Effectiveness of drug targeting

The particular models used in drug targeting research are dealt with in Section 13.3, and quantitative measures of the effectiveness of drug targeting are described in Section 13.4, followed by a discussion relating to their application in Section 13.5. 

The effectiveness of drug targeting should be evaluated by taking into account not only pharmacokinetic aspects, but also the pharmacodynamic aspects. The latter include the concentration-effect relationship in the target tissue and at the sites where toxicity may occur [7,12]. The therapeutic effect of the drug and its toxic effect may be different with regard to their mechanisms, and hence their concentration-effect relationship may also be different, both qualitatively (different PD models) and quantitatively (different model parameters). 

PK models (Section 13.2.4), PD models (Section 13.2.5), and PK/PD models (Section 13.2.6) can be used in two different ways, that is, in simulations (Section 13.2.7) and in data analysis (Section 13.2.8). Simulations can be performed if the model structure and its underlying parameter values are known. In fact, for any arbitrary dose or dosing schedule the drug concentration profile in each part of the model can be calculated. The quantitative measures of the effectiveness of drug targeting (Section 13.4) can also be evaluated. If actual measurements have been performed in in-vivo experiments in laboratory animals or man, the relevant model structure and its parameter values can be assessed by analysis of plasma disappearance curves, excretion rate profiles, tissue concentration data, and so forth (Section 13.2.8). 

If an appropriate model is selected and the model parameters are known, the time course of the drug concentration in each compartment (PK models) and the drug effect (PK/PD models) can be calculated for any dosing regimen. In addition, the relevant measures of the effectiveness of drug targeting can be calculated (see Section 13.4). 

For practical purposes, measures of the effectiveness of drug targeting are required. Such measures have been derived based on the pharmacokinetic profiles of the drug targeting system and that of the active drug. 

Evaluation of Effectiveness of Drug Targeting Using PK and PK/PD Modelling... 

It is preferable to test the effects of drug-targeting preparations on the whole body as early as possible... 

Coverage of the importance of considering wildlife as targets when assessing potential adverse effects of drugs or chemicals on the immune system... 

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