Special Issue "Pharmacokinetic Processes of Active Substance in Drug Formulations"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 1213

Special Issue Editor

1. Department of Chemical and Environmental Process Engineering, Budapest University of Technology and Economics, Műegyetem Quay 3, H-1111 Budapest, Hungary
2. Institute of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös street 6., H-6720 Szeged, Hungary
Interests: in vitro dissolution/permeability; tissue specific permeability; biomimetic models for drug metabolism; ophthalmic drug formulation; plasma prorein binding; physicochemical profiling; lead optimization; in silico candidate selection

Special Issue Information

Dear Colleagues,

Pharmacokinetic-driven drug formulation is gaining more and more importance in novel drug research and development programs. One of the reasons for this is to be found in the physico-chemical properties of the active ingredient candidates, where mainly poor solubility and/or absorption is a challenge. Another possible reason can be related to various protein and enzyme related PK problems, such as increased plasma protein binding, metabolism and active transport mechanisms. In the face of these problems, there are already many formulation solutions with a new approach available, the knowledge and repertoire of which we would like to enrich with the present special issue. In the Special Issue of Pharmaceuticals ‘Pharmacokinetic Processes of Active Substance in Drug Formulations’, in addition to the new drug formulation and drug delivery systems, we are also expecting the presentation of novel in vitro, in vivo and ex vivo test methods or mechanistic approaches that can be linked to ADME processes, which present dissolution, drug release kinetics, in vitro/ex works related to vivo permeability studies specifically for formulation strategy or test systems for alternative drug delivery routes for drug targeting, smart drug delivery. 

Dr. György Tibor Balogh
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • dissolution studies
  • drug release kinetics
  • in vitro/ex vivo permeability studies
  • diffusion studies
  • exploiting alternative drug delivery routes for drug targeting
  • improved bioavailability of poorly water soluble/permeable drugs
  • smart drug delivery systems
  • complexes facilitation drug release
  • metabolism-coupled drug release

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:


A Study on Pharmacokinetic Functionalities and Safety Margins of an Optimized Simvastatin Nanoformulation
Pharmaceuticals 2023, 16(3), 380; https://doi.org/10.3390/ph16030380 - 01 Mar 2023
Viewed by 898
A pharmaceutical formulation with favorable pharmacokinetic parameters is more likely to be efficacious and safe to overcome the failures of the drug resulting from lack of efficacy, poor bioavailability, and toxicity. In this view, we aimed to evaluate the pharmacokinetic functionalities and safety [...] Read more.
A pharmaceutical formulation with favorable pharmacokinetic parameters is more likely to be efficacious and safe to overcome the failures of the drug resulting from lack of efficacy, poor bioavailability, and toxicity. In this view, we aimed to evaluate the pharmacokinetic functionalities and safety margin of an optimized CS-SS nanoformulation (F40) by in vitro/in vivo methods. The everted sac technique was used to evaluate the improved absorption of a simvastatin formulation. In vitro protein binding in bovine serum and mice plasma was performed. The formulation’s liver and intestinal CYP3A4 activity and metabolic pathways were investigated by the qRT-PCR technique. The excretion of cholesterol and bile acids was measured to demonstrate the formulation’s cholesterol depletion effect. Safety margins were determined by histopathology as well as fiber typing studies. In vitro protein binding results revealed the existence of a high percentage of free drugs (22.31 ± 3.1%, 18.20 ± 1.9%, and 16.9 ± 2.2%, respectively) compared to the standard formulation. The controlled metabolism in the liver was demonstrated from CYP3A4 activity. The formulation showed enhanced PK parameters in rabbits such as a lower Cmax, clearance, and a higher Tmax, AUC, Vd, and t1/2. qRT-PCR screening further proved the different metabolic pathways followed by simvastatin (SREBP-2) and chitosan (PPAR-γ pathway) in the formulation. The results from qRT-PCR and histopathology confirmed the toxicity level. Hence, this pharmacokinetic profile of the nanoformulation proved it has a unique synergistic hypolipidemic modality. Full article
(This article belongs to the Special Issue Pharmacokinetic Processes of Active Substance in Drug Formulations)
Show Figures

Figure 1

Back to TopTop