Special Issue "Functional Polymers for Controlled Drug Release"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: 31 July 2019

Special Issue Editor

Guest Editor
Prof. Umile Gianfranco Spizzirri

University of Calabria, Department of Pharmacy, Health and Nutritional Sciences, Cosenza, Italy
E-Mail
Interests: stimuli-responsive drug delivery systems, munti-functional hydrogels, antioxidant polymers

Special Issue Information

Dear Colleagues,

In the last decade, high-performing functional polymers for specific uses, including stimuli-responsive materials, molecularly imprinted polymers, mucoadhesive materials, carriers for the delivery of high MW drugs, and gene-delivery have emerged as one of the most significant trends in the area of nanotechnology. In this regard, polymeric devices that are able to undergo morphological modifications in response to an external stimulus (pH, redox balance, temperature, magnetic field, and light) represent an innovative field in the delivery of therapeutics. Additionally, in an effort to further improve delivery device performance, a combination of two or more signals have recently been developed by incorporating different stimulus responsive elements into the same polymeric network with the aim to improve the situ-controlled delivery of bioactive compounds. These smart polymeric materials lead to superior in vitro and/or in vivo therapeutic efficacy, with programmed site-specific features and remarkable potential for targeted therapy. Specifically, the correlation between the physical features and the situ-controlled delivery of bioactive compounds represents an important aspect worthy of investigation. This Special Issue welcomes any topics regarding recent progress in the synthesis and characterization of innovative functional polymers suitable to be employed as drug carriers in the pharmaceutical and biomedical fields.

Prof. Umile Gianfranco Spizzirri
Guest Editor

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Keywords

  • Functional polymer
  • Drug delivery
  • External stimulus
  • Site-specific release

Published Papers (3 papers)

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Research

Open AccessArticle
Use of nPSi-βCD Composite Microparticles for the Controlled Release of Caffeic Acid and Pinocembrin, Two Main Polyphenolic Compounds Found in a Chilean Propolis
Pharmaceutics 2019, 11(6), 289; https://doi.org/10.3390/pharmaceutics11060289
Received: 13 May 2019 / Revised: 14 June 2019 / Accepted: 17 June 2019 / Published: 19 June 2019
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Abstract
Propolis is widely recognized for its various therapeutic properties. These are attributed to its rich composition in polyphenols, which exhibit multiple biological properties (e.g., antioxidant, anti-inflammatory, anti-angiogenic). Despite its multiple benefits, oral administration of polyphenols results in low bioavailability at the action site. [...] Read more.
Propolis is widely recognized for its various therapeutic properties. These are attributed to its rich composition in polyphenols, which exhibit multiple biological properties (e.g., antioxidant, anti-inflammatory, anti-angiogenic). Despite its multiple benefits, oral administration of polyphenols results in low bioavailability at the action site. An alternative to face this problem is the use of biomaterials at nano-micro scale due to its high versatility as carriers and delivery systems of various drugs and biomolecules. The aim of this work is to determine if nPSi-βCD microparticles are a suitable material for the load and controlled release of caffeic acid (CA) and pinocembrin (Pin), two of the main components of a Chilean propolis with anti-atherogenic and anti-angiogenic activity. Polyphenols and nPSi-βCD microparticles cytocompatibility studies were carried out with human umbilical vein endothelial cells (HUVECs). Results from physicochemical characterization demonstrated nPSi-βCD microparticles successfully retained and controlled release CA and Pin. Furthermore, nPSi-βCD microparticles presented cytocompatibility with HUVECs culture at concentrations of 0.25 mg/mL. These results suggest that nPSi-βCD microparticles could safely be used as an alternate oral delivery system to improve controlled release and bioavailability of CA or Pin—and eventually other polyphenols—thus enhancing its therapeutic effect for the treatment of different diseases. Full article
(This article belongs to the Special Issue Functional Polymers for Controlled Drug Release)
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Open AccessArticle
Thermally-Responsive Loading and Release of Elastin-Like Polypeptides from Contact Lenses
Pharmaceutics 2019, 11(5), 221; https://doi.org/10.3390/pharmaceutics11050221
Received: 25 March 2019 / Revised: 20 April 2019 / Accepted: 24 April 2019 / Published: 7 May 2019
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Abstract
Contact lenses are widely prescribed for vision correction, and as such they are an attractive platform for drug delivery to the anterior segment of the eye. This manuscript explores a novel strategy to drive the reversible adsorption of peptide-based therapeutics using commercially available [...] Read more.
Contact lenses are widely prescribed for vision correction, and as such they are an attractive platform for drug delivery to the anterior segment of the eye. This manuscript explores a novel strategy to drive the reversible adsorption of peptide-based therapeutics using commercially available contact lenses. To accomplish this, thermo-sensitive elastin-like polypeptides (ELPs) alone or tagged with a candidate ocular therapeutic were characterized. For the first time, this manuscript demonstrates that Proclear CompatiblesTM contact lenses are a suitable platform for ELP adsorption. Two rhodamine-labelled ELPs, V96 (thermo-sensitive) and S96 (thermo-insensitive), were employed to test temperature-dependent association to the contact lenses. During long-term release into solution, ELP coacervation significantly modulated the release profile whereby more than 80% of loaded V96 retained with a terminal half-life of ~4 months, which was only 1–4 days under solubilizing conditions. A selected ocular therapeutic candidate lacritin-V96 fusion (LV96), either free or lens-bound LV96, was successfully transferred to HCE-T cells. These data suggest that ELPs may be useful to control loading or release from certain formulations of contact lenses and present a potential for this platform to deliver a biologically active peptide to the ocular surface via contact lenses. Full article
(This article belongs to the Special Issue Functional Polymers for Controlled Drug Release)
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Graphical abstract

Open AccessArticle
Modulation of the Release of a Non-Interacting Low Solubility Drug from Chitosan Pellets Using Different Pellet Size, Composition and Numerical Optimization
Pharmaceutics 2019, 11(4), 175; https://doi.org/10.3390/pharmaceutics11040175
Received: 22 February 2019 / Revised: 6 April 2019 / Accepted: 8 April 2019 / Published: 10 April 2019
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Abstract
Two size classes of piroxicam (PXC) pellets (mini (380–550 μm) and conventional (700–1200 μm)) were prepared using extrusion/spheronization and medium viscosity chitosan (CHS). Mixture experimental design and numerical optimization were applied to distinguish formulations producing high sphericity pellets with fast or extended release. [...] Read more.
Two size classes of piroxicam (PXC) pellets (mini (380–550 μm) and conventional (700–1200 μm)) were prepared using extrusion/spheronization and medium viscosity chitosan (CHS). Mixture experimental design and numerical optimization were applied to distinguish formulations producing high sphericity pellets with fast or extended release. High CHS content required greater wetting liquid volume for pellet formation and the diameter decreased linearly with volume. Sphericity increased with CHS for low-to-medium drug content. Application of PXRD showed that the drug was a mixture of form II and I. Crystallinity decreased due to processing and was significant at 5% drug content. Raman spectroscopy showed no interactions. At pH 1.2, the dissolved CHS increased ‘apparent’ drug solubility up to 0.24 mg/mL while, at pH 5.6, the suspended CHS increased ‘apparent’ solubility to 0.16 mg/mL. Release at pH 1.2 was fast for formulations with intermediate CHS and drug levels. At pH 5.6, conventional pellets showed incomplete release while mini pellets with a CHS/drug ratio ≥2 and up to 21.25% drug, showed an extended release that was completed within 8 h. Numerical optimization provided optimal formulations for fast release at pH 1.2 with drug levels up to 40% as well as for extended release formulations with drug levels of 5% and 10%. The Weibull model described the release kinetics indicating complex or combined release (parameter ‘b’ > 0.75) for release at pH 1.2, and normal diffusion for the mini pellets at pH 5.6 (‘b’ from 0.63 to 0.73). The above results were attributed mainly to the different pellet sizes and the extensive dissolution/erosion of the gel matrix was observed at pH 1.2 but not at pH 5.6. Full article
(This article belongs to the Special Issue Functional Polymers for Controlled Drug Release)
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Graphical abstract

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