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Pharmaceutics
Special Issues
Optimizing Pharmacokinetics Through Formulation Science and Technology
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Optimizing Pharmacokinetics Through Formulation Science and Technology

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmacokinetics and Pharmacodynamics".

Deadline for manuscript submissions: closed (20 April 2026) | Viewed by 8883

Special Issue Editor

Prof. Dr. David R. Taft

E-Mail Website
Guest Editor
Samuel J. and Joan B. Williamson Institute for Pharmacometrics, Division of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201, USA
Interests: pharmacokinetics; pharmacodynamics; PBPK modeling; drug–drug interactions; special populations
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

To ensure safe and effective drug therapy, it is crucial to administer the correct medication dosage within an appropriate timeframe, achieving and maintaining target plasma concentrations. Pharmacokinetics plays a key role in determining drug action in vivo, as it affects the systemic exposure following drug administration. Unsatisfactory pharmacokinetic properties can compromise both the safety and efficacy of a drug. For example, medications with a short elimination half-life may require multiple daily doses, which can impact patient adherence. Additionally, significant fluctuations in plasma levels during a dosing interval can result in adverse effects from high peak concentrations or diminished efficacy due to low trough levels. In such scenarios, formulation scientists can develop innovative delivery systems to improve the plasma profile of a medication, thereby optimizing therapeutic outcomes.

This issue is dedicated to research that demonstrates how formulation science can enhance pharmacokinetic profiles by modifying drug absorption, distribution, metabolism, or excretion. We invite pharmaceutical scientists to share their studies showcasing how formulation development has optimized the pharmacokinetic properties of drug products, leading to improved bioavailability, reduced food interactions, minimized drug–drug interactions, more patient-friendly dosing regimens, and enhanced safety profiles.

We welcome original research articles and reviews for this Special Issue. Potential research areas include, but are not limited to, the development and in vivo characterization of modified release formulations, innovative delivery systems for extravascular administration (such as nasal and pulmonary routes), and the use of model-informed formulation development approaches, including physiologically based biopharmaceutics modeling (PBBM).

We look forward to your valuable contributions.

Prof. Dr. David R. Taft
Guest Editor

Manuscript Submission Information

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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. Pharmaceutics 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.

Keywords

  • formulation development
  • formulation science
  • pharmacokinetics
  • biopharmaceutics
  • in vitro/in vivo extrapolation/correlation
  • bioavailability
  • modified release

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Published Papers (4 papers)

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Research

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20 pages, 806 KB  
Article
Dermal Concentration Versus Systemic Bioavailability of Topical Lidocaine and Tetracaine: An Exploratory Pharmacokinetic Pilot Study in Göttingen Minipigs
by Paweł Biernat, Dawid Bursy, Dominik Marciniak, Konrad Krajewski, Jan Meler and Radosław Balwierz
Pharmaceutics 2026, 18(1), 40; https://doi.org/10.3390/pharmaceutics18010040 - 28 Dec 2025
Cited by 2 | Viewed by 1244
Abstract
Background: Lidocaine, classified as an amide-type agent, and tetracaine, designated as an ester-type agent, are frequently co-formulated for dermatologic procedures. Despite the extensive literature on the pharmacokinetics (PK) of these substances, there is a paucity of head-to-head comparisons of intravenous (IV) and topical [...] Read more.
Background: Lidocaine, classified as an amide-type agent, and tetracaine, designated as an ester-type agent, are frequently co-formulated for dermatologic procedures. Despite the extensive literature on the pharmacokinetics (PK) of these substances, there is a paucity of head-to-head comparisons of intravenous (IV) and topical administration in the same preclinical model. Absolute bioavailability (F%) is imperative for optimizing formulation design and safety. Methods: A single-dose, single-sequence, three-period pilot study was performed in male Göttingen mini-pigs. The first period of the study involved the intravenous bolus administration of lidocaine HCl and tetracaine HCl, with a dosage of 1 mg/kg for each agent. In Period 2, the topical application of Pliaglis (a combination of 7% lidocaine and 7% tetracaine, with a concentration of 10 g/100 cm2 and a duration of 60 min) was utilized. In Period 3, the pharmacokinetic profile of Z4T4L4 (a formulation comprising 4% lidocaine HCl and 4% tetracaine HCl) was assessed under the same experimental conditions. Blood samples were collected up to 24 h after the administration of the drug; skin biopsies were obtained 90 min after the application of the test substance. Plasma and skin concentrations were measured by means of validated liquid chromatography–tandem mass spectrometry (LC–MS/MS). PK parameters were derived using a noncompartmental analysis approach, while F% was calculated through AUC comparison with IV dosing. Results: Subsequent to intravenous administration, the mean elimination half-lives of lidocaine and tetracaine were determined to be 1.62 h and 1.85 h, respectively. Pliaglis demonstrated higher skin concentrations of lidocaine (358 μg/g) and tetracaine (465 μg/g) compared to Z4T4L4 (33.6 μg/g and 46.1 μg/g, respectively). Despite lower skin levels, Z4T4L4 produced higher F% (lidocaine: 1.98% vs. 1.41%; tetracaine: 3.34% vs. 1.26%). The time to maximum plasma concentration (Tmax) for lidocaine was found to be 2–4 h (Pliaglis) and 2–8 h (Z4T4L4), while for tetracaine, it was 1–8 h (Pliaglis) and 2–8 h (Z4T4L4). Conclusions: In this preliminary study, which included three subjects, Z4T4L4 exhibited a numerical tendency towards increased systemic bioavailability in comparison with Pliaglis. This observation was noted despite the fact that Z4T4L4 resulted in markedly lower skin concentrations. Due to the exploratory nature of the pilot study (n = 3), observed differences are reported as numerical trends. The data suggest that Z4T4L4 may enhance systemic absorption while reducing skin retention, highlighting a potential formulation-dependent dissociation between local concentration and systemic bioavailability. These preliminary findings provide in vivo evidence of a divergence between eutectic-based tissue retention and enhancer-driven systemic flux. This highlights that formulation design fundamentally dictates the safety profile of local anesthetics, necessitating a balance between local efficacy and systemic safety. Full article
(This article belongs to the Special Issue Optimizing Pharmacokinetics Through Formulation Science and Technology)
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13 pages, 4641 KB  
Article
Formulation and Characterization of Bone-Targeting Vancomycin-Loaded Liposomes
by Basel Karzoun, Wala’a Albenayan, Shilpa Raut and Eman Atef
Pharmaceutics 2025, 17(6), 792; https://doi.org/10.3390/pharmaceutics17060792 - 18 Jun 2025
Cited by 6 | Viewed by 1640
Abstract
Background: We report the successful formulation of a bone-targeted vancomycin-loaded liposomal carrier. Method: The basic liposomal structure is composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, and dicetyl phosphate (DCP) in a molar ratio of 3:1:0.25, respectively. The dehydration–rehydration method was used to maximize the liposomal-encapsulation [...] Read more.
Background: We report the successful formulation of a bone-targeted vancomycin-loaded liposomal carrier. Method: The basic liposomal structure is composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, and dicetyl phosphate (DCP) in a molar ratio of 3:1:0.25, respectively. The dehydration–rehydration method was used to maximize the liposomal-encapsulation efficiency of vancomycin after the initial preparation using thin-film hydration. Results: Sodium alendronate was used as a targeting moiety and was successfully conjugated to DSPE–PEG–COOH via carbodiimide chemistry, as was confirmed using IR spectroscopy. The resulting conjugate, DSPE–PEG-alendronate, was subsequently used in the formulation of bone-targeting vancomycin-loaded liposomes. In vitro binding assays with hydroxyapatite demonstrated preferential binding of the surface-modified liposomes to hydroxyapatite crystals. Furthermore, ex vivo studies revealed that the surface-modified liposomes exhibited enhanced binding affinity to the tibial bone tissue of 4-week-old male CD1 mice, in comparison to unmodified liposomes. Conclusions: The successfully formulated surface-modified vancomycin loaded liposomes showed enhanced bone affinity with a great potential for targeting the antibiotic to infected bones. Full article
(This article belongs to the Special Issue Optimizing Pharmacokinetics Through Formulation Science and Technology)
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Review

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37 pages, 11900 KB  
Review
Controlled Release Technologies for Diltiazem Hydrochloride: A Comprehensive Review of Solid Dosage Innovations
by Estefanía Troches-Mafla, Constain H. Salamanca and Yhors Ciro
Pharmaceutics 2025, 17(11), 1491; https://doi.org/10.3390/pharmaceutics17111491 - 19 Nov 2025
Viewed by 1708
Abstract
Introduction: Diltiazem hydrochloride (DH) is a calcium channel blocker used in the treatment of hypertension, angina pectoris, and arrhythmias. Its short half-life and frequent dosing requirements limit patient adherence and cause plasma concentration fluctuations. Objective: This review critically examines recent pharmaceutical [...] Read more.
Introduction: Diltiazem hydrochloride (DH) is a calcium channel blocker used in the treatment of hypertension, angina pectoris, and arrhythmias. Its short half-life and frequent dosing requirements limit patient adherence and cause plasma concentration fluctuations. Objective: This review critically examines recent pharmaceutical technologies and formulation strategies for modified-release dosage forms (MRDFs) of diltiazem hydrochloride, emphasizing their impact on pharmacokinetics, clinical performance, and regulatory aspects. Methodology: A structured literature review (2010–2025) was conducted using databases such as PubMed, ScienceDirect, MDPI, and ACS Publications. Studies were selected based on relevance to solid oral MRDFs of DH and their associated manufacturing techniques. Results: Techniques including direct compression, granulation, extrusion–spheronization, spray drying, solvent evaporation, and ionotropic gelation have enabled the development of hydrophilic matrices, coated pellets, microspheres, and osmotic systems. Functional polymers such as HPMC, Eudragit®, and ethylcellulose play a central role in modulating release kinetics and improving bioavailability. Conclusions: This review not only synthesizes current formulation strategies but also explores reverse engineering of ideal release profiles and the integration of advanced modeling tools such as physiologically based pharmacokinetic (PBPK) modeling and in vitro–in vivo correlation (IVIVC). These approaches support the rational design of personalized, regulatory-compliant DH therapies. Full article
(This article belongs to the Special Issue Optimizing Pharmacokinetics Through Formulation Science and Technology)
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26 pages, 3302 KB  
Review
Improving In Vitro–In Vivo Correlation (IVIVC) for Lipid-Based Formulations: Overcoming Challenges and Exploring Opportunities
by Arnaud Bourderi-Cambon, Khaled Fadhlaoui, Ghislain Garrait, Emmanuelle Lainé, Imen Dhifallah, Manon Rossano, Philippe Caisse and Eric Beyssac
Pharmaceutics 2025, 17(10), 1310; https://doi.org/10.3390/pharmaceutics17101310 - 9 Oct 2025
Cited by 6 | Viewed by 3526
Abstract
Lipid-based formulations (LBFs) play a crucial role in enhancing the oral bioavailability of poorly water-soluble drugs by leveraging lipid digestion and solubilization processes. However, developing robust in vitro–in vivo correlations (IVIVCs) for LBFs presents unique challenges due to the complex interplay of digestion, [...] Read more.
Lipid-based formulations (LBFs) play a crucial role in enhancing the oral bioavailability of poorly water-soluble drugs by leveraging lipid digestion and solubilization processes. However, developing robust in vitro–in vivo correlations (IVIVCs) for LBFs presents unique challenges due to the complex interplay of digestion, permeation, and dynamic solubilization. This article reviews the construction of IVIVC in the context of LBFs, highlighting the limitations of traditional methods and the need for tailored approaches. It examines the in vitro tools commonly employed for LBF characterization, such as USP dissolution tests, lipolysis assays, and combined models, and discusses their relevance to in vivo performance prediction. The review also explores the sources of in vivo data essential for validating IVIVC and describes the most popular in silico tools for predicting in vivo performance, focusing on lipid-based formulations. This work aims to pave the way for more effective and adaptable IVIVC methodologies for lipid-based drug delivery systems. Full article
(This article belongs to the Special Issue Optimizing Pharmacokinetics Through Formulation Science and Technology)
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