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Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials

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A special issue of Materials (ISSN 1996-1944).

Deadline for manuscript submissions: closed (20 February 2019) | Viewed by 18715

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Special Issue Editor

Dr. Donato Cosco

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Guest Editor

Department of Health Sciences, University "Magna Graecia" of Catanzaro, Campus "S. Venuta", Building of BioSciences, I-88100 Catanzaro, Italy
Interests: drug delivery; liposomes; pharmaceutical technology; polymeric micro/nanoparticles; selective targeting
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

As you are aware, the use of biocompatible materials noticeably modulates the physico-chemical, biopharmaceutical, and pharmacological properties of many active compounds. In particular, the encapsulation/complexation of drugs using biodegradable delivery systems, made up of phospholipids, polymers, polysaccharides, proteins, etc., represents a suitable approach that is able to increase their therapeutic efficacy and decrease their side effects. The lack of toxicity of the aforementioned formulations favours their application through various administration routes, obtaining a significant increase of the half-life of the delivered compound(s).

Moreover, the opportunity of promoting the localization of drugs in specific tissues is another feature of biomaterial-based drug carriers obtained by passive and active targeting approaches as a function of their composition and surface characteristics.

The aim of this Special Issue is to describe the advancements concerning the development of innovative biocompatible formulations for pharmaceutical applications.

All researchers working in the field are cordially invited to contribute. Original research papers, brief communication reports, and review articles are all welcome.

Prof. Dr. Cosco Donato
Guest Editor

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. Materials is an international peer-reviewed open access semimonthly 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 2600 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

self-assembling biosystems
phospholipids
biopolymers
(poly)saccharides
colloidal structures
microparticulates
drug delivery

Published Papers (5 papers)

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Research

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15 pages, 2589 KiB

Open AccessFeature PaperArticle

Unsaturated Poly(Hydroxyalkanoates) for the Production of Nanoparticles and the Effect of Cross-Linking on Nanoparticle Features

by Rosario Pignatello, Giuseppe Impallomeni, Sarha Cupri, Giuseppe Puzzo, Claudia Curcio, Maria Giovanna Rizzo, Salvatore Guglielmino and Alberto Ballistreri

Materials 2019, 12(6), 868; https://doi.org/10.3390/ma12060868 - 15 Mar 2019

Cited by 11 | Viewed by 2380

Abstract

A biodegradable poly(3-R-hydroxyalkanoate) synthesized by Pseudomonas mediterranea was investigated as a biomaterial to obtain colloidal drug delivery systems. Using a nanoprecipitation method, nanoparticles with a mean size of 155 nm and a negative surface charge were formed. They can be freeze-dried by adding hydroxypropyl-β-cyclodextrin as a cryoprotectant, and they have been shown to efficiently load both a hydrophilic (calcein) and a lipophilic (Nile red) model probe. Since this polymer contains terminal double bonds in the side chains, cross-linking conditions were tested. In particular, under the action of UV rays or irradiation with an incandescent yellow lamp, this polymer tended to cross-link. Full article

(This article belongs to the Special Issue Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials)

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Graphical abstract

20 pages, 4051 KiB

Open AccessArticle

Surface Modification of Liposomes by a Lipopolymer Targeting Prostate Specific Membrane Antigen for Theranostic Delivery in Prostate Cancer

by Hooman Yari, Gregory Nkepang and Vibhudutta Awasthi

Materials 2019, 12(5), 756; https://doi.org/10.3390/ma12050756 - 05 Mar 2019

Cited by 29 | Viewed by 3628

Abstract

Prostate specific membrane antigen (PSMA) is a marker for diagnosis and targeted delivery of therapeutics to advanced/metastasized prostate cancer. We report a liposome-based system for theranostic delivery to PSMA-expressing (PSMA⁺) LNCaP cells. A lipopolymer (P³) comprising of PSMA ligand (PSMAL), polyethylene glycol (PEG₂₀₀₀), and palmitate was synthesized and post-inserted into the surface of preformed liposomes. These P³-liposomes were loaded with doxorubicin and radiolabeled with ^99mTc radionuclide to study their theranostic characteristics. Differential expression of PSMA on LNCaP and PC3 cells was confirmed by immunoblotting as well as by uptake of PSMAL labeled with ¹⁸F radionuclide. We found that the uptake of ^99mTc-labeled P³-liposomes by LNCaP cells was >3-fold higher than ^99mTc-labeled Plain-liposomes; the amount of doxorubicin delivered to LNCaP cells was also found to be >3-fold higher by P³-liposomes. Cell-based cytotoxicity assay results showed that doxorubicin-loaded P³-liposomes were significantly more toxic to LNCaP cells (p < 0.05), but not to PSMA-negative PC3 cells. Compared to doxorubicin-loaded Plain-liposomes, the IC₅₀ value of doxorubicin-loaded P³-liposomes was reduced by ~5-fold in LNCaP cells. Together, these results suggest that surface functionalization of liposomes with small PSMA-binding motifs, such as PSMAL, can provide a viable platform for specific delivery of theranostics to PSMA⁺ prostate cancer. Full article

(This article belongs to the Special Issue Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials)

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23 pages, 2572 KiB

Open AccessFeature PaperArticle

Mathematical Models as Tools to Predict the Release Kinetic of Fluorescein from Lyotropic Colloidal Liquid Crystals

by Donatella Paolino, Andra Tudose, Christian Celia, Luisa Di Marzio, Felisa Cilurzo and Constantin Mircioiu

Materials 2019, 12(5), 693; https://doi.org/10.3390/ma12050693 - 26 Feb 2019

Cited by 51 | Viewed by 3683

Abstract

In this study, we investigated the release kinetic of fluorescein from colloidal liquid crystals made from monoglyceride and different non-ionic surfactants. The crystals were physicochemically characterized and the release experiments were carried out under the sink conditions, while mathematical models were described as extrapolations from solutions of the diffusion equation, in different initial and boundary conditions imposed by pharmaceutical formulations. The diffusion equation was solved using Laplace and Fourier transformed functions for release kinetics from infinite reservoirs in a semi-infinite medium. Solutions represents a general square root law and can be applied for the release kinetic of fluorescein from lyotropic colloidal liquid crystals. Akaike, Schwartz, and Imbimbo criteria were used to establish the appropriate mathematical model and the hierarchy of the performances of different models applied to the release experiments. The Fisher statistic test was applied to obtain the significance of differences among mathematical models. Differences of mathematical criteria demonstrated that small or no significant statistic differences were carried out between the various applied models and colloidal formulations. Phenomenological models were preferred over the empirical and semi-empirical ones. The general square root model shows that the diffusion-controlled release of fluorescein is the mathematical models extrapolated for lyotropic colloidal liquid crystals. Full article

(This article belongs to the Special Issue Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials)

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Graphical abstract

11 pages, 1380 KiB

Open AccessArticle

PLA-PEG Nanoparticles Improve the Anti-Inflammatory Effect of Rosiglitazone on Macrophages by Enhancing Drug Uptake Compared to Free Rosiglitazone

by Giovanna Giacalone, Nicolas Tsapis, Ludivine Mousnier, Hélène Chacun and Elias Fattal

Materials 2018, 11(10), 1845; https://doi.org/10.3390/ma11101845 - 27 Sep 2018

Cited by 24 | Viewed by 3343

Abstract

Among cardiovascular diseases, atherosclerosis remains the first cause of death in the United States of America and Europe, as it leads to myocardial infarction or stroke. The high prevalence of heart diseases is due to the difficulty in diagnosing atherosclerosis, since it can develop for decades before symptoms occur, and to the complexity of the treatment since targets are also important components of the host defenses. The antidiabetics thiazolidinediones, among which is rosiglitazone (RSG), have demonstrated anti-atherosclerotic effect in animal models, and are therefore promising candidates for the improvement of atherosclerosis management. Nevertheless, their administration is hindered by the insurgence of severe side effects. To overcome this limitation, rosiglitazone has been encapsulated into polymeric nanoparticles, which permit efficient delivery to its nuclear target, and selective delivery to the site of action, allowing the reduction of unwanted effects. In the present work, we describe nanoparticle formulation using polylactic acid (PLA) coupled to polyethylene glycol (PEG), their characterization, and their behavior on RAW264.7 macrophages, an important target in atherosclerosis treatment. RSG nanocarriers showed no toxicity on cells at all concentrations tested, an anti-inflammatory effect in a dose-dependent manner, up to 5 times more efficient than the free molecule, and an increased RSG uptake which is consistent with the effect shown. These biodegradable nanoparticles represent a valid tool to be further investigated for the treatment of atherosclerosis. Full article

(This article belongs to the Special Issue Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials)

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Review

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16 pages, 1471 KiB

Open AccessReview

Antileishmanial Activity of Amphotericin B-loaded-PLGA Nanoparticles: An Overview

by Ernesto Palma, Antonella Pasqua, Agnese Gagliardi, Domenico Britti, Massimo Fresta and Donato Cosco

Materials 2018, 11(7), 1167; https://doi.org/10.3390/ma11071167 - 09 Jul 2018

Cited by 38 | Viewed by 5122

Abstract

In recent decades, nanotechnology has made phenomenal strides in the pharmaceutical field, favouring the improvement of the biopharmaceutical properties of many active compounds. Many liposome-based formulations containing antitumor, antioxidant and antifungal compounds are presently on the market and are used daily (for example Doxil^®/Caelyx^® and Ambisome^®). Polymeric nanoparticles have also been used to entrap many active compounds with the aim of improving their pharmacological activity, bioavailability and plasmatic half-life while decreasing their side effects. The modulation of the structural/morphological properties of nanoparticles allows us to influence various technological parameters, such as the loading capacity and/or the release profile of the encapsulated drug(s). Amongst the biocompatible polymers, poly(D,L-lactide) (PLA), poly(D,L-glycolide) (PLG) and their co-polymers poly(lactide-co-glycolide) (PLGA) are the most frequently employed due to their approval by the FDA for human use. The aim of this review is to provide a description of the foremost recent investigations based on the encapsulation of amphotericin B in PLGA nanoparticles, in order to furnish an overview of the technological properties of novel colloidal formulations useful in the treatment of Leishmaniasis. The pharmacological efficacy of the drug after nanoencapsulation will be compared to the commercial formulations of the drug (i.e., Fungizone^®, Ambisome^®, Amphocil^® and Abelcet^®). Full article

(This article belongs to the Special Issue Modulation of Physico-chemical and Therapeutic Features of Drugs by Biocompatible Materials)

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