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Drug Delivery Systems for Overcoming the Biological Barriers and Improving the Therapeutic Effect

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 18471

Special Issue Editors


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Guest Editor
Arbuzov Institute of Organic and Physical Chemistry—Subdivision of the Federal Research Center “Kazan Scientific Center of Russian Academy of Sciences”, Kazan, Russia
Interests: amphiphilic compounds; cationic surfactants; self-assembly; polyfunctional supramolecular systems; polyelectrolytes; micellar catalysis; solubilization; drug delivery
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Guest Editor
Arbuzov Institute of Organic and Physical Chemistry—Subdivision of the Federal Research Center “Kazan Scientific Center of Russian Academy of Sciences”, Kazan, Russia
Interests: supramolecular chemistry; calixarenes; cyclodextrins; surfactants; quantum dots; drug delivery; biomimetics; sensors

Special Issue Information

Dear Colleagues,

We invite you to contribute a full research paper or review article for peer review and possible publication in the Special Issue “Drug Delivery Systems for Overcoming the Biological Barriers and Improving the Therapeutic Effect”. This Special Issue will be devoted to the fundamental aspects of design of effective drug delivery systems and the potential application of these systems in different therapies, with special emphasis on overcoming biological barriers. Given the structural features and functions of biological barriers, improved therapy with drug nanocarriers will provide a better chance of mitigating the harmful effects on the human body. We believe that this Special Issue topic is very interesting and timely and hope that it will present a collection of works that will be a useful reference for scholars in the field.

Dr. Lucia Zakharova
Dr. Ruslan R. Kashapov
Guest Editors

Manuscript Submission Information

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Keywords

  • drug delivery
  • biological barriers
  • nanoparticles
  • encapsulation
  • solubilization
  • colloids
  • supramolecular systems
  • bio- and nanotechnology

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Published Papers (5 papers)

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Research

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14 pages, 2386 KiB  
Article
Formulation and Characterization of Chitosan-Decorated Multiple Nanoemulsion for Topical Delivery In Vitro and Ex Vivo
by Muhammad Rehan Malik, Fatemah Farraj Al-Harbi, Asif Nawaz, Adnan Amin, Arshad Farid, Mohammed Al Mohaini, Abdulkhaliq J. Alsalman, Maitham A. Al Hawaj and Yousef N. Alhashem
Molecules 2022, 27(10), 3183; https://doi.org/10.3390/molecules27103183 - 17 May 2022
Cited by 18 | Viewed by 3323
Abstract
In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was evaluated physiochemically for its size and zeta potential, surface morphology, creaming and cracking, viscosity and pH. A Franz diffusion cell apparatus was used [...] Read more.
In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was evaluated physiochemically for its size and zeta potential, surface morphology, creaming and cracking, viscosity and pH. A Franz diffusion cell apparatus was used to carry out in vitro drug-release and permeation studies. The formulated nanoemulsion showed uniform droplet size and zeta potential. The pH and viscosity of the formulated emulsion were in the range of and suitable for topical delivery. The drug contents of the simple nanoemulsion (SNE), the chitosan-decorated nanoemulsion (CNE) and the MNE were 71 ± 2%, 82 ± 2% and 90 ± 2%, respectively. The formulated MNE showed controlled release of itraconazole as compared with that of the SNE and CNE. This was attributed to the chitosan decoration as well as to formulating multiple emulsions. The significant permeation and skin drug retention profile of the MNE were attributed to using the surfactants tween 80 and span 20 and the co-surfactant PEG 400. ATR-FTIR analysis confirmed that the MNE mainly affects the lipids and proteins of the skin, particularly the stratum corneum, which results in significantly higher permeation and retention of the drug. It was concluded that the proposed MNE formulation delivers drug to the target site of the skin and can be therapeutically used for various cutaneous fungal infections. Full article
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12 pages, 1742 KiB  
Article
Permeability of the Perindopril Arginine under In Vitro Conditions across Caco-2 Monolayer and Biomimetic Phospholipid Membrane
by Marta Kus, Klaudia Gorniak, Piotr Czaklosz, Anna Olejnik, Paulina Skupin-Mrugalska, Izabela Ibragimow and Hanna Piotrowska-Kempisty
Molecules 2022, 27(7), 2232; https://doi.org/10.3390/molecules27072232 - 30 Mar 2022
Cited by 2 | Viewed by 3011
Abstract
Perindopril arginine (PA) as an angiotensin-converting enzyme (ACE) inhibitor is widely used in cardiovascular diseases, especially in systemic hypertension and heart failure. Although the pharmacokinetics of PA are well documented, there is no available detailed data on its permeation in in vitro conditions. [...] Read more.
Perindopril arginine (PA) as an angiotensin-converting enzyme (ACE) inhibitor is widely used in cardiovascular diseases, especially in systemic hypertension and heart failure. Although the pharmacokinetics of PA are well documented, there is no available detailed data on its permeation in in vitro conditions. The present study aimed to assess the transport of PA across both biological membranes and artificial biomimetic ones. For the determination of PA transport, the Caco-2 cell line was selected as a reliable in vitro model of gastrointestinal biological barriers. Additionally, a novel 96-well plate with phospholipid membrane PermeaPad was used to evaluate the transport of PA by passive diffusion. We confirmed that PA is relatively poorly permeable across the Caco-2 monolayer. The permeability results obtained from the non-cell-based model demonstrated higher transport of PA as compared to that of Caco-2. Thus, PA transport across the biological membranes might be suggested to be regulated by the membrane transporters. Full article
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21 pages, 4887 KiB  
Article
Phytochemical Analysis, Antioxidant, and Wound Healing Activity of Pluchea indica L. (Less) Branch Extract Nanoparticles
by Rattanakorn Chiangnoon, Weerasak Samee, Pimpon Uttayarat, Wullapa Jittachai, Warintorn Ruksiriwanich, Sarana Rose Sommano, Sirivan Athikomkulchai and Chuda Chittasupho
Molecules 2022, 27(3), 635; https://doi.org/10.3390/molecules27030635 - 19 Jan 2022
Cited by 20 | Viewed by 3166
Abstract
Proliferation and migration of keratinocytes and fibroblasts play an important role in cutaneous wound healing, while oral mucosal squamous cell proliferation and migration are crucial for oral wound healing. In this study, the phytochemical profile of Pluchea indica branch ethanolic extract was characterized. [...] Read more.
Proliferation and migration of keratinocytes and fibroblasts play an important role in cutaneous wound healing, while oral mucosal squamous cell proliferation and migration are crucial for oral wound healing. In this study, the phytochemical profile of Pluchea indica branch ethanolic extract was characterized. The bioactive compound of Pluchea indica branch ethanolic extract was identified and analyzed by the validated HPLC method. The nanoparticles of P. indica branch extract were formulated by solvent displacement method to increase the solubility and the colloidal stability of the extract. The stability of the nanoparticles was investigated by using the dynamic light scattering technique. Effects of P. indica crude extract and nanoparticles on cell viability, proliferation and migration of primary epidermal keratinocytes, human dermal fibroblasts, and oral mucosal keratinocyte cells were investigated by MTT assay and scratch assay, respectively. The results showed that P. indica branch extract contained a high content of total phenolic and total flavonoids. The HPLC analysis revealed that the main compound in the extract was 4,5-O-dicaffeoylquinic acid. The cell viability of the extract and nanoparticles decreased when cells were exposed to a high concentration of extract and nanoparticles. These results demonstrate that P. indica branch extract and extract nanoparticles at specific concentrations possess in vitro wound healing activity and they may be possibly used to treat different types of wounds including dermal and oral mucosal wounds. Full article
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15 pages, 3715 KiB  
Article
Ultrasound Microbubbles Enhance the Efficacy of Insulin-Like Growth Factor-1 Therapy for the Treatment of Noise-Induced Hearing Loss
by Yi-Chun Lin, Yuan-Yung Lin, Hsin-Chien Chen, Chao-Yin Kuo, Ai-Ho Liao, Ying-Liang Chou, Chia-Lien Hung, Cheng-Ping Shih and Chih-Hung Wang
Molecules 2021, 26(12), 3626; https://doi.org/10.3390/molecules26123626 - 13 Jun 2021
Cited by 9 | Viewed by 2822
Abstract
The application of insulin-like growth factor 1 (IGF-1) to the round window membrane (RWM) is an emerging treatment for inner ear diseases. RWM permeability is the key factor for efficient IGF-1 delivery. Ultrasound microbubbles (USMBs) can increase drug permeation through the RWM. In [...] Read more.
The application of insulin-like growth factor 1 (IGF-1) to the round window membrane (RWM) is an emerging treatment for inner ear diseases. RWM permeability is the key factor for efficient IGF-1 delivery. Ultrasound microbubbles (USMBs) can increase drug permeation through the RWM. In the present study, the enhancing effect of USMBs on the efficacy of IGF-1 application and the treatment effect of USMB-mediated IGF-1 delivery for noise-induced hearing loss (NIHL) were investigated. Forty-seven guinea pigs were assigned to three groups: the USM group, which received local application of recombinant human IGF-1 (rhIGF-1, 10 µg/µL) following application of USMBs to the RWM; the RWS group, which received IGF-1 application alone; and the saline-treated group. The perilymphatic concentration of rhIGF-1 in the USM group was 1.95- and 1.67- fold of that in the RWS group, 2 and 24 h after treatment, respectively. After 5 h of 118 dB SPL noise exposure, the USM group had the lowest threshold shift in auditory brainstem response, least loss of cochlear outer hair cells, and least reduction in the number of synaptic ribbons on postexposure day 28 among the three groups. The combination of USMB and IGF-1 led to a better therapeutic response to NIHL. Two hours after treatment, the USM group had significantly higher levels of Akt1 and Mapk3 gene expression than the other two groups. The most intense immunostaining for phosphor-AKT and phospho-ERK1/2 was detected in the cochlea in the USM group. These results suggested that USMB can be applied to enhance the efficacy of IGF-1 therapy in the treatment of inner ear diseases. Full article
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Review

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40 pages, 12284 KiB  
Review
Self-Assembling Drug Formulations with Tunable Permeability and Biodegradability
by Gulnara Gaynanova, Leysan Vasileva, Ruslan Kashapov, Darya Kuznetsova, Rushana Kushnazarova, Anna Tyryshkina, Elmira Vasilieva, Konstantin Petrov, Lucia Zakharova and Oleg Sinyashin
Molecules 2021, 26(22), 6786; https://doi.org/10.3390/molecules26226786 - 10 Nov 2021
Cited by 34 | Viewed by 4673
Abstract
This review focuses on key topics in the field of drug delivery related to the design of nanocarriers answering the biomedicine criteria, including biocompatibility, biodegradability, low toxicity, and the ability to overcome biological barriers. For these reasons, much attention is paid to the [...] Read more.
This review focuses on key topics in the field of drug delivery related to the design of nanocarriers answering the biomedicine criteria, including biocompatibility, biodegradability, low toxicity, and the ability to overcome biological barriers. For these reasons, much attention is paid to the amphiphile-based carriers composed of natural building blocks, lipids, and their structural analogues and synthetic surfactants that are capable of self-assembly with the formation of a variety of supramolecular aggregates. The latter are dynamic structures that can be used as nanocontainers for hydrophobic drugs to increase their solubility and bioavailability. In this section, biodegradable cationic surfactants bearing cleavable fragments are discussed, with ester- and carbamate-containing analogs, as well as amino acid derivatives received special attention. Drug delivery through the biological barriers is a challenging task, which is highlighted by the example of transdermal method of drug administration. In this paper, nonionic surfactants are primarily discussed, including their application for the fabrication of nanocarriers, their surfactant-skin interactions, the mechanisms of modulating their permeability, and the factors controlling drug encapsulation, release, and targeted delivery. Different types of nanocarriers are covered, including niosomes, transfersomes, invasomes and chitosomes, with their morphological specificity, beneficial characteristics and limitations discussed. Full article
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