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Pharmaceutics
Special Issues
Intranasal Drug Delivery Systems
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Intranasal Drug Delivery Systems

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

Deadline for manuscript submissions: closed (30 September 2020) | Viewed by 27506

Special Issue Editors

Prof. Dr. Piroska Szabó-Révész

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Guest Editor
Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
Interests: particle engineering; modification of physicochemical properties of drugs; nanotechnology; nose-to-blood; nose-to-brain delivery; intranasal dosage forms
Prof. Dr. Ildikó Csóka

E-Mail Website
Guest Editor
Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
Interests: quality by design-based formulation strategies; regulatory science; patient centeredness in dosage form design; alternative administration routes; nose-to-brain delivery
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Rita Ambrus

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Guest Editor
Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
Interests: top down and bottom up methods; nano- and micro particle formulation; dry powder formulations; pulmonary administration; intranasal administration
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, intranasal (IN) drug delivery has become the focus of attention. IN administration is an effective way to deliver drugs into the systemic circulation (nose-to-blood delivery), resulting in rapid onset. However, we have less knowledge about nose-to-brain delivery where the nasal pathway may bypass the blood–brain barrier and allow centrally acting pharmacons to directly enter the central nervous system. IN drug delivery (particularly targeting specific tissues within the brain) will gain more importance.  The major challenge in IN drug delivery is getting to know the physicochemical properties of mucus and its impact on transmucosal drug delivery (mucus penetrating drug delivery). The physicochemical properties of the drugs fundamentally determine the IN transport, and, therefore, their modification or use of nanotechnology-based carriers are required.
The scope of this Special Issue is to present IN drug delivery systems/technologies that are related to the IN mucus penetrating particle delivery and nose-to-blood as well as nose-to-brain transports. We also welcome manuscripts related to quality assurance and the regulatory environment related to this topic.
We are looking forward to your related publications, hoping that this Special Issue improves our understanding of how the IN drug delivery systems work.

Prof. Dr. Piroska Szabó-Révész
Prof. Dr. Ildikó Csóka
Prof. Dr. Rita Ambrus
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

  • nose-to-blood delivery
  • brain targeting (nose-to-brain delivery)
  • mucosal drug delivery
  • enhance of mucus permeation
  • pharmaceutical nanotechnology
  • non-toxic formulation
  • development of experimental methods
  • nasal dosage forms
  • proteins
  • peptides
  • small molecule agents
  • quality assurance
  • regulatory

Published Papers (6 papers)

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Research

29 pages, 7841 KiB  
Article
Quality by Design Based Formulation Study of Meloxicam-Loaded Polymeric Micelles for Intranasal Administration
by Bence Sipos, Piroska Szabó-Révész, Ildikó Csóka, Edina Pallagi, Dorina Gabriella Dobó, Péter Bélteky, Zoltán Kónya, Ágota Deák, László Janovák and Gábor Katona
Pharmaceutics 2020, 12(8), 697; https://doi.org/10.3390/pharmaceutics12080697 - 24 Jul 2020
Cited by 36 | Viewed by 4757
Abstract
Our study aimed to develop an “ex tempore” reconstitutable, viscosity enhancer- and preservative-free meloxicam (MEL)-loaded polymeric micelle formulation, via Quality by Design (QbD) approach, exploiting the nose-to-brain pathway, as a suitable tool in the treatment of neuroinflammation. The anti-neuroinflammatory effect of nose-to-brain NSAID [...] Read more.
Our study aimed to develop an “ex tempore” reconstitutable, viscosity enhancer- and preservative-free meloxicam (MEL)-loaded polymeric micelle formulation, via Quality by Design (QbD) approach, exploiting the nose-to-brain pathway, as a suitable tool in the treatment of neuroinflammation. The anti-neuroinflammatory effect of nose-to-brain NSAID polymeric micelles was not studied previously, therefore its investigation is promising. Critical product parameters, encapsulation efficiency (89.4%), Z-average (101.22 ± 2.8 nm) and polydispersity index (0.149 ± 0.7) and zeta potential (−25.2 ± 0.4 mV) met the requirements of the intranasal drug delivery system (nanoDDS) and the targeted profile liquid formulation was transformed into a solid preservative-free product by freeze-drying. The viscosity (32.5 ± 0.28 mPas) and hypotonic osmolality (240 mOsmol/L) of the reconstituted formulation provides proper and enhanced absorption and probably guarantees the administration of the liquid dosage form (nasal drop and spray). The developed formulation resulted in more than 20 times faster MEL dissolution rate and five-fold higher nasal permeability compared to starting MEL. The prediction of IVIVC confirmed the great potential for in vivo brain distribution of MEL. The nose-to-brain delivery of NSAIDs such as MEL by means of nanoDDS as polymeric micelles offers an innovative opportunity to treat neuroinflammation more effectively. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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21 pages, 6763 KiB  
Article
Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy
by Stavroula G. Nanaki, Konstantinos Spyrou, Chryssa Bekiari, Pelagia Veneti, Turki N. Baroud, Niki Karouta, Ioannis Grivas, Georgios C. Papadopoulos, Dimitrios Gournis and Dimitrios N. Bikiaris
Pharmaceutics 2020, 12(3), 227; https://doi.org/10.3390/pharmaceutics12030227 - 04 Mar 2020
Cited by 34 | Viewed by 4491
Abstract
In the present study, poly(l-lactic acid) (PLLA) and poly(lactide-co-glycolide) (PLGA) hybrid nanoparticles were developed for intranasal delivery of galantamine, a drug used in severe to moderate cases of Alzheimer’s disease. Galantamine (GAL) was adsorbed first in hierarchical porous carbon [...] Read more.
In the present study, poly(l-lactic acid) (PLLA) and poly(lactide-co-glycolide) (PLGA) hybrid nanoparticles were developed for intranasal delivery of galantamine, a drug used in severe to moderate cases of Alzheimer’s disease. Galantamine (GAL) was adsorbed first in hierarchical porous carbon (HPC). Formulations were characterized by FT-IR, which showed hydrogen bond formation between GAL and HPC. Furthermore, GAL became amorphous after adsorption, as confirmed by XRD and differential scanning calorimetry (DSC) studies. GAL was quantified to be 21.5% w/w by TGA study. Adsorbed GAL was nanoencapsulated in PLLA and PLGA, and prepared nanoparticles were characterized by several techniques. Their sizes varied between 182 and 394 nm, with an exception that was observed in nanoparticles that were prepared by PLLA and adsorbed GAL that was found to be 1302 nm in size. DSC thermographs showed that GAL was present in its crystalline state in nanoparticles before its adsorption to HPC, while it remained in its amorphous phase after its adsorption in the prepared nanoparticles. It was found that the polymers controlled the release of GAL both when it was encapsulated alone and when it was adsorbed on HPC. Lastly, PLGA hybrid nanoparticles were intranasally-administered in healthy, adult, male Wistar rats. Administration led to successful delivery to the hippocampus, the brain area that is primarily and severely harmed in Alzheimer’s disease, just a few hours after a single dose. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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22 pages, 3653 KiB  
Article
Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach
by Gábor Katona, György Tibor Balogh, Gergő Dargó, Róbert Gáspár, Árpád Márki, Eszter Ducza, Anita Sztojkov-Ivanov, Ferenc Tömösi, Gábor Kecskeméti, Tamás Janáky, Tamás Kiss, Rita Ambrus, Edina Pallagi, Piroska Szabó-Révész and Ildikó Csóka
Pharmaceutics 2020, 12(2), 97; https://doi.org/10.3390/pharmaceutics12020097 - 25 Jan 2020
Cited by 31 | Viewed by 4608
Abstract
The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various [...] Read more.
The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various properties, such as the Z-average, zeta potential, encapsulation efficacy (EE), conjugation of MEL and HSA, physical stability, in vitro dissolution, in vitro permeability, and in vivo plasma and brain distribution of MEL were characterized. From a stability point of view, a solid product (Mel-HSA-Tween) is recommended for further development since it met the desired critical parameters (176 ± 0.3 nm Z-average, 0.205 ± 0.01 PdI, −14.1 ± 0.7 mV zeta potential) after 6 months of storage. In vitro examination showed a significantly increased drug dissolution and permeability of MEL-containing nanoparticles, especially in the case of applying Tween 80. The in vivo studies confirmed both the trans-epithelial and axonal transport of nanoparticles, and a significantly higher cerebral concentration of MEL was detected with nose-to-brain delivery, in comparison with intravenous or per os administration. These results indicate intranasal the administration of optimized MEL-containing HSA formulations as a potentially applicable “value-added” product for the treatment of neuroinflammation. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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14 pages, 1418 KiB  
Article
Comparison of Various Cell Lines and Three-Dimensional Mucociliary Tissue Model Systems to Estimate Drug Permeability Using an In Vitro Transport Study to Predict Nasal Drug Absorption in Rats
by Tomoyuki Furubayashi, Daisuke Inoue, Noriko Nishiyama, Akiko Tanaka, Reiko Yutani, Shunsuke Kimura, Hidemasa Katsumi, Akira Yamamoto and Toshiyasu Sakane
Pharmaceutics 2020, 12(1), 79; https://doi.org/10.3390/pharmaceutics12010079 - 17 Jan 2020
Cited by 48 | Viewed by 4666
Abstract
Recently, various types of cultured cells have been used to research the mechanisms of transport and metabolism of drugs. Although many studies using cultured cell systems have been published, a comparison of different cultured cell systems has never been reported. In this study, [...] Read more.
Recently, various types of cultured cells have been used to research the mechanisms of transport and metabolism of drugs. Although many studies using cultured cell systems have been published, a comparison of different cultured cell systems has never been reported. In this study, Caco-2, Calu-3, Madin–Darby canine kidney (MDCK), EpiAirway and MucilAir were used as popular in vitro cell culture systems, and the permeability of model compounds across these cell systems was evaluated to compare barrier characteristics and to clarify their usefulness as an estimation system for nasal drug absorption in rats. MDCK unexpectedly showed the best correlation (r = 0.949) with the fractional absorption (Fn) in rats. Secondly, a high correlation was observed in Calu-3 (r = 0.898). Also, Caco-2 (r = 0.787) and MucilAir (r = 0.750) showed a relatively good correlation with Fn. The correlation between Fn and permeability to EpiAirway was the poorest (r = 0.550). Because EpiAirway forms leakier tight junctions than other cell culture systems, the paracellular permeability was likely overestimated with this system. On the other hand, because MDCK formed such tight cellular junctions that compounds of paracellular model were less likely permeated, the paracellular permeability could be underestimated. Calu-3, Caco-2 and MucilAir form suitable cellular junctions and barriers, indicating that those cell systems enable the precise estimation of nasal drug absorption. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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15 pages, 1504 KiB  
Article
Therapeutic Effects in a Transient Middle Cerebral Artery Occlusion Rat Model by Nose-To-Brain Delivery of Anti-TNF-Alpha siRNA with Cell-Penetrating Peptide-Modified Polymer Micelles
by Takanori Kanazawa, Takumi Kurano, Hisako Ibaraki, Yuuki Takashima, Toyofumi Suzuki and Yasuo Seta
Pharmaceutics 2019, 11(9), 478; https://doi.org/10.3390/pharmaceutics11090478 - 15 Sep 2019
Cited by 35 | Viewed by 4602 | Correction
Abstract
We previously reported that siRNA delivery to the brain is improved by the nose-to-brain delivery route and by conjugation with polyethylene glycol-polycaprolactone (PEG-PCL) polymer micelles and the cell-penetrating peptide, Tat (PEG-PCL-Tat). In this study, we evaluated the nose-to-brain delivery of siRNA targeting TNF-α [...] Read more.
We previously reported that siRNA delivery to the brain is improved by the nose-to-brain delivery route and by conjugation with polyethylene glycol-polycaprolactone (PEG-PCL) polymer micelles and the cell-penetrating peptide, Tat (PEG-PCL-Tat). In this study, we evaluated the nose-to-brain delivery of siRNA targeting TNF-α (siTNF-α) conjugated with PEG-PCL-Tat to investigate its therapeutic effects on a transient middle cerebral artery occlusion (t-MCAO) rat model of cerebral ischemia-reperfusion injury. Intranasal treatment was provided 30 min after infarction induced via suturing. Two hours after infarction induction, the suture was removed, and blood flow was released. At 22 h post-reperfusion, we assessed the infarcted area, TNF-α production, and neurological score to determine the therapeutic effects. The infarcted area was observed over a wide range in the untreated group, whereas shrinkage of the infarcted area was observed in rats subjected to intranasal administration of siTNF-α with PEG-PCL-Tat micelles. Moreover, TNF-α production and neurological score in rats treated by intranasal administration of siTNF-α with PEG-PCL-Tat micelles were significantly lower than those in untreated and naked siTNF-α-treated rats. These results indicate that nose-to-brain delivery of siTNF-α conjugated with PEG-PCL-Tat micelles alleviated the symptoms of cerebral ischemia-reperfusion injury. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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12 pages, 2311 KiB  
Article
Ex-Vivo and In-Vivo Assessment of Cyclamen europaeum Extract After Nasal Administration
by Francisco Fernández-Campos, Beatriz Clares, María J Rodríguez-Lagunas, Olga Jauregui, Isidre Casals and Ana C Calpena
Pharmaceutics 2019, 11(9), 426; https://doi.org/10.3390/pharmaceutics11090426 - 21 Aug 2019
Cited by 6 | Viewed by 3194
Abstract
Rhinosinusitis is a prevalent disorder with a severe impact on the health-related quality of life. Saponins of Cyclamen europaeum exert a clinically proven curative effect on rhinosinusitis symptoms when instilled into the nasal cavity, however, more extensive preclinical assessment is required to better [...] Read more.
Rhinosinusitis is a prevalent disorder with a severe impact on the health-related quality of life. Saponins of Cyclamen europaeum exert a clinically proven curative effect on rhinosinusitis symptoms when instilled into the nasal cavity, however, more extensive preclinical assessment is required to better characterize the efficacy of this botanical extract. This work evaluates the potential use of a natural freeze-dried extract of C. europaeum given as topical nasal administration. Permeation experiment on porcine nasal mucosa was performed with Franz diffusion cells. Experiments in rabbits were performed to test for any toxicological, hematological, biochemical or histological evidence of systemic action. No theoretical levels of saponins were found in the receptor chamber of Franz diffusion cells. Hematological data did not show significant differences between control and experimental animals (p > 0.05). Histological studies also showed that enhanced secretory activity in response to intranasal administration was not accompanied by any visible signs of injury. An examination of the brain, lungs, liver, kidneys, spleen, and gastrointestinal organs did not reveal any abnormality. The absence of mucosal permeation of saponins and negligible probability of C. europaeum saponins absorption in the course of a therapeutic application was demonstrated. Full article
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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