Recent Advances in Prodrug Approach over Conventional Drug Therapy

Background: Prodrugs represent a strategically designed category of medicinal compounds aimed at optimizing drug pharmacokinetics. By modifying the pharmacological action of the drug within a prodrug, subsequent enzymatic bioconversion in the human body facilitates the release of the active drug. This strategy has been highly effective, as demonstrated by the substantial number of prodrugs found in commercial pharmaceutical products. Prodrugs have emerged as a recognized strategy for augmenting the physical, chemical, biological, or pharmacokinetic attributes of pharmacologically active molecules in the realm of drug research and development. Objective: This systematic review intended to offer insights into the recent developments in the prodrug approach used in drug research and development, with a focus on highlighting its effectiveness. The objective was to illustrate the diverse applications of prodrugs and their impact on enhancing drug properties and therapeutic outcomes. Area covered: This review is centered on the most recent developments in the prodrug approach used for drug development and research. The prodrug concept has a wide range of practical uses, some of which are illustrated in this review article. These illustrations are categorized based on the intention behind their creation. Results: Prodrugs have been designed to address challenges, such as poor water solubility and low bioavailability. Strategies, like using neutral or charged promoieties, have been reported to be successful in enhancing solubility. For permeability and bioavailability, prodrugs have been employed to mask polar groups, enabling better absorption. Prolonged half-life prodrugs have been developed to extend drug action, while tissue-targeted delivery prodrugs have shown promise in enhancing drug delivery to specific sites. Conclusion: Prodrug design offers promising strategies to optimize drug delivery and efficacy. Despite challenges, ongoing clinical trials and research efforts indicate the potential of prodrugs in improving therapeutic outcomes. Addressing formulation challenges and understanding pharmacokinetic variability are essential for successful prodrug development.