Prodrug Synthesis and Drug Targeting

Prodrugs are drug molecules that are pharmacologically inactive but need to be transformed chemically or enzymatically to release the active drug in vivo and produce a pharmacological effect. Prodrugs outperform their parent drug molecule in terms of delivery. The concept of a prodrug is justified because it allows the active drug to overcome a barrier that would otherwise prevent it from reaching the site of action and exerting the necessary pharmacological activity. The following are some of the difficulties that the prodrug strategy helps to overcome: Low bioavailability due to poor aqueous solubility (corticosteroids); poor permeability or absorption (ampicillin); high first-pass metabolism (propranolol); metabolic instability leading to short half-life (dopamine); poor site specificity (anticancer agents); incomplete absorption (epinephrine); unfavourable organoleptic properties (chloramphenicol); difficulties during formulation; adverse effects and toxicity The prodrug strategy is quickly becoming a critical component of drug delivery strategy. The application of a prodrug strategy in the last 20 years has resulted in consistent progress in the biopharmaceutical, physicochemical, and/or pharmacokinetic properties of pharmacologically active molecules. The number of prodrugs now on the market can be used to assess the success of the prodrug method. Currently, prodrugs account for about 10% of all marketed medications.

Drug-targeting has the potential to improve drug delivery efficacy, reduce adverse effects, and lower treatment costs significantly. The vast majority of drug-targeting studies, on the other hand, presume that the drug-particles are already at or near the target site.

• Synthesis and Characterization
• Prodrug Design
• Pharmacokinetic Evaluation
• Carriers for Prodrug Synthesis