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Pharmaceutics
Special Issues
Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers
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Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers

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

Deadline for manuscript submissions: closed (31 January 2020) | Viewed by 16166

Special Issue Editors

Prof. Dr. Andrea Cappelli

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Guest Editor
Dipartimento di Biotecnologie, Chimica e Farmacia (Dipartimento di Eccellenza 2018-2022), Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy
Interests: polymeric materials; drug delivery systems; dendrimers; drug discovery; protein derivatization
Dr. Marco Paolino

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Guest Editor
University of Siena (Italy), Dipartimento di Biotecnologia, Chimica e Farmacia
Interests: polymeric materials; drug delivery systems; dendrimers; drug discovery; protein derivatization

Special Issue Information

Dear Colleagues,

Micro- and nanopolymeric materials of natural or synthetic origin are taking more and more space in the preparation of numerous innovative drug delivery systems. Physical and chemical properties affect the release mechanisms. In fact, in the design of new DDSs, much importance should be given to size and shape of the particles, to the modulation of aggregation phenomena, and to the hydrophobic/lipophilic balance. In addition, surface charge features may influence drug/polymer interactions or even DDS interactions with biological systems (i.e., interactions with serum proteins, cell membranes, or target compartments). Furthermore, optical, radioactive, or magnetic properties can play important roles in the traceability of polymeric materials; thus, structures showing light emission or radioactive properties could be considered in the DDS design in order to facilitate the evaluation of the stability, biodistribution, and excretion. The important role of these parameters in the success of a DDS is sometimes eclipsed by its effectiveness; therefore, in this Special Issue, we want to collect a series of articles in which the study of the physicochemical properties becomes the basis for the design of innovative systems for controlled release.

Prof. Andrea Cappelli
Dr. Marco Paolino
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

  • Aggregation
  • Solubility
  • Z-potential
  • Size
  • Shape
  • Optical properties
  • Imaging properties
  • Magnetic properties
  • Drug–polymer interaction
  • Polymer–membrane interaction
  • Biodistribution
  • Structure–property relationships

Published Papers (5 papers)

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Research

20 pages, 3717 KiB  
Article
Long-Acting Paliperidone Parenteral Formulations Based on Polycaprolactone Nanoparticles; the Influence of Stabilizer and Chitosan on In Vitro Release, Protein Adsorption, and Cytotoxicity
by Mohammed Elmowafy, Nabil K. Alruwaili, Khaled Shalaby, Khalid S. Alharbi, Waleed M. Altowayan, Naveed Ahmad, Ameeduzzafar Zafar and Mohammed Elkomy
Pharmaceutics 2020, 12(2), 160; https://doi.org/10.3390/pharmaceutics12020160 - 16 Feb 2020
Cited by 25 | Viewed by 3885
Abstract
Long-acting preparations containing the antipsychotic paliperidone for intramuscular injection has drawn considerable attention to achieve harmless long-term treatment. This study aimed to develop paliperidone loaded polycaprolactone (PCL) nanoparticles and investigate the influence of PCL/drug ratio, stabilizer type, and chitosan coating on physicochemical properties, [...] Read more.
Long-acting preparations containing the antipsychotic paliperidone for intramuscular injection has drawn considerable attention to achieve harmless long-term treatment. This study aimed to develop paliperidone loaded polycaprolactone (PCL) nanoparticles and investigate the influence of PCL/drug ratio, stabilizer type, and chitosan coating on physicochemical properties, protein adsorption, and cellular toxicity. Results showed that chitosan coating produced enlarged particle sizes, shifted the surface charges from negative into positive and did not influence encapsulation efficiencies. Chitosan coating relatively sustained the drug release especially in pluronic stabilized formulations. Pluronic F127 based formulations exhibited the least protein adsorption (384.3 μg/mL). Chitosan coating of Tween 80 and polyvinyl alcohol stabilized formulations significantly (p < 0.05) increased protein adsorption. Cellular viability was concentration-dependent and negatively affected by stabilizers. All formulations did not show cellular death at 1.56 μg/mL. Inflammatory responses and oxidative stress were less affected by Tween 80 compared with other stabilizers. Chitosan minimized all aspects of cellular toxicity. Collectively, stabilizer type and chitosan coating play critical roles in developing safe and effective long-acting PCL nanoparticles intended for parenteral drug delivery. The coated formulations containing Tween 80 and Pluronic F127 as stabilizers are warranted a future in vivo study to delineate its safety and efficacy profiles. Full article
(This article belongs to the Special Issue Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers)
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14 pages, 3376 KiB  
Article
Treating Intracranial Abscesses in Rats with Stereotactic Injection of Biodegradable Vancomycin-Embedded Microparticles
by Yuan-Yun Tseng, Ching-Wei Kao, Kuo-Sheng Liu, Ya-Ling Tang, Yen-Wei Liu and Shih-Jung Liu
Pharmaceutics 2020, 12(2), 91; https://doi.org/10.3390/pharmaceutics12020091 - 22 Jan 2020
Cited by 6 | Viewed by 2544
Abstract
Brain abscesses are emergent and life-threating despite advances in modern neurosurgical techniques and antibiotics. The present study explores the efficacy of vancomycin embedded to 50:50 poly(lactic-co-glycolide acid) (PLGA) microparticles in the treatment of brain abscess. The vancomycin embedded microparticles (VMPs) were [...] Read more.
Brain abscesses are emergent and life-threating despite advances in modern neurosurgical techniques and antibiotics. The present study explores the efficacy of vancomycin embedded to 50:50 poly(lactic-co-glycolide acid) (PLGA) microparticles in the treatment of brain abscess. The vancomycin embedded microparticles (VMPs) were stereotactically introduced into the cerebral parenchyma in Staphylococcus aureus bacteria- induced brain abscess-bearing rats. Experimental rats were divided into three groups: group A (n = 13; no treatment), group B (n = 14; daily vancomycin injection (5 mg intraperitoneally), and group C (n = 12; stereotactic introduction of VMPs into the abscess cavity). Group C exhibited no inflammatory response and significantly increased survival and reduced mean abscess volumes (p <0.001) at the eighth week, compared with other groups. Vancomycin delivery via a biodegradable PLGA vehicle can easily attain Area Under the Curve (AUC)/minimum inhibitory concentration (MIC) ratios of ≥400, and strengthens the therapeutic efficacy of antibiotics without provoking any potential toxicity. Biodegradable VMPs are a safe and sustainable drug delivery vehicle for the treatment of brain abscess. Full article
(This article belongs to the Special Issue Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers)
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20 pages, 4224 KiB  
Article
Hyaluronan Graft Copolymers Bearing Fatty-Acid Residues as Self-Assembling Nanoparticles for Olanzapine Delivery
by Marco Paolino, Mariano Licciardi, Cristina Savoca, Gaetano Giammona, Laura Modica De Mohac, Annalisa Reale, Germano Giuliani, Hartmut Komber, Alessandro Donati, Gemma Leone, Agnese Magnani, Maurizio Anzini and Andrea Cappelli
Pharmaceutics 2019, 11(12), 675; https://doi.org/10.3390/pharmaceutics11120675 - 12 Dec 2019
Cited by 9 | Viewed by 3839
Abstract
In order to evaluate the potential of a technology platform based on hyaluronan copolymers grafted with propargylated ferulate fluorophores (HA-FA-Pg) in the development of drug delivery systems, the propargyl groups of HA-FA-Pg derivatives were employed with oleic acid (OA) or stearic acid (SA) [...] Read more.
In order to evaluate the potential of a technology platform based on hyaluronan copolymers grafted with propargylated ferulate fluorophores (HA-FA-Pg) in the development of drug delivery systems, the propargyl groups of HA-FA-Pg derivatives were employed with oleic acid (OA) or stearic acid (SA) residues across a biocompatible hexa(ethylene glycol) (HEG) spacer. The designed materials (i.e., HA-FA-HEG-OA or HA-FA-HEG-SA) showed clear-cut aggregation features in an aqueous environment, as confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM), generating nanoaggregate systems. In fact, HA-FA-HEG-OA and HA-FA-HEG-SA derivatives showed the property to create self-assembled cytocompatible nanostructured aggregates in water, thanks to the simultaneous presence of hydrophilic portions in the polymeric backbone, such as hyaluronic acid, and hydrophobic portions in the side chains. Furthermore, the designed materials interact with living cells showing a high degree of cytocompatibility. The potential ability of nanosystems to load pharmacologically active molecules was assessed by the physical entrapment of olanzapine into both polymeric systems. The drug loading evaluation demonstrated that the nanoparticles are able to incorporate a good quantity of olanzapine, as well as improve drug solubility, release profile, and cytocompatibility. Full article
(This article belongs to the Special Issue Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers)
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22 pages, 7210 KiB  
Article
Physicochemical Properties of a New PEGylated Polybenzofulvene Brush for Drug Encapsulation
by Marco Paolino, Annalisa Reale, Vincenzo Razzano, Germano Giuliani, Alessandro Donati, Gianluca Giorgi, Antonella Caterina Boccia, Raniero Mendichi, Daniele Piovani, Chiara Botta, Laura Salvini, Filippo Samperi, Cristina Savoca, Mariano Licciardi, Eugenio Paccagnini, Mariangela Gentile and Andrea Cappelli
Pharmaceutics 2019, 11(9), 444; https://doi.org/10.3390/pharmaceutics11090444 - 01 Sep 2019
Cited by 7 | Viewed by 2520
Abstract
A new polymer brush was synthesized by spontaneous polymerization of benzofulvene macromonomer 6-MOEG-9-T-BF3k bearing a nona(ethylene glycol) side chain linked to the 3-phenylindene scaffold by means of a triazole heterocycle. The polymer structure was studied by SEC-MALS, NMR spectroscopy, and MALDI-TOF MS [...] Read more.
A new polymer brush was synthesized by spontaneous polymerization of benzofulvene macromonomer 6-MOEG-9-T-BF3k bearing a nona(ethylene glycol) side chain linked to the 3-phenylindene scaffold by means of a triazole heterocycle. The polymer structure was studied by SEC-MALS, NMR spectroscopy, and MALDI-TOF MS techniques, and the results supported the role of oligomeric initiatory species in the spontaneous polymerization of polybenzofulvene derivatives. The aggregation features of high molecular weight poly-6-MOEG-9-T-BF3k-FE were investigated by pyrene fluorescence analysis, dynamic light scattering studies, and transmission electron microscopy, which suggested a tendency towards the formation of spherical objects showing dimensions in the range of 20–200 nm. Moreover, poly-6-MOEG-9-T-BF3k-FE showed an interesting cytocompatibility in the whole concentration range tested that, besides its aggregation features, makes this polybenzofulvene brush a good polymer candidate for nanoencapsulation and delivery of drug molecules. Finally, the photo-physical features of poly-6-MOEG-9-T-BF3k-FE could allow the biodistribution of the resulting drug delivery systems to be monitored by fluorescence microscopy techniques. Full article
(This article belongs to the Special Issue Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers)
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20 pages, 6761 KiB  
Article
Superhydrophobic Substrates for Ultrahigh Encapsulation of Hydrophilic Drug into Controlled-Release Polyelectrolyte Complex Beads: Statistical Optimization and In Vivo Evaluation
by Carol Yousry, Iman S. Ahmed, Maha M. Amin and Omaima N. El Gazayerly
Pharmaceutics 2019, 11(6), 257; https://doi.org/10.3390/pharmaceutics11060257 - 01 Jun 2019
Cited by 8 | Viewed by 2849
Abstract
In this work, ultrahigh drug-loaded chitosan (Ch)/K-carrageenan (Kc) polyelectrolyte complex (PEC) beads were formed in situ by cross-linking in a glutaraldehyde-saturated atmosphere and were prepared on superhydrophobic substrates fabricated by spraying glass surfaces with ready-made spray for domestic use (NeverWet®). Verapamil [...] Read more.
In this work, ultrahigh drug-loaded chitosan (Ch)/K-carrageenan (Kc) polyelectrolyte complex (PEC) beads were formed in situ by cross-linking in a glutaraldehyde-saturated atmosphere and were prepared on superhydrophobic substrates fabricated by spraying glass surfaces with ready-made spray for domestic use (NeverWet®). Verapamil hydrochloride (VP), a highly hydrophilic drug with a short biological half-life, was incorporated into a series of Ch-based and/or Ch/Kc-PEC-based beads to control its release profile in vivo. The formulation of VP-loaded beads was optimized using stepwise statistical designs based on a prespecified criterion. Several characteristics of the prepared beads, such as entrapment efficiency (EE%), in vitro drug release, swelling ratio, size and surface microstructure as well as molecular interactions between the drug and formulation ingredients, were investigated. In vivo pharmacokinetic (PK) studies were carried out using the rabbit model to study the ability of the optimized VP-loaded beads to control the absorption rate of VP. Results revealed that the prepared superhydrophobic substrates were able to fabricate VP-loaded beads with extremely high EE exceeding 90% w/w compared to only 27.80% when using conventional ionotropic gelation technique. PK results showed that the rate of VP absorption was well controlled following oral administration of the optimized beads to six rabbits compared to a marketed VP immediate release (IR) tablet, as evidenced by a 2.2-fold increase in mean residence time (MRT) and 5.24-fold extension in half value duration (HVD) over the marketed product without any observed reduction in the relative oral bioavailability. Full article
(This article belongs to the Special Issue Physicochemical Properties of Polymeric Micro- and Nanoparticles as Drug Carriers)
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