01:16

Drug Delivery: Overview

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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
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Drug Delivery: Miscellaneous Routes01:22

Drug Delivery: Miscellaneous Routes

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Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
676
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
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Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

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The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
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Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

1.4K
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Transcriptional Regulation: Riboswitches01:23

Transcriptional Regulation: Riboswitches

468
Riboswitches are RNA elements that regulate gene expression by altering their secondary structures in response to specific effector molecules. These elements, located in the leader regions of certain mRNAs, act as transcriptional regulators by toggling between alternative conformations to control downstream gene expression. Riboswitch-mediated regulation is a precise mechanism for modulating biosynthetic pathways, as exemplified by the riboflavin biosynthesis pathway in Bacillus...
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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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Riboflavin-Targeted Drug Delivery.

Milita Darguzyte1, Natascha Drude1, Twan Lammers1

  • 1Institute for Experimental Molecular Imaging, University Hospital Aachen, Forckenbeckstrasse 55, 52074 Aachen, Germany.

Cancers
|February 5, 2020
PubMed
Summary

Vitamin B2 (riboflavin) targeting shows promise for cancer therapy, shifting focus from folate. Riboflavin transporters (RFVT 1-3) are overexpressed in tumors, enabling targeted drug delivery for improved efficacy.

Keywords:
active targetingmolecular imagingnanomedicinesnanoparticleriboflavintargeted drug deliverytheranosticsvitamin B2

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Area of Science:

  • Oncology
  • Biochemistry
  • Nanomedicine

Background:

  • Active targeting enhances drug delivery system retention in tumors.
  • Vitamin receptors overexpressed in cancers are promising targets for drug delivery.
  • Research focus is shifting from vitamin B9 (folate) to vitamin B2 (riboflavin) for cancer targeting.

Purpose of the Study:

  • To review current knowledge on riboflavin transporter (RFVT) expression in healthy and pathological tissues.
  • To discuss riboflavin internalization pathways.
  • To provide an overview of riboflavin-targeted diagnostics and therapeutics.

Main Methods:

  • Review of scientific literature on riboflavin transporters and their role in cancer.
  • Analysis of riboflavin internalization mechanisms.
  • Summary of preclinical and clinical studies on riboflavin-targeted drug delivery systems.

Main Results:

  • Riboflavin carrier protein and riboflavin transporters (RFVT 1-3) are overexpressed in various tumor types, stem cells, and neovasculature.
  • Tumor cells exhibit increased riboflavin metabolism compared to normal cells.
  • Riboflavin conjugates with nanoparticles, polymers, dendrimers, and liposomes show high tumor affinity in preclinical studies.

Conclusions:

  • Riboflavin transporters represent a promising target for active tumor targeting.
  • Riboflavin-based drug delivery systems offer potential for enhanced cancer diagnostics and therapeutics.
  • Further research into riboflavin internalization and targeted delivery is warranted.