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Pharmaceutics
Special Issues
Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes
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Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes

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 (15 December 2021) | Viewed by 12747

Special Issue Editors

Dr. Viviana De Caro

E-Mail Website
Guest Editor
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, 90123 Palermo, Italy
Interests: controlled drug release; bio-adhesive buccal delivery systems; sublingual delivery; lipid-micro and nanoparticles; drug absorption from the oral cavity
Special Issues, Collections and Topics in MDPI journals
Dr. Giulia Di Prima

E-Mail Website
Guest Editor
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, 90123 Palermo, Italy
Interests: ex-vivo permeation; oromucosal formulations; ocular administration; nanosystems; drug delivery systems; biopolymers; buccal tablets; microparticles; sublingual patches; dissolution kinetics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In the last decade, interest in the formulation of therapeutic systems suitable for drug administration on the epithelia (buccal, sublingual, cutaneous, ocular, etc.) greatly increased in order to obtain loco-regional or systemic effects, thus overcoming the limits of conventional administration. High molecular weight substances, insoluble drugs, and degradable antioxidant biomolecules represent the greatest challenge to penetration and/or permeation through the epithelia in sufficient amounts needed in order to achieve a therapeutic effect. The synthesis of new polymeric structures as well as the use of biopolymers for the formulation of micro- and nano-systems, solid solutions, and bioerodible sponges can represent such innovative strategies to obtain effective polymer-based systems able to enhance the bioavailability of actives through bioadhesion and bio-interaction with the membranes. This Special Issue will be focused on the accurate design of polymer-based dosage forms able to interact with the biological tissue, promoting drug penetration and/or permeation through the considered biomembrane. This contribution to the expansion of knowledge on new polymeric systems can be of great appeal in the pharmaceutical, cosmetic, and nutraceutical fields.

Prof. Dr. Viviana De Caro
Dr. Giulia Di Prima
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

  • polymers
  • buccal administration
  • sublingual administration
  • ocular administration
  • biomembrane routes
  • loco-regional effect
  • systemic effect
  • bio-adhesion
  • chemical enhancement
  • natural compounds
  • nutraceuticals
  • cosmetics
  • dietary supplements

Published Papers (4 papers)

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Research

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24 pages, 2590 KiB  
Article
Inulin-Based Polymeric Micelles Functionalized with Ocular Permeation Enhancers: Improvement of Dexamethasone Permeation/Penetration through Bovine Corneas
by Giulia Di Prima, Mariano Licciardi, Flavia Bongiovì, Giovanna Pitarresi and Gaetano Giammona
Pharmaceutics 2021, 13(9), 1431; https://doi.org/10.3390/pharmaceutics13091431 - 09 Sep 2021
Cited by 10 | Viewed by 1825
Abstract
Ophthalmic drug delivery is still a challenge due to the protective barriers of the eye. A common strategy to promote drug absorption is the use of ocular permeation enhancers, while an innovative approach is the use of polymeric micelles. In the present work, [...] Read more.
Ophthalmic drug delivery is still a challenge due to the protective barriers of the eye. A common strategy to promote drug absorption is the use of ocular permeation enhancers, while an innovative approach is the use of polymeric micelles. In the present work, the two mentioned approaches were coupled by conjugating ocular permeation enhancers (PEG2000, carnitine, creatine, taurine) to an inulin-based co-polymer (INU-EDA-RA) in order to obtain self-assembling biopolymers with permeation enhancer properties for the hydrophobic drug dexamethasone (DEX). Inulin derivatives were properly synthetized, were found to expose about 2% mol/mol of enhancer molecules in the side chain, and resulted able to self-assemble at various concentrations by varying the pH and the ionic strength of the medium. Moreover, the ability of polymeric micelles to load dexamethasone was demonstrated, and size, mucoadhesiveness, and cytocompatibility against HCE cells were evaluated. Furthermore, the efficacy of the permeation enhancer was evaluated by ex vivo permeation studies to determine the performance of the used enhancers, which resulted in PEG2000 > CAR > TAU > CRE, while entrapment ability studies resulted in CAR > TAU > PEG2000 > CRE, both for fluorescent-labelled and DEX-loaded micelles. Finally, an increase in terms of calculated Kp and Ac parameters was demonstrated, compared with the values calculated for DEX suspension. Full article
(This article belongs to the Special Issue Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes)
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26 pages, 8392 KiB  
Article
Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets
by Giulia Di Prima, Giuseppe Angellotti, Amalia Giulia Scarpaci, Denise Murgia, Fabio D’agostino, Giuseppina Campisi and Viviana De Caro
Pharmaceutics 2021, 13(9), 1370; https://doi.org/10.3390/pharmaceutics13091370 - 31 Aug 2021
Cited by 13 | Viewed by 3123
Abstract
Resveratrol (RSV) is a natural polyphenol with several interesting broad-spectrum pharmacological properties. However, it is characterized by poor oral bioavailability, extensive first-pass effect metabolism and low stability. Indeed, RSV could benefit from the advantage of the sublingual route of administration. In this view, [...] Read more.
Resveratrol (RSV) is a natural polyphenol with several interesting broad-spectrum pharmacological properties. However, it is characterized by poor oral bioavailability, extensive first-pass effect metabolism and low stability. Indeed, RSV could benefit from the advantage of the sublingual route of administration. In this view, RSV attitudes to crossing the porcine sublingual mucosa were evaluated and promoted both by six different chemical permeation enhancers (CPEs) as well as by preparing four innovative fast-disintegrating sublingual mini-tablets by spray drying followed by direct compression. Since RSV by itself exhibits a low permeation aptitude, this could be significantly enhanced by the use of CPEs as well as by embedding RSV in a spray-dried powder to be compressed in order to prepare fast-disintegrating mini-tablets. The most promising observed CPEs (menthol, lysine and urea) were then inserted into the most promising spray-dried excipients’ compositions (RSV-B and RSV-C), thus preparing CPE-loaded mini-tablets. However, this procedure leads to unsatisfactory results which preclude the possibility of merging the two proposed approaches. Finally, the best spray-dried composition (RSV-B) was further evaluated by SEM, FTIR, XRD and disintegration as well as dissolution behavior to prove its effectiveness as a sublingual fast-disintegrating formulation. Full article
(This article belongs to the Special Issue Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes)
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21 pages, 3139 KiB  
Article
Solid and Semisolid Innovative Formulations Containing Miconazole-Loaded Solid Lipid Microparticles to Promote Drug Entrapment into the Buccal Mucosa
by Viviana De Caro, Libero Italo Giannola and Giulia Di Prima
Pharmaceutics 2021, 13(9), 1361; https://doi.org/10.3390/pharmaceutics13091361 - 29 Aug 2021
Cited by 11 | Viewed by 2071
Abstract
The currently available antifungal therapy for oral candidiasis (OC) has various limitations restricting its clinical use, such as short retention time, suboptimal drug concentration and low patients compliance. These issues could be overcome using micro or nanotechnology. In particular, solid lipid microparticles (SLMs) [...] Read more.
The currently available antifungal therapy for oral candidiasis (OC) has various limitations restricting its clinical use, such as short retention time, suboptimal drug concentration and low patients compliance. These issues could be overcome using micro or nanotechnology. In particular, solid lipid microparticles (SLMs) resulted as a particularly promising penetration enhancer carrier for lipophilic drugs, such as the antifungal miconazole (MCZ). Based on these considerations, cetyl decanoate (here synthesized without the use of metal catalysis) was employed together with 1-hexadecanol to prepare MCZ-loaded SLMs. These resulted in a powder composed of 45–300 µm diameter solid spherical particles, able to load a high amount of MCZ in the amorphous form and characterized by a melting temperature range perfectly compatible with oromucosal administration (35–37 °C). Moreover, when compared to Daktarin® 2% oral gel in ex vivo experiments, SLMs were able to increase up to three-fold MCZ accumulation into the porcine buccal mucosa. The prepared SLMs were then loaded into a buccal gel or a microcomposite mucoadhesive buccal film and evaluated in terms of MCZ permeation and/or accumulation into porcine buccal mucosa by using lower doses than the conventional dosage form. The promising results obtained highlighted an enhancement in terms of MCZ accumulation even at low doses. Furthermore, the prepared buccal film was eligible as stable, reproducible and also highly mucoadhesive. Therefore, the formulated SLMs represent a penetration enhancer vehicle suitable to reduce the dose of lipophilic drugs to be administered to achieve the desired therapeutic effects, as well as being able to be effectively embedded into easily administrable solid or semisolid dosage forms. Full article
(This article belongs to the Special Issue Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes)
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Review

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20 pages, 1954 KiB  
Review
Polymeric Implants for the Treatment of Intraocular Eye Diseases: Trends in Biodegradable and Non-Biodegradable Materials
by Paulina García-Estrada, Miguel A. García-Bon, Edgar J. López-Naranjo, Dulce N. Basaldúa-Pérez, Arturo Santos and Jose Navarro-Partida
Pharmaceutics 2021, 13(5), 701; https://doi.org/10.3390/pharmaceutics13050701 - 12 May 2021
Cited by 32 | Viewed by 5053
Abstract
Intraocular/Intravitreal implants constitute a relatively new method to treat eye diseases successfully due to the possibility of releasing drugs in a controlled and prolonged way. This particularity has made this kind of method preferred over other methods such as intravitreal injections or eye [...] Read more.
Intraocular/Intravitreal implants constitute a relatively new method to treat eye diseases successfully due to the possibility of releasing drugs in a controlled and prolonged way. This particularity has made this kind of method preferred over other methods such as intravitreal injections or eye drops. However, there are some risks and complications associated with the use of eye implants, the body response being the most important. Therefore, material selection is a crucial factor to be considered for patient care since implant acceptance is closely related to the physical and chemical properties of the material from which the device is made. In this regard, there are two major categories of materials used in the development of eye implants: non-biodegradables and biodegradables. Although non-biodegradable implants are able to work as drug reservoirs, their surgical requirements make them uncomfortable and invasive for the patient and may put the eyeball at risk. Therefore, it would be expected that the human body responds better when treated with biodegradable implants due to their inherent nature and fewer surgical concerns. Thus, this review provides a summary and discussion of the most common non-biodegradable and biodegradable materials employed for the development of experimental and commercially available ocular delivery implants. Full article
(This article belongs to the Special Issue Polymeric Systems to Enhance Drug Penetration and/or Permeation through Biomembranes)
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