Journal of Pharmaceutical Chemistry and Drug formulation ISSN: 3108-0782 (Online)

Authors: Dr. Radhika Joshi, Dr. Vikram Patel

Abstract: Prodrugs are chemically modified derivatives of active pharmaceutical ingredients (APIs) designed to overcome limitations related to solubility, permeability, stability, and targeted delivery. By strategically incorporating functional moieties, prodrugs enhance pharmacokinetic profiles, improve oral bioavailability, and reduce toxicity. This paper reviews the principles of prodrug design, classification, strategies for enhancing absorption and distribution, and enzymatic or chemical activation mechanisms. Emphasis is placed on structure-activity relationship (SAR) approaches, linker chemistry, and computational tools for rational design. Case studies on clinically approved prodrugs demonstrate the impact on bioavailability and therapeutic outcomes. Formulation challenges, regulatory considerations, and future perspectives in prodrug research are discussed, highlighting their pivotal role in modern drug development.

Keywords: Prodrug, Pharmacokinetics, Bioavailability, Enzymatic activation, Solubility enhancement, Targeted delivery, Rational design, Drug formulation.