In particular, we exemplified the application of PK-PD modeling in the development of extended-release formulations, liposomal drugs, modified proteins, and antibody-drug conjugates. The linkage between PK and PD was highlighted. In this review, we summarized the basic PK-PD modeling theory in drug delivery and demonstrated how it had been applied to help the development of new delivery systems and modified large molecules. As the pharmacokinetic and pharmacodynamic (PK-PD) modeling allows for the separation of the drug-, carrier- and pharmacological system-specific parameters, it has been widely used to improve understanding of the in vivo behavior of these complex delivery systems and help their development. ![]() As a result, the drug absorption and disposition processes after administration of these drug delivery systems and engineered molecules become exceedingly complex. With the advancement of technology, drug delivery systems and molecules with more complex architecture are developed.
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