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Special Issue "Drug Candidates and Drug Delivery Systems for Tuberculosis Treatment"

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 31 July 2023 | Viewed by 2733

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Dr. Sara Consalvi

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Guest Editor

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universitaà di Roma, Piazzale Aldo Moro 5, 00185 Rome, Italy
Interests: medicinal chemistry; drug discovery and development; antimycobacterial agents; small molecules; tuberculosis

Special Issue Information

Dear Colleagues,

Tuberculosis (TB) is the leading cause of death from a bacterial infection worldwide, causing an estimated 1.5 million of deaths in 2020. The spread of drug-resistant infections strongly limits treatment options and underscores the importance of finding new drugs, new bacterial targets, as well as innovative delivery systems to improve available therapeutic tools. An urgent response is then required to prevent and treat infections, limit the spread of resistance, and foster progress towards the WHO End TB strategy goal of a 90% reduction in deaths and an 80% reduction in the TB incidence rate by 2030, compared to the 2015 baseline.

This Special Issue aims to summarize recent research in the field of TB drug development, discussing state-of-the art advances and latest development in the field and covering all the aspects and stages of investigation of innovative candidates for TB treatment, including innovative delivery protocols of both existing and novel antimycobacterial agents.

Potential topics to be covered include, but are not limited to:

Development of novel and effective antimycobacterial agents;
Innovative drug delivery systems for TB treatment;
Innovative strategies to overcome drug resistance;
Emerging molecular targets for TB drug discovery;
Host-targeted therapies.

Dr. Sara Consalvi
Guest Editor

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2600 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

medicinal chemistry
tuberculosis
TB drug discovery and development
drug resistance
antimycobacterials

Published Papers (3 papers)

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Research

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Open AccessArticle

In Vivo Toxicity, Redox-Modulating Capacity and Intestinal Permeability of Novel Aroylhydrazone Derivatives as Anti-Tuberculosis Agents

and

Pharmaceutics 2023, 15(1), 79; https://doi.org/10.3390/pharmaceutics15010079 - 26 Dec 2022

Cited by 1 | Viewed by 776

Abstract

The emergence and spread of Mycobacterium tuberculosis strains resistant to many or all anti-tuberculosis (TB) drugs require the development of new compounds both efficient and with minimal side effects. Structure-activity-toxicity relationships of such novel, structurally diverse compounds must be thoroughly elucidated before further development. Here, we present the aroylhydrazone compounds (3a and 3b) regarding their: (i) acute and subacute toxicity in mice; (ii) redox-modulating in vivo and in vitro capacity; (iii) pathomorphology in the liver, kidney, and small intestine tissue specimens; and (iv) intestinal permeability. The acute toxicity test showed that the two investigated compounds exhibited low toxicity by oral and intraperitoneal administration. Changes in behavior, food amount, and water intake were not observed during 14 days of the oral administration at two doses of 1/10 and 1/20 of the LD₅₀. The histological examination of the different tissue specimens did not show toxic changes. The in vitro antioxidant assays confirmed the ex vivo results. High gastrointestinal tract permeability at all tested pH values were demonstrated for both compounds. To conclude, both compounds 3a and 3b are highly permeable with low toxicity and can be considered for further evaluation and/or lead optimization. Full article

(This article belongs to the Special Issue Drug Candidates and Drug Delivery Systems for Tuberculosis Treatment)

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Open AccessArticle

Determination of the Pharmacokinetics and Pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a Cross-Over Cynomolgus Macaque Model of Mycobacterium tuberculosis Infection

Pharmaceutics 2022, 14(12), 2666; https://doi.org/10.3390/pharmaceutics14122666 - 30 Nov 2022

Viewed by 861

Abstract

Innovative cross-over study designs were explored in non-human primate (NHP) studies to determine the value of this approach for the evaluation of drug efficacy against tuberculosis (TB). Firstly, the pharmacokinetics (PK) of each of the drugs Isoniazid (H), Rifampicin (R), Pyrazinamide (Z) and Ethambutol (E), that are standardly used for the treatment of tuberculosis, was established in the blood of macaques after oral dosing as a monotherapy or in combination. Two studies were conducted to evaluate the pharmacokinetics and pharmacodynamics of different drug combinations using cross-over designs. The first employed a balanced, three-period Pigeon design with an extra period; this ensured that treatment by period interactions and carry-over could be detected comparing the treatments HR, HZ and HRZ using H37Rv as the challenge strain of Mycobacterium tuberculosis (M. tb). Although the design accounted for considerable variability between animals, the three regimens evaluated could not be distinguished using any of the alternative endpoints assessed. However, the degree of pathology achieved using H37Rv in the model during this study was less than expected. Based on these findings, a second experiment using a classical AB/BA design comparing HE with HRZ was conducted using the M. tb Erdman strain. More extensive pathology was observed, and differences in computerized tomography (CT) scores and bacteriology counts in the lungs were detected, although due to the small group sizes, clearer differences were not distinguished. Type 1 T helper (Th1) cell response profiles were characterized using the IFN-γ ELISPOT assay and revealed differences between drug treatments that corresponded to decreases in disease burden. Therefore, the studies performed support the utility of the NHP model for the determination of PK/PD of TB drugs, although further work is required to optimize the use of cross-over study designs. Full article

(This article belongs to the Special Issue Drug Candidates and Drug Delivery Systems for Tuberculosis Treatment)

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Review

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Open AccessReview

Infant Exposure to Antituberculosis Drugs via Breast Milk and Assessment of Potential Adverse Effects in Breastfed Infants: Critical Review of Data

Engi Abdelhady Algharably

Reinhold Kreutz

and

Ursula Gundert-Remy

Pharmaceutics 2023, 15(4), 1228; https://doi.org/10.3390/pharmaceutics15041228 - 13 Apr 2023

Viewed by 612

Abstract

Infants of mothers treated for tuberculosis might be exposed to drugs via breast milk. The existing information on the exposure of breastfed infants lacks a critical review of the published data. We aimed to evaluate the quality of the existing data on antituberculosis (anti-TB) drug concentrations in the plasma and milk as a methodologically sound basis for the potential risk of breastfeeding under therapy. We performed a systematic search in PubMed for bedaquiline, clofazimine, cycloserine/terizidone, levofloxacin, linezolid, pretomanid/pa824, pyrazinamide, streptomycin, ethambutol, rifampicin and isoniazid, supplemented with update references found in LactMed^®. We calculated the external infant exposure (EID) for each drug and compared it with the recommended WHO dose for infants (relative external infant dose) and assessed their potential to elicit adverse effects in the breastfed infant. Breast milk concentration data were mainly not satisfactory to properly estimate the EID. Most of the studies suffer from limitations in the sample collection, quantity, timing and study design. Infant plasma concentrations are extremely scarce and very little data exist documenting the clinical outcome in exposed infants. Concerns for potential adverse effects in breastfed infants could be ruled out for bedaquiline, cycloserine/terizidone, linezolid and pyrazinamide. Adequate studies should be performed covering the scenario in treated mothers, breast milk and infants. Full article

(This article belongs to the Special Issue Drug Candidates and Drug Delivery Systems for Tuberculosis Treatment)

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Special Issue "Drug Candidates and Drug Delivery Systems for Tuberculosis Treatment"

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