ORIENTAL JOURNAL OF CHEMISTRY www.orientjchem.org An International Open Access, Peer Reviewed Research Journal ISSN: 0970-020 X CODEN: OJCHEG 2020, Vol. 36, No.(6): Pg. 985-1000 This is an Open Access article licensed under a Creative Commons license: Attribution 4.0 International (CC- BY). Published by Oriental Scientific Publishing Company © 2018 Highly Efficient Prodrugs: Design and Therapeutic Applications (A-Review) ASHUTOSH PAL 1 * and BIMAL KRISHNA BANIK 2 * 1 Raja Peary Mohan College, West Bengal, India. 2 Department of Mathematics and Natural Sciences, College of Sciences and Human Studies, Deanship of Research, Prince Mohammad Bin Fahd University, Al Khobar, Kingdom of Saudi Arabia. *Corresonding author E-mail: ashupal33@gmail.com, bbanik@pmu.edu.sa http://dx.doi.org/10.13005/ojc/360601 (Received: November 30, 2020; Accepted: December 20, 2020) ABSTRACT Prodrug is a very powerful way for the improvement of biopharmaceutical, physicochemical, or pharmacokinetic possessions of pharmacologically dynamic mediators. Prodrug is a pharmacologically not an active compound, which can be converted into an active drug by biotransformation which is metabolic and such process the efficiency of drugs gets improved with specific target delivery. The conversion of a prodrug to drug may happen before concentration, after concentration, or at a precise part of the physique. This approach has many advantages over drug administration which is in our convention. In this review, different types of carriers, which can be used for prodrug synthesis are summarized. Examples of both marketed and investigational prodrugs from several promoieties are discussed not only for their advantages and uses but also their prospects. The purpose of this review is to introduce in detail the foundation behind the use of the prodrug methodology from past to present and at the same time to consider the possible consequences, which may evolve from insufficient initiation of prodrugs. Furthermore the concept of prodrug and the classifications of prodrugs will be discussed in this article and it is expected that this review will be helpful for medicinal chemists for their research in the upcoming days. Keywords: Prodrug, Biopharmaceutical, Physicochemical, Pharmacokinetic, Metabolic biotransformation, Drug administration. INTRODUCTION Most of the drugs have undesirable physico-chemical properties that include good water solubility, unstable chemical nature, inadequate oral absorption, rapid metabolism, short half-life and moderate toxicity. It is noticeable that many potential drug compounds have been discontinued due to weak pharmacokinetic belongings and or otherwise unexpected poisonousness. Their healing power is enhanced by not only minimizing the unacceptable harmful properties but also by maintaining the good ones. An improvement is performed by biological, physical or chemical methods. The physical approach is dependable on a modification of the dosage. Chemical approach holds the most effective approach in enhancing drug selectivity. The aim of this approach is to design or develop new drugs or to do structural alterations creating prodrugs.