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Pharmaceutics
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Transport of Drugs through Biological Barriers—an Asset or Risk
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Transport of Drugs through Biological Barriers—an Asset or Risk

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

Deadline for manuscript submissions: 20 December 2024 | Viewed by 7039

Special Issue Editors

Dr. Anna Sobańska

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Guest Editor
Department of Analytical Chemistry, Faculty of Pharmacy, Medical University of Lodz, Łódź, Poland
Interests: QSAR; liquid chromatography; ADMET studies in silico and in vitro; environmental toxicology; spectroscopy
Special Issues, Collections and Topics in MDPI journals
Dr. Heidi Kidron

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Guest Editor
Drug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, Finland
Interests: transporters; permeability; blood-brain barrier; pharmacokinetics
Dr. Franciska Erdő

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Guest Editor
Faculty of Information Technology and Bionics, Pázmány Péter Catholic University, Práter u. 50A, H-1083 Budapest, Hungary
Interests: drug-delivery; nose-to-brain delivery; transporters; dermal barrier; blood-brain barrier; lab-on-a-chip technology; Franz diffusion cells
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drug transport across biological barriers in humans and animals plays a key role in drug delivery to a biological target. Insufficient drug transport is a serious obstacle to a drug’s intended activity.  In some cases, however, undesired compounds are absorbed through biological barriers (e.g., the skin, placenta or blood–brain barrier), posing a danger to humans and animals alike. 

This Special Issue primarily focuses on (but it is not limited to) the following:

  • In vivo, in vitro or in silico studies of drug transport through biological membranes;
  • Compound absorption from the gastro-intestinal tract, through skin or mucous membranes;
  • Pulmonary or ophthalmic absorption;
  • Transport of unwanted chemicals through the placenta or to mothers' milk;
  • Blood–brain barrier transport of xenobiotics;
  • Human and animal absorption of environmental contaminants via different routes;
  • Studies of compounds’ drug-likeness;
  • QSAR permeability studies;
  • Alternative drug delivery routes—novel methods or formulations.

Dr. Anna Sobańska
Dr. Heidi Kidron
Dr. Franciska Erdő
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. 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

  • ADMET studies
  • blood–brain barrier
  • gastro-intestinal absorption
  • placenta permeability
  • drug-likeness
  • skin/dermal absorption
  • drug delivery routes
  • compound transport across biological membranes
  • absorption of environmental contaminants
  • QSAR permeability studies

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Published Papers (6 papers)

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Research

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15 pages, 3327 KiB  
Article
Palmitoylethanolamide-Incorporated Elastic Nano-Liposomes for Enhanced Transdermal Delivery and Anti-Inflammation
by Chuanpeng Ren, Yanyun Ma, Yizhen Wang, Dan Luo, Yanhan Hong, Xinyuan Zhang, Hexiang Mei and Wei Liu
Pharmaceutics 2024, 16(7), 876; https://doi.org/10.3390/pharmaceutics16070876 - 29 Jun 2024
Viewed by 577
Abstract
Palmitoylethanolamide (PEA) exhibits multiple skincare functions such as anti-nociceptive and anti-inflammatory effects. However, its topical application is limited due to its difficulty in bypassing the stratum corneum barrier, relatively low bioavailability, and low stability. Herein, elastic nano-liposomes (ENLs) with excellent deformability and elasticity [...] Read more.
Palmitoylethanolamide (PEA) exhibits multiple skincare functions such as anti-nociceptive and anti-inflammatory effects. However, its topical application is limited due to its difficulty in bypassing the stratum corneum barrier, relatively low bioavailability, and low stability. Herein, elastic nano-liposomes (ENLs) with excellent deformability and elasticity were utilized as a novel drug delivery system to encapsulate PEA to overcome the abovementioned issues and enhance the biological effects on the skin. ENL was prepared with phosphatidylcholine, cholesterol, and cetyl-PG hydroxyethyl palmitamide with a molar ratio mimicking skin epidermal lipids, and PEA was loaded. The PEA-loaded ENL (PEA-ENL) demonstrated efficient transdermal delivery and enhanced skin retention, with negligible cytotoxicity toward HaCaT cells and no allergic reaction in the human skin patch test. Notably, PEA-ENL treatment increased cell migration and induced significant regulation in the expression of genes associated with anti-nociceptive, anti-inflammatory, and skin barrier repair. The mechanism of the anti-nociceptive and anti-inflammatory effects of PEA was further investigated and explained by molecular docking site analysis. This novel PEA-ENL, with efficient transdermal delivery efficiency and multiple skincare functionalities, is promising for topical application. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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15 pages, 1621 KiB  
Article
Layered Double Hydroxides (LDH) as Delivery Vehicles of a Chimeric Protein Carrying Epitopes from the Porcine Reproductive and Respiratory Syndrome Virus
by María José Alonso-Cerda, Mariano J. García-Soto, Arleth Miranda-López, René Segura-Velázquez, José Ivan Sánchez-Betancourt, Omar González-Ortega and Sergio Rosales-Mendoza
Pharmaceutics 2024, 16(7), 841; https://doi.org/10.3390/pharmaceutics16070841 - 21 Jun 2024
Viewed by 680
Abstract
The Porcine Reproductive and Respiratory Syndrome Virus (PRRSV) causes reproductive failure and respiratory symptoms, leading to huge economic losses for the pig farming industry. Although several vaccines against PRRSV are available in the market; they show an overall low efficacy, and several countries [...] Read more.
The Porcine Reproductive and Respiratory Syndrome Virus (PRRSV) causes reproductive failure and respiratory symptoms, leading to huge economic losses for the pig farming industry. Although several vaccines against PRRSV are available in the market; they show an overall low efficacy, and several countries have the need for vaccines covering the local, circulating variants. This project aims at developing a new chimeric antigen targeting specific epitopes from PRRSV and evaluating two test adjuvants to formulate a vaccine candidate. The test antigen was called LTB–PRRSV, which was produced recombinantly in Escherichia coli and consisted of the heat labile enterotoxin B subunit from E. coli (LTB) and four epitopes from PRRSV. LTB–PRRSV was rescued as inclusion bodies and methods for its solubilization, IMAC-based purification, and refolding were standardized, leading to mean yields of 18 mg of pure protein per liter culture. Layered double hydroxides (LDH) have been used as vaccine adjuvants given their biocompatibility, low cost, and positive surface charge that allows an efficient adsorption of negatively charged biomolecules. Therefore, LDH were selected as delivery vehicles of LTB–PRRSV. Pure LTB–PRRSV was adsorbed onto LDH by incubation at different LDH:LTB–PRRSV mass ratios (1:0.25, 1:0.5, 1:1, and 1:2) and at pH 9.5. The best adsorption occurred with a 1:2 mass ratio, and in a sucrose-tween solution. The conjugates obtained had a polydispersity index of 0.26, a hydrodynamic diameter of 192 nm, and a final antigen concentration of 64.2 μg/mL. An immunogenicity assessment was performed by injecting mice with LDH:LTB–PRRSV, Alum/LTB–PRRSV, or LTB–PRRSV in a scheme comprising three immunizations at two-week intervals and two dose levels (1 and 5 μg). LTB–PRRSV was capable of inducing strong humoral responses, which lasted for a longer period when LDH was used as the delivery vehicle/adjuvant. The potential of LDH to serve as an attractive carrier for veterinary vaccines is discussed. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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12 pages, 1025 KiB  
Article
ABCG2 Transports the Flukicide Nitroxynil and Affects Its Biodistribution and Secretion into Milk
by Laura Álvarez-Fernández, Esther Blanco-Paniagua and Gracia Merino
Pharmaceutics 2024, 16(4), 558; https://doi.org/10.3390/pharmaceutics16040558 - 19 Apr 2024
Viewed by 837
Abstract
The ABCG2 transporter plays a key role in pharmacological and toxicological processes, affecting bioavailability, tissue accumulation and milk secretion of its substrates. This protein is expressed in several biological barriers acting as a protective mechanism against xenobiotic exposure by pumping out a broad [...] Read more.
The ABCG2 transporter plays a key role in pharmacological and toxicological processes, affecting bioavailability, tissue accumulation and milk secretion of its substrates. This protein is expressed in several biological barriers acting as a protective mechanism against xenobiotic exposure by pumping out a broad range of compounds. However, its induced expression during lactation in alveolar cells of mammary gland represents a relevant route for active transport of unwanted chemicals into milk. This work aimed to characterize the involvement of ABCG2 in systemic exposure and milk secretion of the flukicide nitroxynil. Using MDCK–II cells overexpressing the transporter, we showed that nitroxynil is an in vitro substrate of different species variants of ABCG2. Moreover, using wild-type and Abcg2−/− mice, we showed that murine Abcg2 clearly affects plasma levels of nitroxynil. We also reported differences in nitroxynil accumulation in several tissues, with almost 2-fold higher concentration in kidney, small intestine and testis of Abcg2−/− mice. Finally, we proved that nitroxynil secretion into milk was also affected by Abcg2, with a 1.9-fold higher milk concentration in wild-type compared with Abcg2−/− mice. We conclude that ABCG2 significantly impacts nitroxynil biodistribution by regulating its passage across biological barriers. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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19 pages, 1407 KiB  
Article
Transport of Non-Steroidal Anti-Inflammatory Drugs across an Oral Mucosa Epithelium In Vitro Model
by Grace C. Lin, Heinz-Peter Friedl, Sarah Grabner, Anna Gerhartl and Winfried Neuhaus
Pharmaceutics 2024, 16(4), 543; https://doi.org/10.3390/pharmaceutics16040543 - 15 Apr 2024
Viewed by 1121
Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most prescribed drugs to treat pain or fever. However, oral administration of NSAIDs is frequently associated with adverse effects due to their inhibitory effect on the constitutively expressed cyclooxygenase enzyme 1 (COX-1) in, for instance, [...] Read more.
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most prescribed drugs to treat pain or fever. However, oral administration of NSAIDs is frequently associated with adverse effects due to their inhibitory effect on the constitutively expressed cyclooxygenase enzyme 1 (COX-1) in, for instance, the gastrointestinal tract. A systemic delivery, such as a buccal delivery, of NSAIDs would be beneficial and additionally has the advantage of a non-invasive administration route, especially favourable for children or the elderly. To investigate the transport of NSAIDs across the buccal mucosa and determine their potential for buccal therapeutic usage, celecoxib, diclofenac, ibuprofen and piroxicam were tested using an established oral mucosa Transwell® model based on human cell line TR146. Carboxyfluorescein and diazepam were applied as internal paracellular and transcellular marker molecule, respectively. Calculated permeability coefficients revealed a transport ranking of ibuprofen > piroxicam > diclofenac > celecoxib. Transporter protein inhibitor verapamil increased the permeability for ibuprofen, piroxicam and celecoxib, whereas probenecid increased the permeability for all tested NSAIDs. Furthermore, influence of local inflammation of the buccal mucosa on the transport of NSAIDs was mimicked by treating cells with a cytokine mixture of TNF-α, IL-1ß and IFN-γ followed by transport studies with ibuprofen (+ probenecid). Cellular response to pro-inflammatory stimuli was confirmed by upregulation of cytokine targets at the mRNA level, increased secreted cytokine levels and a significant decrease in the paracellular barrier. Permeability of ibuprofen was increased across cell layers treated with cytokines, while addition of probenecid increased permeability of ibuprofen in controls, but not across cell layers treated with cytokines. In summary, the suitability of the in vitro oral mucosa model to measure NSAID transport rankings was demonstrated, and the involvement of transporter proteins was confirmed; an inflammation model was established, and increased NSAID transport upon inflammation was measured. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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15 pages, 5905 KiB  
Article
An Improved In Vitro Blood-Brain Barrier Model for the Evaluation of Drug Permeability Using Transwell with Shear Stress
by Junhyeong Kim, Seong-Ah Shin, Chang Sup Lee and Hye Jin Chung
Pharmaceutics 2024, 16(1), 48; https://doi.org/10.3390/pharmaceutics16010048 - 28 Dec 2023
Cited by 1 | Viewed by 2039
Abstract
The development of drugs targeting the central nervous system (CNS) is challenging because of the presence of the Blood-Brain barrier (BBB). Developing physiologically relevant in vitro BBB models for evaluating drug permeability and predicting the activity of drug candidates is crucial. The transwell [...] Read more.
The development of drugs targeting the central nervous system (CNS) is challenging because of the presence of the Blood-Brain barrier (BBB). Developing physiologically relevant in vitro BBB models for evaluating drug permeability and predicting the activity of drug candidates is crucial. The transwell model is one of the most widely used in vitro BBB models. However, this model has limitations in mimicking in vivo conditions, particularly in the absence of shear stress. This study aimed to overcome the limitations of the transwell model using immortalized human endothelial cells (hCMEC/D3) by developing a novel dish design for an orbital shaker, providing shear stress. During optimization, we assessed cell layer integrity using trans-endothelial electrical resistance measurements and the % diffusion of lucifer yellow. The efflux transporter activity and mRNA expression of junctional proteins (claudin-5, occludin, and VE-cadherin) in the newly optimized model were verified. Additionally, the permeability of 14 compounds was evaluated and compared with published in vivo data. The cell-layer integrity was substantially increased using the newly designed annular shaking-dish model. The results demonstrate that our model provided robust conditions for evaluating the permeability of CNS drug candidates, potentially improving the reliability of in vitro BBB models in drug development. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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Review

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16 pages, 560 KiB  
Review
Assessment of Infant Exposure to Antidepressants through Breastfeeding: A Literature Review of Currently Available Approaches
by Leah Arbitman, Shirley Chen, Brian Kim, Melinda Lee, Peng Zou, Bennett Doughty, Yanyan Li and Tao Zhang
Pharmaceutics 2024, 16(7), 847; https://doi.org/10.3390/pharmaceutics16070847 - 22 Jun 2024
Cited by 1 | Viewed by 792
Abstract
Despite the prevalence of depression in lactating mothers, there is a lack of knowledge about the excretion of antidepressants into breast milk and its potential adverse effects on infants. This creates concern, making depressed lactating mothers more likely to avoid pharmacological treatment. Clinical [...] Read more.
Despite the prevalence of depression in lactating mothers, there is a lack of knowledge about the excretion of antidepressants into breast milk and its potential adverse effects on infants. This creates concern, making depressed lactating mothers more likely to avoid pharmacological treatment. Clinical lactation studies are the most accurate and direct method to predict and demonstrate the excretion of antidepressants into human breast milk, and results from clinical studies can be included in drug labels to help physicians and patients make decisions on antidepressant use during lactation. However, there are limited clinical trials and studies on the pharmacokinetics of antidepressants in lactating women because of a lack of enrollment and ethical and confounding factors, creating a lack of knowledge in this area. To bridge this gap in knowledge, alternative methods should be sought to help estimate the antidepressant concentration in breast milk, which is used to assess the safety and transfer of antidepressants into breast milk. We provide a comprehensive review of the usage of these cost-effective, time-efficient, and ethically feasible methods that serve to provide a valuable estimation of the safety and transfer of antidepressants into breast milk before conducting clinical studies. Full article
(This article belongs to the Special Issue Transport of Drugs through Biological Barriers—an Asset or Risk)
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