Targeted drug delivery (TDD) modality promises a smart localization of appropriate dose of therapeutic drugs to the targeted part of the body at reduced system toxicity. To achieve the desired goals of TDD, accurate analysis of the system is important. Recent advances in molecular communication (MC) present prospects to analyzing the TDD process using engineering concepts and tools. Specifically, the MC platform supports the abstraction of TDD process as a communication engineering problem in which the injection and transportation of drug particles in the human body and the delivery to a specific tissue or organ can be analyzed using communication engineering tools. In this paper we stand on the MC platform to present the information-theoretic model and analysis of the TDD systems. We present a modular structure of the TDD system and the probabilistic models of the MC-abstracted modules in an intuitive manner. Simulated results of information-theoretic measures such as the mutual information are employed to analyze the performance of the TDD system. Results indicate that uncertainties in drug injection/release systems, nanoparticles propagation channel and nanoreceiver systems influence the mutual information of the system, which is relative to the system’s bioequivalence measure.