[go: up one dir, main page]

 
 
molecules-logo

Journal Browser

Journal Browser

Nanosystems in Pharmaceutical Technology

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Nanochemistry".

Deadline for manuscript submissions: closed (31 July 2021) | Viewed by 42769

Special Issue Editors


E-Mail Website
Guest Editor
Università degli Studi di Messina, Messina, Italy
Interests: drug delivery systems; polymeric materials; FTIR-ATR spectroscopy; Raman spectroscopy; neutron techniques; materials characterization

E-Mail Website
Guest Editor
Università degli Studi di Messina, Messina, Italy
Interests: cyclodextrins; inclusion complex; pharmaceutical development; nanotechnology in drug delivery

E-Mail Website
Guest Editor
Università degli Studi di Messina, Messina, Italy
Interests: cyclodextrins; inclusion complex; pharmaceutical development; nanotechnology in drug delivery

E-Mail Website
Guest Editor
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy
Interests: drug delivery; drug/cyclodextrin inclusion complexes; polymeric nanoparticles; cancer diseases; antimicrobial drugs; Alzheimer’s disease
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98122 Messina, Italy
Interests: drug delivery systems; polymeric materials; FTIR-ATR spectroscopy; Raman spectroscopy; neutron techniques; materials characterization
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Università degli Studi di Messina, Messina, Italy
Interests: drug delivery systems; polymeric materials; FTIR-ATR spectroscopy; Raman spectroscopy; neutron techniques; materials characterization

Special Issue Information

Dear Colleagues,

The development of new therapeutic products is not very often adequate to properly enhance those properties that usually limit their biological applications, such as water solubility, circulation time, and pharmacokinetic profile. Furthermore, new potentially therapeutic molecules fail to permeate the cell membrane, thus requiring a high dose to obtain a good bioavailability with consequent toxicity and undesired side effects. In this scenario, nanotechnology, through the employment of materials in the nanoscale range, is currently being developed and looks particularly promising in revolutionizing targeted drug delivery, gene therapy, diagnostics, and many related areas of research.

The aim of this Special Issue is to go deep inside the challenges in “Nanosystems in Pharmaceutical Technology”, presenting recent innovations in nanomaterials for biomedical applications. As Guest Editors, we cordially invite you to contribute a research paper or comprehensive review on any aspect related to this topic.

Prof. Dr. Valentina Venuti
Prof. Dr. Rosanna Stancanelli
Prof. Dr. Silvana Tommasini
Prof. Dr. Cinzia Anna Ventura
Prof. Dr. Vincenza Crupi
Prof. Dr. Domenico Majolino
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. Molecules 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 2700 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

  • Nanopharmaceuticals
  • Nanodiagnostics
  • Nanotherapeutics
  • Nanosized targeted drug delivery
  • Biomedical applications
  • Nanomedicine

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • e-Book format: Special Issues with more than 10 articles can be published as dedicated e-books, ensuring wide and rapid dissemination.

Further information on MDPI's Special Issue polices can be found here.

Published Papers (9 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

17 pages, 2548 KiB  
Article
Development of New Targeted Inulin Complex Nanoaggregates for siRNA Delivery in Antitumor Therapy
by Gennara Cavallaro, Carla Sardo, Emanuela Fabiola Craparo and Gaetano Giammona
Molecules 2021, 26(6), 1713; https://doi.org/10.3390/molecules26061713 - 19 Mar 2021
Cited by 7 | Viewed by 1974
Abstract
Here, a novel strategy of formulating efficient polymeric carriers based on the already described INU-IMI-DETA for gene material whose structural, functional, and biological properties can be modulated and improved was successfully investigated. In particular, two novel derivatives of INU-IMI-DETA graft copolymer were synthesized [...] Read more.
Here, a novel strategy of formulating efficient polymeric carriers based on the already described INU-IMI-DETA for gene material whose structural, functional, and biological properties can be modulated and improved was successfully investigated. In particular, two novel derivatives of INU-IMI-DETA graft copolymer were synthesized by chemical functionalisation with epidermal growth factor (EGF) or polyethylenglycol (PEG), named INU-IMI-DETA-EGF and INU-IMI-DETA-PEG, respectively, in order to improve the performance of already described “inulin complex nanoaggregates” (ICONs). The latter were thus prepared by appropriately mixing the two copolymers, by varying each component from 0 to 100 wt% on the total mixture, named EP-ICONs. It was seen that the ability of the INU-IMI-DETA-EGF/INU-IMI-DETA-PEG polymeric mixture to complex siGL3 increases with the increase in the EGF-based component in the EP-ICONs and, for each sample, with the increase in the copolymer:siRNA weight ratio (R). On the other hand, the susceptibility of loaded siRNA towards RNase decreases with the increase in the pegylated component in the polymeric mixture. At all R values, the average size and the zeta potential values are suitable for escaping from the RES system and suitable for prolonged intravenous circulation. By means of biological characterisation, it was shown that MCF-7 cells are able to internalize mainly the siRNA-loaded into EGF-decorated complexes, with a significant difference from ICONs, confirming its targeting function. The targeting effect of EGF on EP-ICONs was further demonstrated by a competitive cell uptake study, i.e., after cell pre-treatment with EGF. Finally, it was shown that the complexes containing both EGF and PEG are capable of promoting the internalisation and therefore the transfection of siSUR, a siRNA acting against surviving mRNA, and to increase the sensitivity to an anticancer agent, such as doxorubicin. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>Schematic representation of INU-IMI-DETA-EGF synthesis. (<b>a</b>) PEG<sub>2000</sub>CHO, water, pH5, r.t. overnight; (<b>b</b>) EDCI, NHS, hEGF, water, r.t. 6 h.</p>
Full article ">Figure 2
<p>Fluorescence intensity % of ethidium bromide (EtBr) in the presence of unloaded siGL3 after EP-ICONs, P-ICONs, E-ICONs, and ICONs formation at R ranging between 5 and 50.</p>
Full article ">Figure 3
<p>RNase protection assay. (<b>A</b>) 4 h, (<b>B</b>) 24 h.</p>
Full article ">Figure 4
<p>Size and ζ potential values of E-ICONs and EP-ICONs (obtained at INU-IMI-DETA-EGF: INU-IMI-DETA-PEG copolymer weight ratio equal to 90:10, 70:30, 50:50) at copolymer/siRNA weight ratios (R) ranging between 5 and 50.</p>
Full article ">Figure 5
<p>Quantitative uptake of siGL3-Cy5 in MCF-7 cells after 4 h (<b>A</b>) and 24 h (<b>B</b>) incubation with EP-ICONs at copolymer:siRNA weight ratios (R) comprised between 10 and 50. Results were compared with each other and with P-ICONs, E-ICONs, naked siRNA (siGL3-Cy5) and untreated cells (NT). Connections represent statistical differences with <span class="html-italic">p</span> &lt; 0.05.</p>
Full article ">Figure 6
<p>EGF competitive cellular uptake studies. Data are expressed as the differences between uptake without EGF pre-incubation and EGF competitive uptake. Statistically significant values are indicated with asterisks (* <span class="html-italic">p</span> &lt; 0.05).</p>
Full article ">Figure 7
<p>Proliferation of MCF-7 cells after 72 h incubation with E-ICONs, P-ICONs, or EP-ICONs containing survivin targeted siRNA. * represents <span class="html-italic">p</span> &lt; 0.05 with respect to siRNA naked treated cells. A red asterisk on E-ICONs R10 represents significant reduction when compared with P-ICONs at the same weight ratio.</p>
Full article ">Figure 8
<p>Chemosensitisation experiments. Effects on cell viability of Doxo (24 h) on MCF-7 cells after 24 h pre-treatment with E-ICONs, P-ICONs or EP-ICONs containing siSUR. * represents <span class="html-italic">p</span> &lt; 0.05 with respect to cells treated with naked siSUR and Doxo (siRNA + Doxo).</p>
Full article ">
18 pages, 3522 KiB  
Article
Formulation of Cannabidiol in Colloidal Lipid Carriers
by Nadine Monika Francke, Frederic Schneider, Knut Baumann and Heike Bunjes
Molecules 2021, 26(5), 1469; https://doi.org/10.3390/molecules26051469 - 8 Mar 2021
Cited by 24 | Viewed by 4779
Abstract
In this study, the general processability of cannabidiol (CBD) in colloidal lipid carriers was investigated. Due to its many pharmacological effects, the pharmaceutical use of this poorly water-soluble drug is currently under intensive research and colloidal lipid emulsions are a well-established formulation option [...] Read more.
In this study, the general processability of cannabidiol (CBD) in colloidal lipid carriers was investigated. Due to its many pharmacological effects, the pharmaceutical use of this poorly water-soluble drug is currently under intensive research and colloidal lipid emulsions are a well-established formulation option for such lipophilic substances. To obtain a better understanding of the formulability of CBD in lipid emulsions, different aspects of CBD loading and its interaction with the emulsion droplets were investigated. Very high drug loads (>40% related to lipid content) could be achieved in emulsions of medium chain triglycerides, rapeseed oil, soybean oil and trimyristin. The maximum CBD load depended on the type of lipid matrix. CBD loading increased the particle size and the density of the lipid matrix. The loading capacity of a trimyristin emulsion for CBD was superior to that of a suspension of solid lipid nanoparticles based on trimyristin (69% vs. 30% related to the lipid matrix). In addition to its localization within the lipid core of the emulsion droplets, cannabidiol was associated with the droplet interface to a remarkable extent. According to a stress test, CBD destabilized the emulsions, with phospholipid-stabilized emulsions being more stable than poloxamer-stabilized ones. Furthermore, it was possible to produce emulsions with pure CBD as the dispersed phase, since CBD demonstrated such a pronounced supercooling tendency that it did not recrystallize, even if cooled to −60 °C. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>Kinetics of cannabidiol loading in emulsion MCT-P188-120 nm. Error bars represent the standard deviations but are mostly not visible.</p>
Full article ">Figure 2
<p>(<b>a</b>) Achievable cannabidiol load (mass percent) in emulsions composed of different matrix lipids (emulsions MCT-P188-120 nm, TM-P188-120 nm, SB-P188-120 nm and RS-P188-120 nm). (<b>b</b>) Particle sizes of these emulsions before and after cannabidiol loading. (<b>c</b>) Experimentally observed increase in the volumes of the emulsion droplets as compared to a simulated volume increase based on the molecular volume of the loaded cannabidiol molecules. The molecular volume was based on the van der Waals surface which was computed with MOE Version 2018.01.01.</p>
Full article ">Figure 3
<p>(<b>a</b>) Effect of cannabidiol on the density of soybean oil, demonstrated as density and calculation of the relative increase in density normalized to the cannabidiol concentration. (<b>b</b>) Simulated volume increase of soybean oil with increasing concentrations of cannabidiol.</p>
Full article ">Figure 4
<p>Cannabidiol load (mass percent) of differently sized colloidal soybean oil emulsions (<b>a</b>); (<b>b</b>) illustrates the drug load in dependence on specific interfacial area of the emulsion droplets.</p>
Full article ">Figure 5
<p>Cannabidiol load (mass percent) in a trimyristin emulsion and suspension of equal composition (from TM-P188-120 nm).</p>
Full article ">Figure 6
<p>Stability of soybean oil emulsions stabilized with poloxamer 188 (P188) or poloxamer 407 (P407), respectively, and Lipofundin<sup>®</sup> (composed of phospholipids, medium chain triglycerides and soybean oil) before and after loading with cannabidiol (CBD). Shaking periods that did not induce instability are shown in green, intervals of unstable samples in red; the first destabilizing interval is marked with a color gradient. Investigated samples points are included as lines.</p>
Full article ">Figure 7
<p>DSC reheating curve of cannabidiol (after heating to 85 °C and subsequent cooling to −60 °C).</p>
Full article ">Figure 8
<p>Particle size and PdI of emulsions containing pure cannabidiol as dispersed phase and stabilized with poloxamer 188 (<b>a</b>) or poloxamer 407 (<b>b</b>). The results represent the mean values of <span class="html-italic">n</span> = 2. The error bar shows the upper and lower measured values.</p>
Full article ">
16 pages, 2464 KiB  
Article
Rutin-Loaded Solid Lipid Nanoparticles: Characterization and In Vitro Evaluation
by Federica De Gaetano, Maria Chiara Cristiano, Valentina Venuti, Vincenza Crupi, Domenico Majolino, Giuseppe Paladini, Giuseppe Acri, Barbara Testagrossa, Alessia Irrera, Donatella Paolino, Silvana Tommasini, Cinzia Anna Ventura and Rosanna Stancanelli
Molecules 2021, 26(4), 1039; https://doi.org/10.3390/molecules26041039 - 16 Feb 2021
Cited by 30 | Viewed by 3339
Abstract
This study was aimed at preparing and characterizing solid lipid nanoparticles loading rutin (RT-SLNs) for the treatment of oxidative stress-induced diseases. Phospholipon 80H® as a solid lipid and Polysorbate 80 as surfactant were used for the SLNs preparation, using the solvent emulsification/diffusion [...] Read more.
This study was aimed at preparing and characterizing solid lipid nanoparticles loading rutin (RT-SLNs) for the treatment of oxidative stress-induced diseases. Phospholipon 80H® as a solid lipid and Polysorbate 80 as surfactant were used for the SLNs preparation, using the solvent emulsification/diffusion method. We obtained spherical RT-SLNs with low sizes, ranging from 40 to 60 nm (hydrodynamic radius) for the SLNs prepared starting from 2% and 5% (w/w) theoretical amount. All prepared formulations showed negative zeta-potential values. RT was efficiently encapsulated within SLNs, obtaining high encapsulation efficiency and drug content percentages, particularly for SLNs prepared with a 5% theoretical amount of RT. In vitro release profiles and analysis of the obtained data applying different kinetic models revealed Fickian diffusion as the main mechanism of RT release from the SLNs. The morphology of RT-SLNs was characterized by scanning electron microscopy (SEM), whereas the interactions between RT and the lipid matrix were investigated by Raman spectroscopy, evidencing spectral modifications of characteristic bands of RT due to the establishment of new interactions. Finally, antioxidant activity assay on human glioblastoma astrocytoma (U373) culture cells showed a dose-dependent activity for RT-SLNs, particularly at the highest assayed dose (50 μM), whereas the free drug showed the lesser activity. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>In vitro release profiles of free RT (blue squares) and RT-SLNs (red circles).</p>
Full article ">Figure 2
<p>SEM images of RT-SLNs at different magnification (<b>a</b>,<b>b</b>), together with the Gaussian distribution of the radius peaked at 25 ± 10 nm (<b>c</b>).</p>
Full article ">Figure 3
<p>Experimental Raman spectrum of RT (<b>a</b>) and SLNs (<b>b</b>).</p>
Full article ">Figure 4
<p>Experimental Raman spectra, respectively collected in the 1500–1710 cm<sup>−1</sup> (<b>a</b>) 1220–1330 cm<sup>−1</sup> (<b>b</b>) intervals, for RT (black line), SLNs (red line), and RT-SLNs (green line) systems. The negligible contribution of SLNs to the vibrational profile, in the investigated spectral range, is well evident.</p>
Full article ">Figure 5
<p>Effects on U373 cell viability of 24 h, 48 h, and 72 h treatment with different concentrations of free RT (<b>a</b>), DMSO (<b>b</b>), and blank SLNs (<b>c</b>). Cell viability was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test, and the results are presented as the mean of three different experiments ± standard deviation (S.D.). The error bar, if not shown, was within the symbol.</p>
Full article ">Figure 6
<p>Anti-oxidant effect of RT and RT-SLNs on U373 cells expressed as LDH release reduction. Cells were treated with increased concentration of RT and RT-SLNs for 24 h and then incubated with H<sub>2</sub>O<sub>2</sub> (700 µM) for 1 h. Results are presented as the mean of three different experiments ± S.D. The error bar, if not shown, was within the bar. The data obtained for RT-SLNs are statistically significant with respect to the same concentration of free RT (* <span class="html-italic">p</span> &lt; 0.05), while the data obtained for RT and RT-SLNs are statistically significant with respect to oxidation control (@ <span class="html-italic">p</span> &lt; 0.05; @@ <span class="html-italic">p</span> &lt; 0.001).</p>
Full article ">
13 pages, 7534 KiB  
Article
Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil
by Hilda Amekyeh and Nashiru Billa
Molecules 2021, 26(4), 908; https://doi.org/10.3390/molecules26040908 - 9 Feb 2021
Cited by 12 | Viewed by 3703
Abstract
Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses [...] Read more.
Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses of the lipid matrix to external challenges is crucial. Here, we evaluate the effects of lyophilization on key responses of 1:1 beeswax–theobroma oil matrix SLNs using three model drugs: amphotericin B (AMB), paracetamol (PAR), and sulfasalazine (SSZ). Fresh SLNs were stable with sizes ranging between 206.5–236.9 nm. Lyophilization and storage for 24 months (4–8 °C) caused a 1.6- and 1.5-fold increase in size, respectively, in all three SLNs. Zeta potential was >60 mV in fresh, stored, and lyophilized SLNs, indicating good colloidal stability. Drug release was not significantly affected by lyophilization up to 8 h. Drug release percentages at end time were 11.8 ± 0.4, 65.9 ± 0.04, and 31.4 ± 1.95% from fresh AMB-SLNs, PAR-SLNs, and SSZ-SLNs, respectively, and 11.4 ± 0.4, 76.04 ± 0.21, and 31.6 ± 0.33% from lyophilized SLNs, respectively. Thus, rate of release is dependent on API solubility (AMB < SSZ < PAR). Drug release from each matrix followed the Higuchi model and was not affected by lyophilization. The above SLNs show potential for use in delivering hydrophilic and lipophilic drugs. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>Chemical structures of (<b>a</b>) AMB (amphotericin B), (<b>b</b>) PAR (paracetamol), and (<b>c</b>) SSZ (sulfasalazine).</p>
Full article ">Figure 2
<p>NTA (nanoparticle tracking analysis) size distribution by intensity graphs for fresh (<b>a</b>) AMB-SLNs (solid lipid nanoparticles), (<b>b</b>) PAR-SLNs, and (<b>c</b>) SSZ-SLNs (<span class="html-italic">n</span> = 3).</p>
Full article ">Figure 3
<p>DLS (dynamic light scattering) size distribution by intensity graphs for (<b>a</b>) freshly prepared, (<b>b</b>) stored (24 months), and (<b>c</b>) lyophilized AMB-SLNs, PAR-SLNs, and SSZ-SLNs (<span class="html-italic">n</span> = 3).</p>
Full article ">Figure 4
<p>z-Average diameters and PDIs (polydispersity indexes) of freshly prepared, stored (for 24 months), and lyophilized AMB-SLNs, PAR-SLNs, and SSZ-SLNs (<span class="html-italic">n</span> = 3).</p>
Full article ">Figure 5
<p>ZPs (zeta potentials) of freshly prepared, stored (24 months), and lyophilized AMB-SLNs, PAR-SLNs, and SSZ-SLNs (<span class="html-italic">n</span> = 3).</p>
Full article ">Figure 6
<p>Cumulative drug release from freshly prepared and lyophilized AMB-SLNs, PAR-SLNs, and SSZ-SLNs in PBS (phosphate-buffered saline; pH 7.4).</p>
Full article ">Figure 7
<p>FTIR (Fourier-transform infrared spectroscopy) spectra for (<b>a</b>,<b>b</b>) AMB, (<b>c</b>,<b>d</b>) PAR, and (<b>e</b>,<b>f</b>) SSZ. (<b>a</b>,<b>c</b>,<b>e</b>) Pure drugs. (<b>b</b>,<b>d</b>,<b>f</b>) SLNs.</p>
Full article ">
11 pages, 1200 KiB  
Communication
An Underestimated Factor: The Extent of Cross-Reactions Modifying APIs in Surface-Modified Liposomal Preparations Caused by Comprised Activated Lipids
by Max Sauter, Jürgen Burhenne, Walter E. Haefeli and Philipp Uhl
Molecules 2020, 25(19), 4436; https://doi.org/10.3390/molecules25194436 - 27 Sep 2020
Cited by 2 | Viewed by 5573
Abstract
Despite the nowadays available plentitude of strategies to selectively introduce functional surface modification of liposomes, in preclinical research this process is still primarily performed after liposomal preparation utilizing comprised activated phospholipids with functionalized head groups. However, because these activated lipids are present during [...] Read more.
Despite the nowadays available plentitude of strategies to selectively introduce functional surface modification of liposomes, in preclinical research this process is still primarily performed after liposomal preparation utilizing comprised activated phospholipids with functionalized head groups. However, because these activated lipids are present during the liposomal preparation process, they can cross-react with incorporated drugs, especially the particularly often utilized active esters and maleimide groups. Macromolecular drugs, being composed of amino acids, are particularly prone to such cross-reactions due to their often multiple reactive functionalities such as amino and disulfide groups. To demonstrate this impact on the formulation in liposomal surface modification, we assessed the extent of cross-reaction during the liposomal preparation of two activated phospholipids with typically used head group functionalized phospholipids, with the two peptide drugs vancomycin and insulin comprising disulfide and amino functionalities. Both drugs revealed a considerable fraction of covalent modification (estimated 2 to 12%) generated during the liposome preparation process with comprised activated lipids. Modification of the active pharmaceutical ingredients (APIs) was determined by high-resolution mass spectrometric analysis. These findings clearly demonstrate the non-negligibility of potential cross reactions using the post preparation liposomal surface modification strategy in preclinical research. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>Scheme of the possible cross-reaction of activated ester and maleimide groups of phospholipids with amino and disulfide groups of active pharmaceutical ingredients (APIs).</p>
Full article ">Figure 2
<p>High-resolution mass spectrometric characterization of liposomes comprising Tfp-dPEG<sub>13</sub>-DSPE and encapsulated vancomycin. (<b>A</b>) Mass spectrum of vancomycin-containing liposomes comprising Tfp-dPEG<sub>13</sub>-DSPE. Visible is the formic acid mono-adduct of the conjugate of Tfp-dPEG<sub>13</sub>-DSPE and vancomycin ([M+3H+CHO<sub>2</sub>H]<sup>3+</sup>), while the remaining signals correspond to unmodified vancomycin with three being in-source fragments (desglycosyl-vancomycin, desvancosamine-vancomycin, and its corresponding sodium adduct). (<b>B</b>) Positive product spectrum of the [M+3H+CHO<sub>2</sub>H]<sup>3+</sup> signal of the conjugate of Tfp-dPEG<sub>13</sub>-DSPE and vancomycin after collision-induced dissociation (CID) at 30 V. Besides the parent signal, the primary CID fragments are ions corresponding to vancomycin confirming the conjugates identity.</p>
Full article ">Figure 3
<p>High-resolution mass spectra of liposomal formulations of insulin comprising lipids with maleimide and activated ester functions. (<b>A</b>) Liposomal formulation of insulin containing Tfp-PEG<sub>13</sub>-DSPE. Visible are the [M + 3H]<sup>3+</sup> ion of insulin with its sodium adducts and the [M + 4H]<sup>4+</sup> signal of the conjugate of insulin and Tfp-PEG<sub>13</sub>-DSPE with the corresponding sodium adducts. (<b>B</b>) Liposomal formulation containing Mal-PEG<sub>12</sub>-DSPE. Visible are the [M + 3H]<sup>3+</sup> signal of insulin with its sodium adducts and the [M + 4H]<sup>4+</sup> signal of the conjugate of insulin and Mal-PEG<sub>12</sub>-DSPE.</p>
Full article ">
21 pages, 5037 KiB  
Article
The Rheolaser Master™ and Kinexus Rotational Rheometer® to Evaluate the Influence of Topical Drug Delivery Systems on Rheological Features of Topical Poloxamer Gel
by Maria Chiara Cristiano, Francesca Froiio, Antonia Mancuso, Federica De Gaetano, Cinzia Anna Ventura, Massimo Fresta and Donatella Paolino
Molecules 2020, 25(8), 1979; https://doi.org/10.3390/molecules25081979 - 23 Apr 2020
Cited by 31 | Viewed by 4658
Abstract
Poloxamer 407 copolymer is a versatile and widely used thermo-reversible material. Its use has many advantages, such as bio-adhesion, enhanced solubilization of poorly water-soluble drugs and many applications fields like oral, rectal, topical, nasal drug administration. Hydrogels made up of Poloxamer 407 are [...] Read more.
Poloxamer 407 copolymer is a versatile and widely used thermo-reversible material. Its use has many advantages, such as bio-adhesion, enhanced solubilization of poorly water-soluble drugs and many applications fields like oral, rectal, topical, nasal drug administration. Hydrogels made up of Poloxamer 407 are characterized by specific rheological features, which are affected by temperature, concentration and presence of other compounds. A strategic approach in topical therapeutic treatments may be the inclusion of drug delivery systems, such as ethosomes, transfersomes and niosomes, into hydrogel poloxamer formulation. The evaluation of the interaction between colloidal carriers and the Poloxamer 407 hydrogel network is essential for a suitable design of an innovative topical dosage form. For this reason, the Rheolaser Master™, based on diffusing wave spectroscopy, and a Kinexus Rotational Rheometer were used to evaluate the influence of nanocarriers on the microrheological features of hydrogels. The advantages of the Rheolaser Master™ analyzer are: (i) its ability to determine viscoelastic parameter, without altering or destroying the sample and at rest (zero shear); (ii) possibility of aging analysis on the same sample. This study provide evidence that vesicular systems do not influence the rheological features of the gel, supporting the possibility to encapsulate an innovative system into a three-dimensional network. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Graphical abstract

Graphical abstract
Full article ">Figure 1
<p>Transmission and backscattering profiles of ethosomes (<b>A</b>), transfersomes (<b>B</b>) and niosomes (<b>C</b>) determined by Turbiscan Lab<sup>®</sup> Expert. Various runs were representative of three independent experiments. Data are reported as a function of time (0–1 h) and sample height.</p>
Full article ">Figure 2
<p>Turbiscan Stability Index (TSI) in function of time obtained for ethosomes, transfersomes and niosomes, by using Turbiscan Lab<sup>®</sup> Expert.</p>
Full article ">Figure 3
<p>Mean square displacement MSD of hydrogel prepared with different concentrations of poloxamer 407: 20% (<span class="html-italic">w</span>/<span class="html-italic">w</span>) (<b>A</b>), 25% (<span class="html-italic">w</span>/<span class="html-italic">w</span>) (<b>B</b>) and 30% (<span class="html-italic">w</span>/<span class="html-italic">w</span>) (<b>C</b>), as a function of decorrelation time. The illustrated results were representative of three independent experiments.</p>
Full article ">Figure 4
<p>Elasticity Index (EI) (<b>A</b>) and Solid Liquid Balance (<b>B</b>) profiles versus time for 20% poloxamer 407, 25% poloxamer 407 and 30% poloxamer 407 samples.</p>
Full article ">Figure 5
<p>Mean square displacement of hydrogels made up of poloxamer 407 at 20% (<span class="html-italic">w</span>/<span class="html-italic">w</span>) alone (<b>A</b>) or in the presence of ethosomes (<b>B</b>), transfersomes (<b>C</b>) and niosomes (<b>D</b>) as a function of decorrelation time. The illustrated results were representative of three independent experiments.</p>
Full article ">Figure 6
<p>Elasticity Index (EI) (<b>A</b>) and Solid Liquid Balance profile (<b>B</b>) versus time for 20% poloxamer 407 with and without TDDSs.</p>
Full article ">Figure 7
<p>Flow curves (shear viscosity versus shear rate) of (<b>A</b>) 20% Poloxamer 407, (<b>B</b>) 25% Poloxamer 407 and (<b>C</b>) 30% Poloxamer 407, with and without carriers. The illustrated results were representative of three independent experiments.</p>
Full article ">Figure 8
<p>Complex shear modulus (<span class="html-italic">G*</span>) versus Frequency for 20% Poloxamer 407 (<b>A</b>), 25% Poloxamer 407 (<b>B</b>) and 30% Poloxamer 407 (<b>C</b>) with and without TDDSs. The illustrated results were representative of three independent experiments.</p>
Full article ">Figure 9
<p>In vitro percutaneous permeation of paclitaxel from different formulations through SCE membranes, in comparison with a hydroalcoholic drug solution (as the control). Values represent the mean of three different experiments ± standard deviation.</p>
Full article ">
7 pages, 222 KiB  
Article
The Use of Different Commercial Mineral Water Brands to Produce Oil-In-Water Nanoemulsions
by Pedro A Rocha-Filho, Antonio D. Monteiro, Luciana C. Agostinho and Marina P. A. Oliveira
Molecules 2020, 25(3), 603; https://doi.org/10.3390/molecules25030603 - 30 Jan 2020
Cited by 3 | Viewed by 2985
Abstract
Nanoemulsions are submicron-size colloidal systems that have the ability to encapsulate, protect, and deliver active ingredients. They have been used in the pharmaceutical, cosmetics, and food industries to improve the absorption of drugs by the skin or via the gastrointestinal tract, aide in [...] Read more.
Nanoemulsions are submicron-size colloidal systems that have the ability to encapsulate, protect, and deliver active ingredients. They have been used in the pharmaceutical, cosmetics, and food industries to improve the absorption of drugs by the skin or via the gastrointestinal tract, aide in food conservation, and treat skin problems. To proper formulate a nanoemulsion, it is important to know the characteristics of its components (aqueous and oil phases, surfactants and additives), as well as the influence on the production method that will be used. This study investigates the influence of aqueous phase composition, stability and particle size in an oil-and-water nanoemulsion formation. By using a low energy method, the purified water was exchanged for different commercial mineral water and saline solutions, and the results of stability, particle size, pH and conductivity tests, were compared. These results show that the minerals present in commercial waters may alter the particle size, pH and conductivity values of nanoemulsions, as well as their stability. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)

Review

Jump to: Research

30 pages, 2538 KiB  
Review
Influence of Materials Properties on Bio-Physical Features and Effectiveness of 3D-Scaffolds for Periodontal Regeneration
by Nicola d’Avanzo, Maria Chiara Bruno, Amerigo Giudice, Antonia Mancuso, Federica De Gaetano, Maria Chiara Cristiano, Donatella Paolino and Massimo Fresta
Molecules 2021, 26(6), 1643; https://doi.org/10.3390/molecules26061643 - 15 Mar 2021
Cited by 25 | Viewed by 4489
Abstract
Periodontal diseases are multifactorial disorders, mainly due to severe infections and inflammation which affect the tissues (i.e., gum and dental bone) that support and surround the teeth. These pathologies are characterized by bleeding gums, pain, bad breath and, in more severe forms, can [...] Read more.
Periodontal diseases are multifactorial disorders, mainly due to severe infections and inflammation which affect the tissues (i.e., gum and dental bone) that support and surround the teeth. These pathologies are characterized by bleeding gums, pain, bad breath and, in more severe forms, can lead to the detachment of gum from teeth, causing their loss. To date it is estimated that severe periodontal diseases affect around 10% of the population worldwide thus making necessary the development of effective treatments able to both reduce the infections and inflammation in injured sites and improve the regeneration of damaged tissues. In this scenario, the use of 3D scaffolds can play a pivotal role by providing an effective platform for drugs, nanosystems, growth factors, stem cells, etc., improving the effectiveness of therapies and reducing their systemic side effects. The aim of this review is to describe the recent progress in periodontal regeneration, highlighting the influence of materials’ properties used to realize three-dimensional (3D)-scaffolds, their bio-physical characteristics and their ability to provide a biocompatible platform able to embed nanosystems. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Figure 1

Figure 1
<p>Schematic representation of the main scaffolds used in periodontitis and periodontal regeneration.</p>
Full article ">Figure 2
<p>Natural and synthetic polymers mainly used in periodontal tissue regeneration.</p>
Full article ">Figure 3
<p>Schematic representation of composite scaffolds, made up of nanosystems embedded into three-dimensional (3D) scaffold.</p>
Full article ">
29 pages, 2356 KiB  
Review
Chitosan Nanoparticles-Insight into Properties, Functionalization and Applications in Drug Delivery and Theranostics
by Jhanvi Jhaveri, Zarna Raichura, Tabassum Khan, Munira Momin and Abdelwahab Omri
Molecules 2021, 26(2), 272; https://doi.org/10.3390/molecules26020272 - 7 Jan 2021
Cited by 157 | Viewed by 10001
Abstract
Nanotechnology-based development of drug delivery systems is an attractive area of research in formulation driven R&D laboratories that makes administration of new and complex drugs feasible. It plays a significant role in the design of novel dosage forms by attributing target specific drug [...] Read more.
Nanotechnology-based development of drug delivery systems is an attractive area of research in formulation driven R&D laboratories that makes administration of new and complex drugs feasible. It plays a significant role in the design of novel dosage forms by attributing target specific drug delivery, controlled drug release, improved, patient friendly drug regimen and lower side effects. Polysaccharides, especially chitosan, occupy an important place and are widely used in nano drug delivery systems owing to their biocompatibility and biodegradability. This review focuses on chitosan nanoparticles and envisages to provide an insight into the chemistry, properties, drug release mechanisms, preparation techniques and the vast evolving landscape of diverse applications across disease categories leading to development of better therapeutics and superior clinical outcomes. It summarizes recent advancement in the development and utility of functionalized chitosan in anticancer therapeutics, cancer immunotherapy, theranostics and multistage delivery systems. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
Show Figures

Graphical abstract

Graphical abstract
Full article ">Figure 1
<p>Classification of NPs.</p>
Full article ">Figure 2
<p>Synthesis of chitosan from chitin and structures of some of functionalized chitosan derivatives.</p>
Full article ">Figure 3
<p>Multifaceted chitosan in drug delivery.</p>
Full article ">Figure 4
<p>Drug release mechanism from chitosan NPs.</p>
Full article ">Figure 5
<p>Chitosan NPs as theranostics.</p>
Full article ">
Back to TopTop