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Maximising Drug Delivery for Improved Pharmacokinetics and Pharmacodynamics

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

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 3785

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Special Issue Editors

Prof. Dr. Sias Hamman

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Guest Editor

Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, North-West, South Africa
Interests: drug delivery; drug absorption enhancement; herb–drug interactions; nose-to-brain delivery; ex vivo pharmacokinetic models
Special Issues, Collections and Topics in MDPI journals

Dr. Dewald Steyn

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Guest Editor

Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, North-West, South Africa
Interests: drug delivery; drug absorption enhancement; in vitro pharmacokinetics; herb-drug interactions; nose-to-brain delivery
Special Issues, Collections and Topics in MDPI journals

Dr. Marius Brits

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Guest Editor

Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, North-West, South Africa
Interests: solid-state properties of pharmaceuticals; quality control of medicines; analytical method development

Special Issue Information

Dear Colleagues,

The pharmaceutical industry is challenged by the poor bioavailability of a large portion of approved and pipeline drugs. Various reasons exist for the poor systemic delivery of these drugs, which include low aqueous solubility, inadequate membrane permeability, high pre-systemic metabolism, susceptibility to absorption barriers such as efflux transporters, and unfavourable physico-chemical properties. Innovative approaches have been employed by scientists to overcome drug delivery challenges in order to maximise bioavailability.This Special Issue of the journal Pharmaceuticals aims at publishing original research and review articles on topics related to the facilitation of drug delivery in order to maximise bioavailability. The following topics form part of the scope of this Special Issue:

Formulation and dosage form design (e.g., specialised drug delivery devices, permeation enhancers, nanotechnology, inclusion complexes, amorphous solid dispersions, functional excipients, solubilization with surfactants to increase solubility, etc.);
Alternative routes of drug administration (e.g., pulmonary, intranasal, transdermal, rectal, buccal, sublingual, etc.);
Targeted drug delivery (e.g., region specific delivery such as colon targeted delivery, nose-to-brain delivery, etc.);
Chemical strategies (e.g., structural modification, prodrugs, salts, conjugation with proteins, etc.);
Physical strategies (e.g., magnetic retention, expandable systems, microneedles, iontophoresis, etc.).

Prof. Dr. Sias Hamman
Dr. Dewald Steyn
Dr. Marius Brits
Guest Editors

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.

Keywords

drug delivery
bioavailability
absorption enhancement
formulation
alternative route of drug administration

Published Papers (3 papers)

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Research

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12 pages, 941 KiB

Open AccessArticle

Early Stage Preclinical Formulation Strategies to Alter the Pharmacokinetic Profile of Two Small Molecule Therapeutics

by Le An, Tom De Bruyn, Jodie Pang, Savita Ubhayakar, Laurent Salphati, Xing Zhang, Liling Liu, Ruina Li, Bryan Chan, Anwesha Dey and Elizabeth S. Levy

Pharmaceuticals 2024, 17(2), 179; https://doi.org/10.3390/ph17020179 - 30 Jan 2024

Viewed by 1012

Abstract

Early stage chemical development presents numerous challenges, and achieving a functional balance is a major hurdle, with many early compounds not meeting the clinical requirements for advancement benchmarks due to issues like poor oral bioavailability. There is a need to develop strategies for achieving the desired systemic concentration for these compounds. This will enable further evaluation of the biological response upon a compound–target interaction, providing deeper insight into the postulated biological pathways. Our study elucidates alternative drug delivery paradigms by comparing formulation strategies across oral (PO), intraperitoneal (IP), subcutaneous (SC), and intravenous (IV) routes. While each modality boasts its own set of merits and constraints, it is the drug’s formulation that crucially influences its pharmacokinetic (PK) trajectory and the maintenance of its therapeutic levels. Our examination of model compounds G7883 and G6893 highlighted their distinct physio-chemical attributes. By harnessing varied formulation methods, we sought to fine-tune their PK profiles. PK studies showcased G7883′s extended half-life using an SC oil formulation, resulting in a 4.5-fold and 2.5-fold enhancement compared with the IP and PO routes, respectively. In contrast, with G6893, we achieved a prolonged systemic coverage time above the desired target concentration through a different approach using an IV infusion pump. These outcomes underscore the need for tailored formulation strategies, which are dictated by the compound’s innate properties, to reach the optimal in vivo systemic concentrations. Prioritizing formulation and delivery optimization early on is pivotal for effective systemic uptake, thereby facilitating a deeper understanding of biological pathways and expediting the overall clinical drug development timeline. Full article

(This article belongs to the Special Issue Maximising Drug Delivery for Improved Pharmacokinetics and Pharmacodynamics)

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12 pages, 4996 KiB

Open AccessArticle

Tigecycline Absorption Improved by Selected Excipients

by Hubert Ziółkowski, Kalina Szteyn, Dawid Jędrzkiewicz, Bartosz Rasiński and Jerzy Jaroszewski

Pharmaceuticals 2023, 16(8), 1111; https://doi.org/10.3390/ph16081111 - 5 Aug 2023

Cited by 1 | Viewed by 848

Abstract

To investigate the effects of (2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD), (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), tocopherol polyethylene glycol 1000 succinate (TPGS), sodium desoxycholate (SDOCH), trimethyl chitosan (TMC), and sodium caprate (C10) on the plasma concentration and the oral bioavailability of tigecycline in broiler chickens. To test the effects of the excipients on absorption of tigecycline, a tetracycline that is poorly absorbed from the gastrointestinal tract, broiler chickens were used as an animal model. Tigecycline (10 mg/kg body weight) was administered intravenously, orally, and orally with one of the excipients. Plasma samples were taken after administration. To measure tigecycline concentrations, high-performance liquid chromatography coupled with tandem mass spectrometry was used. Compartmental and non-compartmental analyses were used for pharmacokinetic analyses of mean plasma concentrations versus time. With the exception of sodium caprate, all the excipients significantly increased the area under the curve and bioavailability of tigecycline (p < 0.05). These parameters were approximately doubled by HP-β-CD, TPGS, and SDOCH, with 95% confidence intervals (95% CIs) for the difference that included only increases of 1.5-fold or higher (bioavailability: control, 1.67%; HP-β-CD, 3.24%; TPGS, 3.30%; and SDOCH, 3.24%). The increases in these parameters were smaller with DM-β-CD and TMC (DM-β-CD, 2.41%; TMC, 2.55%), and the 95% CIs ranged from close to no difference to nearly double the values in the control group. These results indicate that HP-β-CD, TPGS, and SDOCH substantially increase the area under the curve and oral bioavailability of tigecycline. They suggest that DM-β-CD and TMC may also substantially increase these parameters, but more research is needed for more precise estimates of their effects. Full article

(This article belongs to the Special Issue Maximising Drug Delivery for Improved Pharmacokinetics and Pharmacodynamics)

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Other

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9 pages, 610 KiB

Open AccessCase Report

Compounded Effervescent Magnesium for Familial Hypomagnesemia: A Case Report

by Giada Bennati, Mario Cirino, Giulia Benericetti, Natalia Maximova, Monica Zanier, Federico Pigato, Anna Parzianello, Alessandra Maestro, Egidio Barbi and Davide Zanon

Pharmaceuticals 2023, 16(6), 785; https://doi.org/10.3390/ph16060785 - 24 May 2023

Cited by 1 | Viewed by 1458

Abstract

Familial hypomagnesemia with hypercalciuria and nephrocalcinosis (FHHNC) is a rare autosomal recessive disorder affecting <1/1,000,000 people. It is caused by mutations in the CLDN16 (FHHNC Type 1) or CLDN19 (FHHNC Type 2) genes, which are located on Chromosomes 3q27 and 1p34.2, respectively. There are no drug therapies for this condition. Although magnesium salts represent an important class of compounds and exhibit various therapeutic actions as a supplement for magnesium deficiency in FHHNC, various formulations on the market have different bioavailability. We report the case of a patient with FHNNC first treated, in our Pediatric Institute, with high doses of magnesium pidolate and magnesium and potassium citrate. The patient began to neglect this therapy after experiencing frequent daily episodes of diarrhoea. Our pharmacy received a request for an alternative magnesium supplement that would better comply by ensuring a good magnesium intake which will result in adequate blood magnesium levels. In response, we developed a galenic compound in the form of effervescent magnesium. Here, we report on the promise of this formulation not only for better compliance than pidolate, but also for better bioavailability. Full article

(This article belongs to the Special Issue Maximising Drug Delivery for Improved Pharmacokinetics and Pharmacodynamics)

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