Related Experiment Video
Updated: May 23, 2025
10:10
Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
10.2K
Redesigning Ibuprofen for Improved Oral Delivery and Reduced Side Effects
Szilvia H Toth1,2, Anca D Stoica1, Cristian Sevcencu3,2
1Department of Molecular Biology and Biotechnology, Faculty of Biology and Geology, Babeş-Bolyai University, Cluj-Napoca, 400006, Romania.
Bioconjugate Chemistry
|April 28, 2025
Summary
Ibuprofen (IBP), a common pain reliever, can cause toxicity. Researchers are developing new IBP conjugates to reduce side effects while maintaining pain relief efficacy.
Area of Science:
- Pharmacology
- Drug Development
Background:
- Ibuprofen (IBP) is a widely used nonsteroidal anti-inflammatory drug (NSAID) effective for pain and fever.
- IBP inhibits cyclooxygenases, reducing prostaglandin synthesis involved in inflammation and pain.
- Despite its benefits, IBP exhibits dose-dependent toxicity, primarily affecting the gastrointestinal system and causing cellular damage.
Purpose of the Study:
- To review recent advancements in Ibuprofen conjugation techniques.
- To highlight novel IBP formulations designed for reduced toxicity.
- To assess the efficacy and safety profile of these new IBP conjugates.
Main Methods:
- Literature review of recent studies on IBP conjugation.
- Analysis of data on the efficacy and toxicity of novel IBP conjugates.
- Comparison of the parent drug's profile with that of the conjugates.
Main Results:
- Several conjugation strategies have yielded IBP formulations with improved safety profiles.
- These novel conjugates demonstrate comparable or enhanced efficacy to conventional IBP.
- Reduced gastrointestinal toxicity and cellular damage have been observed in conjugate studies.
Conclusions:
- Ibuprofen conjugation represents a promising approach to mitigate NSAID-induced toxicity.
- Novel IBP conjugates offer a potential for safer and equally effective pain and inflammation management.
- Further research and clinical trials are warranted to fully establish the therapeutic potential of these advanced drug formulations.
Related Concept Videos
01:18Drug Delivery: Enteral Route
361
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.
361
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
660
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
660
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
164
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
164
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
112
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
112
01:24Factors Influencing Drug Absorption: Presystemic Elimination
173
The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
173
01:18Routes of Drug Administration: Enteral
3.1K
Medications can be administered through the enteral route using liquids, capsules, or tablets.
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
3.1K