Special Issue "Drug Delivery across Biological Barriers"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: 20 November 2019.

Special Issue Editors

Prof. Tatiana B. Tennikova
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Guest Editor
Saint Petersburg State University, Saint Petersburg, 199034, Russia
Interests: advanced biomaterials; nanotechnology; drug delivery systems; polymers; biodegradation; proteins; receptor-ligand interactions
Prof. Evgenia G. Korzhikova-Vlakh
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Guest Editor
Institute of Macromolecular Compounds, Russian Academy of Sciences, Saint-Petersburg, 199004, Russia
Interests: amphiphilic polymers; self-assembling; nanoparticles; biodegradation; drug delivery systems; proteins, DNA/RNA

Special Issue Information

Dear Colleagues,

Assuring the efficient transport of therapeutics in the body represents the crucial problem that should be taken into consideration during the construction of advanced drug delivery nanosystems. Recent advances in the development of biomaterials, including their nanoparticulated forms, have rendered a significant improvement of the currently proposed drug delivery strategies. Besides the increased bioavailability of pharmaceutical agents as a result of protecting them from degradation, targeting them directly to diseased sites, and controlling their circulation time and release rate, the problem of penetration across tissues and/or entry within cells seems to be important and needs to be solved. The design of strategies to control the transport of therapeutic compounds through such physiological barriers as mucosal, endothelial, blood–brain, cellular membrane and numerous other barriers has become an imperative and a challenging need to provide better therapy efficacy.

This Special Issue will provide readers with an overview of the current advances in this field regarding delivery systems that facilitate the transport of drug-containing nanosystems at the tissue, cell, and subcellular levels.

Prof. Tatiana B. Tennikova
Prof. Evgenia G. Korzhikova-Vlakh
Guest Editors

Manuscript Submission Information

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Keywords

  • drug delivery
  • nanosystems
  • biological barriers
  • drug transport across the barriers

Published Papers (4 papers)

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Research

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Open AccessArticle
Improved In Vitro Model for Intranasal Mucosal Drug Delivery: Primary Olfactory and Respiratory Epithelial Cells Compared with the Permanent Nasal Cell Line RPMI 2650
Pharmaceutics 2019, 11(8), 367; https://doi.org/10.3390/pharmaceutics11080367 - 01 Aug 2019
Abstract
Background: The epithelial layer of the nasal mucosa is the first barrier for drug permeation during intranasal drug delivery. With increasing interest for intranasal pathways, adequate in vitro models are required. Here, porcine olfactory (OEPC) and respiratory (REPC) primary cells were characterised against [...] Read more.
Background: The epithelial layer of the nasal mucosa is the first barrier for drug permeation during intranasal drug delivery. With increasing interest for intranasal pathways, adequate in vitro models are required. Here, porcine olfactory (OEPC) and respiratory (REPC) primary cells were characterised against the nasal tumour cell line RPMI 2650. Methods: Culture conditions for primary cells from porcine nasal mucosa were optimized and the cells characterised via light microscope, RT-PCR and immunofluorescence. Epithelial barrier function was analysed via transepithelial electrical resistance (TEER), and FITC-dextran was used as model substance for transepithelial permeation. Beating cilia necessary for mucociliary clearance were studied by immunoreactivity against acetylated tubulin. Results: OEPC and REPC barrier models differ in TEER, transepithelial permeation and MUC5AC levels. In contrast, RPMI 2650 displayed lower levels of MUC5AC, cilia markers and TEER, and higher FITC-dextran flux rates. Conclusion: To screen pharmaceutical formulations for intranasal delivery in vitro, translational mucosal models are needed. Here, a novel and comprehensive characterisation of OEPC and REPC against RPMI 2650 is presented. The established primary models display an appropriate model for nasal mucosa with secreted MUC5AC, beating cilia and a functional epithelial barrier, which is suitable for long-term evaluation of sustained release dosage forms. Full article
(This article belongs to the Special Issue Drug Delivery across Biological Barriers)
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Open AccessArticle
Boosting Drug Discovery for Parkinson’s: Enhancement of the Delivery of a Monoamine Oxidase-B Inhibitor by Brain-Targeted PEGylated Polycaprolactone-Based Nanoparticles
Pharmaceutics 2019, 11(7), 331; https://doi.org/10.3390/pharmaceutics11070331 - 12 Jul 2019
Abstract
The current pharmacological treatments for Parkinson’s disease only offer symptomatic relief to the patients and are based on the administration of levodopa and catechol-O-methyltransferase or monoamine oxidase-B inhibitors (IMAO-B). Since the majority of drug candidates fail in pre- and clinical trials, due largely [...] Read more.
The current pharmacological treatments for Parkinson’s disease only offer symptomatic relief to the patients and are based on the administration of levodopa and catechol-O-methyltransferase or monoamine oxidase-B inhibitors (IMAO-B). Since the majority of drug candidates fail in pre- and clinical trials, due largely to bioavailability pitfalls, the use of polymeric nanoparticles (NPs) as drug delivery systems has been reported as an interesting tool to increase the stealth capacity of drugs or help drug candidates to surpass biological barriers, among other benefits. Thus, a novel potent, selective, and reversible IMAO-B (chromone C27, IC50 = 670 ± 130 pM) was encapsulated in poly(caprolactone) (PCL) NPs by a nanoprecipitation process. The resulting C27-loaded PEGylated PCL NPs (~213 nm) showed high stability and no cytotoxic effects in neuronal (SH-SY5Y), epithelial (Caco-2), and endothelial (hCMEC/D3) cells. An accumulation of PEGylated PCL NPs in the cytoplasm of SH-SY5Y and hCMEC/D3 cells was also observed, and their permeation across Caco-2 and hCMEC/D3 cell monolayers, used as in vitro models of the human intestine and blood-brain barrier, respectively, was demonstrated. PEGylated PCL NPs delivered C27 at concentrations higher than the MAO-B IC50 value, which provides evidence of their relevance to solving the drug discovery pitfalls. Full article
(This article belongs to the Special Issue Drug Delivery across Biological Barriers)
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Open AccessFeature PaperArticle
pH-Sensitive Chitosan–Heparin Nanoparticles for Effective Delivery of Genetic Drugs into Epithelial Cells
Pharmaceutics 2019, 11(7), 317; https://doi.org/10.3390/pharmaceutics11070317 - 05 Jul 2019
Cited by 2
Abstract
Chitosan has been extensively studied as a genetic drug delivery platform. However, its efficiency is limited by the strength of DNA and RNA binding. Expecting a reduced binding strength of cargo with chitosan, we proposed including heparin as a competing polyanion in the [...] Read more.
Chitosan has been extensively studied as a genetic drug delivery platform. However, its efficiency is limited by the strength of DNA and RNA binding. Expecting a reduced binding strength of cargo with chitosan, we proposed including heparin as a competing polyanion in the polyplexes. We developed chitosan–heparin nanoparticles by a one-step process for the local delivery of oligonucleotides. The size of the polyplexes was dependent on the mass ratio of polycation to polyanion. The mechanism of oligonucleotide release was pH-dependent and associated with polyplex swelling and collapse of the polysaccharide network. Inclusion of heparin enhanced the oligonucleotide release from the chitosan-based polyplexes. Furthermore, heparin reduced the toxicity of polyplexes in the cultured cells. The cell uptake of chitosan–heparin polyplexes was equal to that of chitosan polyplexes, but heparin increased the transfection efficiency of the polyplexes two-fold. The application of chitosan–heparin small interfering RNA (siRNA) targeted to vascular endothelial growth factor (VEGF) silencing of ARPE-19 cells was 25% higher. Overall, chitosan–heparin polyplexes showed a significant improvement of gene release inside the cells, transfection, and gene silencing efficiency in vitro, suggesting that this fundamental strategy can further improve the transfection efficiency with application of non-viral vectors. Full article
(This article belongs to the Special Issue Drug Delivery across Biological Barriers)
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Review

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Open AccessReview
Established and Emerging Strategies for Drug Delivery Across the Blood-Brain Barrier in Brain Cancer
Pharmaceutics 2019, 11(5), 245; https://doi.org/10.3390/pharmaceutics11050245 - 24 May 2019
Cited by 1
Abstract
Brain tumors are characterized by very high mortality and, despite the continuous research on new pharmacological interventions, little therapeutic progress has been made. One of the main obstacles to improve current treatments is represented by the impermeability of the blood vessels residing within [...] Read more.
Brain tumors are characterized by very high mortality and, despite the continuous research on new pharmacological interventions, little therapeutic progress has been made. One of the main obstacles to improve current treatments is represented by the impermeability of the blood vessels residing within nervous tissue as well as of the new vascular net generating from the tumor, commonly referred to as blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB), respectively. In this review, we focused on established and emerging strategies to overcome the blood-brain barrier to increase drug delivery for brain cancer. To date, there are three broad strategies being investigated to cross the brain vascular wall and they are conceived to breach, bypass, and negotiate the access to the nervous tissue. In this paper, we summarized these approaches highlighting their working mechanism and their potential impact on the quality of life of the patients as well as their current status of development. Full article
(This article belongs to the Special Issue Drug Delivery across Biological Barriers)
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