Pharmaceutical Formulations and Bioavailability Enhancement Techniques for Transmucosal Drug Delivery

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

Deadline for manuscript submissions: 30 June 2024 | Viewed by 3215

Special Issue Editors

Laboratory of Pharmaceutical Development (LADEF), Federal University of São João del-Rei, Midwest Campus (Dona Lindu), St. Sebastião Gonçalves Coelho, 400-Chanadour, Divinópolis 35501-296, MG, Brazil
Interests: drug delivery; antioxidants; nutraceuticals; phytotherapics; multivariate statistical analysis; quality-by-design; phytochemicals; cell biology; autophagy; programmed cell death; plant anatomy
Special Issues, Collections and Topics in MDPI journals
Department of Pharmacy, State University of Maringa, Maringa, Brazil
Interests: drug delivery systems; buccal drug administration; smart materials; biopharmaceutics; nanotechnology; biopolymers; biocompatible materials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Efforts to overcome the limitations imposed by the various physiological barriers of the human body in order to reach enhanced treatment outcomes have been challenging scientists worldwide over the last decades.

In this Special Issue of Pharmaceutics, authors from both academic and industrial backgrounds are invited to submit original articles for publication. These should report evidence of preclinical (in silico, in vitro or in vivo) and clinical trials, addressing the promising applications of drug delivery systems and permeation enhancement strategies through the buccal, nasal, ocular, rectal, and vaginal mucosa. Systematic reviews and meta-analyses on related subjects in this field will also be considered for publication.

Prof. Dr. Renê Oliveira Do Couto
Prof. Dr. Marcos Luciano Bruschi
Guest Editors

Manuscript Submission Information

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Keywords

  • drug delivery systems
  • buccal drug administration
  • smart materials
  • biopharmaceutics
  • iontophoresis
  • nanotechnology
  • biopolymers
  • biocompatible Materials
  • dendrimers
  • liposomes
  • phonophoresis
  • oral mucosal absorption
  • mucosal administrations
  • ophthalmic administration
  • nasal administration
  • rectal administration
  • mucoadhesive polymers
  • vaginal administration
  • preclinical drug evaluation

Published Papers (3 papers)

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Research

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14 pages, 16075 KiB  
Article
Intranasal Administration of Mesenchymal Stem Cell-Derived Exosome Alleviates Hypoxic-Ischemic Brain Injury
by Takuma Ikeda, Masahito Kawabori, Yuyuan Zheng, Sho Yamaguchi, Shuho Gotoh, Yo Nakahara, Erika Yoshie and Miki Fujimura
Pharmaceutics 2024, 16(4), 446; https://doi.org/10.3390/pharmaceutics16040446 - 23 Mar 2024
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Abstract
Hypoxic-ischemic brain injury arises from inadequate oxygen delivery to the brain, commonly occurring following cardiac arrest, which lacks effective treatments. Recent studies have demonstrated the therapeutic potential of exosomes released from mesenchymal stem cells. Given the challenge of systemic dilution associated with intravenous [...] Read more.
Hypoxic-ischemic brain injury arises from inadequate oxygen delivery to the brain, commonly occurring following cardiac arrest, which lacks effective treatments. Recent studies have demonstrated the therapeutic potential of exosomes released from mesenchymal stem cells. Given the challenge of systemic dilution associated with intravenous administration, intranasal delivery has emerged as a promising approach. In this study, we investigate the effects of intranasally administered exosomes in an animal model. Exosomes were isolated from the cell supernatants using the ultracentrifugation method. Brain injury was induced in Sprague-Dawley rats through a transient four-vessel occlusion model. Intranasal administration was conducted with 3 × 108 exosome particles in 20 µL of PBS or PBS alone, administered daily for 7 days post-injury. Long-term cognitive behavioral assessments, biodistribution of exosomes, and histological evaluations of apoptosis and neuroinflammation were conducted. Exosomes were primarily detected in the olfactory bulb one hour after intranasal administration, subsequently distributing to the striatum and midbrain. Rats treated with exosomes exhibited substantial improvement in cognitive function up to 28 days after the insult, and demonstrated significantly fewer apoptotic cells along with higher neuronal cell survival in the hippocampus. Exosomes were found to be taken up by microglia, leading to a decrease in the expression of cytotoxic inflammatory markers. Full article
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12 pages, 5080 KiB  
Article
Dynamic Ex Vivo Porcine Eye Model to Measure Ophthalmic Drug Penetration under Simulated Lacrimal Flow
by Geisa N. Barbalho, Manuel A. Falcão, Jefferson M. S. Lopes, Júlia M. Lopes, Jonad L. A. Contarato, Guilherme M. Gelfuso, Marcilio Cunha-Filho and Tais Gratieri
Pharmaceutics 2023, 15(9), 2325; https://doi.org/10.3390/pharmaceutics15092325 - 15 Sep 2023
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Abstract
Animal models are still used in the research and development of ophthalmic drug products, mainly due to the difficulty in simulating natural physiological conditions with in vitro models, as there is a lack of dynamic protection mechanisms. Therefore, developing alternative ophthalmic models that [...] Read more.
Animal models are still used in the research and development of ophthalmic drug products, mainly due to the difficulty in simulating natural physiological conditions with in vitro models, as there is a lack of dynamic protection mechanisms. Therefore, developing alternative ophthalmic models that evaluate drug penetration in the cornea while applying dynamic protection barriers is a contemporary challenge. This study aimed to develop a dynamic ex vivo model using porcine eyes with a simulated lacrimal flow to evaluate the performance of pharmaceutical drug products. A glass donor cell to support a simulated tear flow was designed, optimized, and custom-made. The system was challenged with different formulations (with fluconazole) including excipients with different viscosities (poloxamer 407) and mucoadhesive properties (chitosan). The results were compared to those obtained from a conventional excised cornea model mounted in Franz-type diffusion cells. The dynamic model could differentiate formulations, while the static model did not, overestimating ex vivo drug penetrated amounts. Hence, the dynamic model with simulated tear flow showed to be a simple and promising new alternative method for the drug penetration of ophthalmic formulations that ultimately can reduce the number of animals used in research. Full article
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Review

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28 pages, 2428 KiB  
Review
The Potential of Films as Transmucosal Drug Delivery Systems
by Ana Clara Wada de Carvalho, Natália Floriano Paiva, Isabella Kriunas Demonari, Maíra Peres Ferreira Duarte, Renê Oliveira do Couto, Osvaldo de Freitas and Fabiana Testa Moura de Carvalho Vicentini
Pharmaceutics 2023, 15(11), 2583; https://doi.org/10.3390/pharmaceutics15112583 - 04 Nov 2023
Viewed by 1321
Abstract
Pharmaceutical films are polymeric formulations used as a delivery platform for administration of small and macromolecular drugs for local or systemic action. They can be produced by using synthetic, semi-synthetic, or natural polymers through solvent casting, electrospinning, hot-melt extrusion, and 3D printing methods, [...] Read more.
Pharmaceutical films are polymeric formulations used as a delivery platform for administration of small and macromolecular drugs for local or systemic action. They can be produced by using synthetic, semi-synthetic, or natural polymers through solvent casting, electrospinning, hot-melt extrusion, and 3D printing methods, and depending on the components and the manufacturing methods used, the films allow the modulation of drug release. Moreover, they have advantages that have drawn interest in the development and evaluation of film application on the buccal, nasal, vaginal, and ocular mucosa. This review aims to provide an overview of and critically discuss the use of films as transmucosal drug delivery systems. For this, aspects such as the composition of these formulations, the theories of mucoadhesion, and the methods of production were deeply considered, and an analysis of the main transmucosal pathways for which there are examples of developed films was conducted. All of this allowed us to point out the most relevant characteristics and opportunities that deserve to be taken into account in the use of films as transmucosal drug delivery systems. Full article
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