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Pharmaceutical Nanotechnology: Novel Approaches
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Pharmaceutical Nanotechnology: Novel Approaches

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

Deadline for manuscript submissions: closed (30 January 2016) | Viewed by 154862

Special Issue Editor

Dr. Alexandru Mihai Grumezescu

E-Mail Website
Guest Editor
Department of Science and Engineereing of Oxide Materials and Nanomaterials, Faculty of Applied Chemistry and Materials Science, Politehnica University of Bucharest, RO-011061 Bucharest, Romania
Interests: synthesis and characterization of nanobiomaterials; polymers; pharmaceutical nanotechnology; drug delivery; anti-biofilm surfaces; nanomodified surfaces; natural products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Due to the rapid development of nanostructures with biological applications, most of them with a great impact on the treatment of various diseases, this Special Issue of Molecules, "Pharmaceutical Nanotechnology: Novel Approaches," aims to provide an up to date and comprehensive overview of the fabrication, characterization, and current applications of smart nanoarchitectonics. Both bottom up and top down approaches intended to enrich the knowledge and applicative potential of this recent field are welcome.

The Special Issue scope is broad and includes the following areas: bioceramics, nanoparticles, biopolymers, liposomes, hybrid materials, nanocomposites, scaffolds, bio-printing, biomimetic nanomaterials, drug delivery and controlled release nanoshuttles, nano-functionalized surfaces, etc.

Considering the great interest regarding the development of personalized therapeutic and explorative approaches to efficiently coping with severe diseases, this Special Issue is expected to have an important scientific and applicative contribution on the field of molecular pharmaceutics.

Dr. Alexandru Mihai Grumezescu
Guest Editor

Manuscript Submission Information

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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

  • drug targeting
  • modulation of biofilm development
  • wound healing
  • magnetic resonance imaging
  • antimicrobial therapy
  • drug delivery
  • cancer therapy
  • diagnostics

Published Papers (19 papers)

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22720 KiB  
Article
Fabrication, Characterization, and Evaluation of Bionanocomposites Based on Natural Polymers and Antibiotics for Wound Healing Applications
by Marius Rădulescu, Alina Maria Holban, Laurențiu Mogoantă, Tudor-Adrian Bălşeanu, George Dan Mogoșanu, Diana Savu, Roxana Cristina Popescu, Oana Fufă, Alexandru Mihai Grumezescu, Eugenia Bezirtzoglou, Veronica Lazar and Mariana Carmen Chifiriuc
Molecules 2016, 21(6), 761; https://doi.org/10.3390/molecules21060761 - 10 Jun 2016
Cited by 21 | Viewed by 6274
Abstract
The aim of our research activity was to obtain a biocompatible nanostructured composite based on naturally derived biopolymers (chitin and sodium alginate) loaded with commercial antibiotics (either Cefuroxime or Cefepime) with dual functions, namely promoting wound healing and assuring the local delivery of [...] Read more.
The aim of our research activity was to obtain a biocompatible nanostructured composite based on naturally derived biopolymers (chitin and sodium alginate) loaded with commercial antibiotics (either Cefuroxime or Cefepime) with dual functions, namely promoting wound healing and assuring the local delivery of the loaded antibiotic. Compositional, structural, and morphological evaluations were performed by using the thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and fourier transform infrared spectroscopy (FTIR) analytical techniques. In order to quantitatively and qualitatively evaluate the biocompatibility of the obtained composites, we performed the tetrazolium-salt (MTT) and agar diffusion in vitro assays on the L929 cell line. The evaluation of antimicrobial potential was evaluated by the viable cell count assay on strains belonging to two clinically relevant bacterial species (i.e., Escherichia coli and Staphylococcus aureus). Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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5351 KiB  
Article
Antimicrobial Lemongrass Essential Oil—Copper Ferrite Cellulose Acetate Nanocapsules
by Ioannis L. Liakos, Mohamed H. Abdellatif, Claudia Innocenti, Alice Scarpellini, Riccardo Carzino, Virgilio Brunetti, Sergio Marras, Rosaria Brescia, Filippo Drago and Pier Paolo Pompa
Molecules 2016, 21(4), 520; https://doi.org/10.3390/molecules21040520 - 20 Apr 2016
Cited by 26 | Viewed by 8288
Abstract
Cellulose acetate (CA) nanoparticles were combined with two antimicrobial agents, namely lemongrass (LG) essential oil and Cu-ferrite nanoparticles. The preparation method of CA nanocapsules (NCs), with the two antimicrobial agents, was based on the nanoprecipitation method using the solvent/anti-solvent technique. Several physical and [...] Read more.
Cellulose acetate (CA) nanoparticles were combined with two antimicrobial agents, namely lemongrass (LG) essential oil and Cu-ferrite nanoparticles. The preparation method of CA nanocapsules (NCs), with the two antimicrobial agents, was based on the nanoprecipitation method using the solvent/anti-solvent technique. Several physical and chemical analyses were performed to characterize the resulting NCs and to study their formation mechanism. The size of the combined antimicrobial NCs was found to be ca. 220 nm. The presence of Cu-ferrites enhanced the attachment of LG essential oil into the CA matrix. The magnetic properties of the combined construct were weak, due to the shielding of Cu-ferrites from the polymeric matrix, making them available for drug delivery applications where spontaneous magnetization effects should be avoided. The antimicrobial properties of the NCs were significantly enhanced with respect to CA/LG only. This work opens novel routes for the development of organic/inorganic nanoparticles with exceptional antimicrobial activities. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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2188 KiB  
Article
Robust Synthesis of Ciprofloxacin-Capped Metallic Nanoparticles and Their Urease Inhibitory Assay
by Muhammad Nisar, Shujaat Ali Khan, Mughal Qayum, Ajmal Khan, Umar Farooq, Hawa Z.E. Jaafar, Muhammad Zia-Ul-Haq and Rashid Ali
Molecules 2016, 21(4), 411; https://doi.org/10.3390/molecules21040411 - 25 Mar 2016
Cited by 22 | Viewed by 7201
Abstract
The fluoroquinolone antibacterial drug ciprofloxacin (cip) has been used to cap metallic (silver and gold) nanoparticles by a robust one pot synthetic method under optimized conditions, using NaBH4 as a mild reducing agent. Metallic nanoparticles (MNPs) showed constancy against variations in pH, [...] Read more.
The fluoroquinolone antibacterial drug ciprofloxacin (cip) has been used to cap metallic (silver and gold) nanoparticles by a robust one pot synthetic method under optimized conditions, using NaBH4 as a mild reducing agent. Metallic nanoparticles (MNPs) showed constancy against variations in pH, table salt (NaCl) solution, and heat. Capping with metal ions (Ag/Au-cip) has significant implications for the solubility, pharmacokinetics and bioavailability of fluoroquinolone molecules. The metallic nanoparticles were characterized by several techniques such as ultraviolet visible spectroscopy (UV), atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) methods. The nanoparticles synthesized using silver and gold were subjected to energy dispersive X-ray tests in order to show their metallic composition. The NH moiety of the piperazine group capped the Ag/Au surfaces, as revealed by spectroscopic studies. The synthesized nanoparticles were also assessed for urease inhibition potential. Fascinatingly, both Ag-cip and Au-cip NPs exhibited significant urease enzyme inhibitory potential, with IC50 = 1.181 ± 0.02 µg/mL and 52.55 ± 2.3 µg/mL, compared to ciprofloxacin (IC50 = 82.95 ± 1.62 µg/mL). MNPs also exhibited significant antibacterial activity against selected bacterial strains. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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6825 KiB  
Article
Self-Assembled Modified Soy Protein/Dextran Nanogel Induced by Ultrasonication as a Delivery Vehicle for Riboflavin
by Bei Jin, Xiaosong Zhou, Xiangzhong Li, Weiqin Lin, Guangbin Chen and Riji Qiu
Molecules 2016, 21(3), 282; https://doi.org/10.3390/molecules21030282 - 15 Mar 2016
Cited by 51 | Viewed by 7273
Abstract
A simple and green approach was developed to produce a novel nanogel via self-assembly of modified soy protein and dextran, to efficiently deliver riboflavin. First, modified soy protein was prepared by heating denaturation at 60 °C for 30 min or Alcalase hydrolysis for [...] Read more.
A simple and green approach was developed to produce a novel nanogel via self-assembly of modified soy protein and dextran, to efficiently deliver riboflavin. First, modified soy protein was prepared by heating denaturation at 60 °C for 30 min or Alcalase hydrolysis for 40 min. Second, modified soy protein was mixed with dextran and ultrasonicated for 70 min so as to assemble nanogels. The modified soy protein-dextran nanogels were characterized by Fourier-transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS) and ζ-potential studies to confirm the formation of NGs. Transmission electron microscopy (TEM) revealed the NGs to be spherical with core-shell structures, in the range of 32–40 nm size. The nanogels were stable against various environmental conditions. Furthermore, the particle size of the nanogels hardly changed with the incorporation of riboflavin. The encapsulation efficiency of nanogels was found to be up to 65.9% at a riboflavin concentration of 250 μg/mL. The nanogels exhibited a faster release in simulated intestine fluid (SIF) compared with simulated gastric fluid (SGF). From the results obtained it can be concluded that modified soy protein-dextran nanogels can be considered a promising carrier for drugs and other bioactive molecule delivery purposes. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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1897 KiB  
Article
Synthesis, Characterization and in Vitro Evaluation of Manganese Ferrite (MnFe2O4) Nanoparticles for Their Biocompatibility with Murine Breast Cancer Cells (4T1)
by Samikannu Kanagesan, Sidek Bin Ab Aziz, Mansor Hashim, Ismayadi Ismail, Subramani Tamilselvan, Noorjahan Banu Binti Mohammed Alitheen, Mallappa Kumara Swamy and Bandaru Purna Chandra Rao
Molecules 2016, 21(3), 312; https://doi.org/10.3390/molecules21030312 - 11 Mar 2016
Cited by 56 | Viewed by 8215
Abstract
Manganese ferrite (MnFe2O4) magnetic nanoparticles were successfully prepared by a sol-gel self-combustion technique using iron nitrate and manganese nitrate, followed by calcination at 150 °C for 24 h. Calcined sample was systematically characterized by X-ray diffraction (XRD), Fourier transform [...] Read more.
Manganese ferrite (MnFe2O4) magnetic nanoparticles were successfully prepared by a sol-gel self-combustion technique using iron nitrate and manganese nitrate, followed by calcination at 150 °C for 24 h. Calcined sample was systematically characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and vibrational sample magnetometry (VSM) in order to identify the crystalline phase, functional group, morphology, particle size, shape and magnetic behavior. It was observed that the resultant spinal ferrites obtained at low temperature exhibit single phase, nanoparticle size and good magnetic behavior. The study results have revealed the existence of a potent dose dependent cytotoxic effect of MnFe2O4 nanoparticles against 4T1 cell lines at varying concentrations with IC50 values of 210, 198 and 171 μg/mL after 24 h, 48 h and 72 h of incubation, respectively. Cells exposed to higher concentrations of nanoparticles showed a progressive increase of apoptotic and necrotic activity. Below 125 μg/mL concentration the nanoparticles were biocompatible with 4T1 cells. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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4052 KiB  
Article
Novel Gold Nanoparticles Reduced by Sargassum glaucescens: Preparation, Characterization and Anticancer Activity
by Zahra Ajdari, Heshu Rahman, Kamyar Shameli, Rasedee Abdullah, Maaruf Abd Ghani, Swee Yeap, Sahar Abbasiliasi, Daniel Ajdari and Arbakariya Ariff
Molecules 2016, 21(3), 123; https://doi.org/10.3390/molecules21030123 - 01 Mar 2016
Cited by 49 | Viewed by 9015
Abstract
The current study investigated the anticancer properties of gold nanoparticles (SG-stabilized AuNPs) synthesized using water extracts of the brown seaweed Sargassum glaucescens (SG). SG-stabilized AuNPs were characterized by ultraviolet-visible spectroscopy, transmission and scanning electron microscopy, and energy dispersive X-ray fluorescence spectrometry. The SG-stabilized [...] Read more.
The current study investigated the anticancer properties of gold nanoparticles (SG-stabilized AuNPs) synthesized using water extracts of the brown seaweed Sargassum glaucescens (SG). SG-stabilized AuNPs were characterized by ultraviolet-visible spectroscopy, transmission and scanning electron microscopy, and energy dispersive X-ray fluorescence spectrometry. The SG-stabilized AuNPs were stable and small at 3.65 ± 1.69 nm in size. The in vitro anticancer effect of SG-stabilized AuNPs was determined on cervical (HeLa), liver (HepG2), breast (MDA-MB-231) and leukemia (CEM-ss) cell lines using fluorescence microscopy, flow cytometry, caspase activity determination, and MTT assays. After 72 h treatment, SG-stabilized AuNPs was shown to be significant (p < 0.05) cytotoxic to the cancer cells in a dose- and time-dependent manner. The IC50 values of SG-stabilized AuNPs on the HeLa, HepG2, CEM-ss, MDA-MB-231 cell lines were 4.75 ± 1.23, 7.14 ± 1.45, 10.32 ± 1.5, and 11.82 ± 0.9 μg/mL, respectively. On the other hand, SG-stabilized AuNPs showed no cytotoxic effect towards the normal human mammary epithelial cells (MCF-10A). SG-stabilized AuNPs significantly (p < 0.05) arrest HeLa cell cycle at G2/M phase and significantly (p < 0.05) activated caspases-3 and -9 activities. The anticancer effect of SG-stabilized AuNPs is via the intrinsic apoptotic pathway. The study showed that SG-stabilized AuNPs is a good candidate to be developed into a chemotherapeutic compound for the treatment of cancers especially cervical cancer. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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2481 KiB  
Article
Exotic Vegetable Oils for Cosmetic O/W Nanoemulsions: In Vivo Evaluation
by Tatiana A. Pereira, Carolina M. Guerreiro, Monica Maruno, Marcio Ferrari and Pedro Alves Rocha-Filho
Molecules 2016, 21(3), 248; https://doi.org/10.3390/molecules21030248 - 24 Feb 2016
Cited by 29 | Viewed by 7082
Abstract
Oil-in-water nanoemulsions are stable systems with droplet sizes in the 20–200 nm range. The physicochemical properties of these systems may be influenced by the addition of additives. Thus, the influence of ethoxylated (EL) and acetylated lanolin (AL) addition on the droplet size, pH [...] Read more.
Oil-in-water nanoemulsions are stable systems with droplet sizes in the 20–200 nm range. The physicochemical properties of these systems may be influenced by the addition of additives. Thus, the influence of ethoxylated (EL) and acetylated lanolin (AL) addition on the droplet size, pH values, electrical conductivity and stability of nanoemulsions was investigated. Then, effect of nano-emulsions additives with EL (NE-EL) or AL (NE-AL) in hydration, oiliness and pH of the skin were evaluated. Nanoemulsion safety was evaluated through the observation of no undesirable effects after skin formulation application. Both additives caused changes in droplet size and electrical conductivity, but not in pH values. Nanoemulsions containing up to 6.0% ethoxylated lanolin and 2.0% acetylated lanolin remained stable after centrifugation tests. Higher concentrations of the additives made the nanoemulsions unstable. Stability tests showed that ethoxylated lanolin produced more stable nanoemulsions then acetylated lanolin and that the major instability phenomenon occurring in these systems is coalescence at elevated temperatures. Nanoemulsion-based lanolin derivatives increased skin hydration and oiliness and did not change cutaneous pH values. These formulations are non-toxic since they did not cause any irritation on the skin surface after nanoemulsion application, showing potential as carriers for pharmaceuticals and cosmetic applications. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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7542 KiB  
Article
Influence of Thermal Treatment Conditions on the Properties of Dental Silicate Cements
by Georgeta Voicu, Alexandru Mihai Popa, Alina Ioana Badanoiu and Florin Iordache
Molecules 2016, 21(2), 233; https://doi.org/10.3390/molecules21020233 - 18 Feb 2016
Cited by 9 | Viewed by 5197
Abstract
In this study the sol-gel process was used to synthesize a precursor mixture for the preparation of silicate cement, also called mineral trioxide aggregate (MTA) cement. This mixture was thermally treated under two different conditions (1400 °C/2 h and 1450 °C/3 h) followed [...] Read more.
In this study the sol-gel process was used to synthesize a precursor mixture for the preparation of silicate cement, also called mineral trioxide aggregate (MTA) cement. This mixture was thermally treated under two different conditions (1400 °C/2 h and 1450 °C/3 h) followed by rapid cooling in air. The resulted material (clinker) was ground for one hour in a laboratory planetary mill (v = 150 rot/min), in order to obtain the MTA cements. The setting time and mechanical properties, in vitro induction of apatite formation by soaking in simulated body fluid (SBF) and cytocompatibility of the MTA cements were assessed in this study. The hardening processes, nature of the reaction products and the microstructural characteristics were also investigated. The anhydrous and hydrated cements were characterized by different techniques e.g., X-ray diffraction (XRD), scanning electron microscopy (SEM), infrared spectroscopy (FT-IR) and thermal analysis (DTA-DTG-TG). The setting time of the MTA cement obtained by thermal treatment at 1400 °C/2 h (MTA1) was 55 min and 15 min for the MTA cement obtained at 1450 °C/3 h (MTA2). The compressive strength values were 18.5 MPa (MTA1) and 22.9 MPa (MTA2). Both MTA cements showed good bioactivity (assessed by an in vitro test), good cytocompatibility and stimulatory effect on the proliferation of cells. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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1557 KiB  
Article
Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
by Giovana Aparecida de Souza Cintra, Larissa Alvarenga Pinto, Giovana Maria Fioramonti Calixto, Christiane Pienna Soares, Eliete De Souza Von Zuben, Maria Virgínia Scarpa, Maria Palmira Daflon Gremião and Marlus Chorilli
Molecules 2016, 21(2), 231; https://doi.org/10.3390/molecules21020231 - 18 Feb 2016
Cited by 32 | Viewed by 6292
Abstract
Methotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) [...] Read more.
Methotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) and a liquid crystalline system (LCS), consisting of a glycol copolymer-based silicone fluid (SFGC) as oil phase, polyether functional siloxane (PFS) as surfactant, and carbomer homopolymer type A (C971) dispersion at 0.5% (wt/wt) as aqueous phase. Polarized light microscopy and small-angle X-ray scattering evidenced the presence of hexagonal and lamellar LCSs, and also a ME. Texture profile and in vitro bioadhesion assays showed that these formulations are suitable for topical application, showing interesting hardness, adhesiveness and compressibility values. Rheology analysis confirmed the Newtonian behaviour of the ME, whereas lamellar and hexagonal LCSs behave as pseudoplastic and dilatant non-Newtonian fluids, respectively. In vitro release profiles indicated that MTX could be released in a controlled manner from all the systems, and the Weibull model showed the highest adjusted coefficient of determination. Finally, the formulations were not cytotoxic to the immortalized human keratinocyte line HaCaT. Therefore, these bioadhesive surfactant systems established with PFS and C971 have great potential as skin delivery systems. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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1958 KiB  
Article
Bioactive ZnO Coatings Deposited by MAPLE—An Appropriate Strategy to Produce Efficient Anti-Biofilm Surfaces
by Alexandra Elena Oprea, Loredana Mihaela Pandel, Ana Maria Dumitrescu, Ecaterina Andronescu, Valentina Grumezescu, Mariana Carmen Chifiriuc, Laurenţiu Mogoantă, Tudor-Adrian Bălşeanu, George Dan Mogoşanu, Gabriel Socol, Alexandru Mihai Grumezescu, Florin Iordache, Horia Maniu, Mariana Chirea and Alina Maria Holban
Molecules 2016, 21(2), 220; https://doi.org/10.3390/molecules21020220 - 16 Feb 2016
Cited by 24 | Viewed by 5665
Abstract
Deposition of bioactive coatings composed of zinc oxide, cyclodextrin and cefepime (ZnO/CD/Cfp) was performed by the Matrix Assisted Pulsed Laser Evaporation (MAPLE) technique. The obtained nanostructures were characterized by X-ray diffraction, IR microscopy and scanning electron microscopy. The efficient release of cefepime was [...] Read more.
Deposition of bioactive coatings composed of zinc oxide, cyclodextrin and cefepime (ZnO/CD/Cfp) was performed by the Matrix Assisted Pulsed Laser Evaporation (MAPLE) technique. The obtained nanostructures were characterized by X-ray diffraction, IR microscopy and scanning electron microscopy. The efficient release of cefepime was correlated with an increased anti-biofilm activity of ZnO/CD/Cfp composites. In vitro and in vivo tests have revealed a good biocompatibility of ZnO/CD/Cfp coatings, which recommend them as competitive candidates for the development of antimicrobial surfaces with biomedical applications. The release of the fourth generation cephalosporin Cfp in a biologically active form from the ZnO matrix could help preventing the bacterial adhesion and the subsequent colonization and biofilm development on various surfaces, and thus decreasing the risk of biofilm-related infections. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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870 KiB  
Article
New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
by Malwina Lachowicz, Michał Kołodziejczyk, Marek Lukosek, Jacek Kosno, Paulina Olszewska and Paweł Szymański
Molecules 2016, 21(2), 197; https://doi.org/10.3390/molecules21020197 - 06 Feb 2016
Cited by 7 | Viewed by 5136
Abstract
As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class [...] Read more.
As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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1191 KiB  
Article
Design and Characterization of a Novel p1025 Peptide-Loaded Liquid Crystalline System for the Treatment of Dental Caries
by Giovana Maria Fioramonti Calixto, Matheus Henrique Garcia, Eduardo Maffud Cilli, Leila Aparecida Chiavacci and Marlus Chorilli
Molecules 2016, 21(2), 158; https://doi.org/10.3390/molecules21020158 - 28 Jan 2016
Cited by 27 | Viewed by 5186
Abstract
Dental caries, mainly caused by the adhesion of Streptococcus mutans to pellicle-coated tooth surfaces, is an important public health problem worldwide. A synthetic peptide (p1025) corresponding to residues 1025–1044 of the adhesin can inhibit this binding. Peptides are particularly susceptible to the biological [...] Read more.
Dental caries, mainly caused by the adhesion of Streptococcus mutans to pellicle-coated tooth surfaces, is an important public health problem worldwide. A synthetic peptide (p1025) corresponding to residues 1025–1044 of the adhesin can inhibit this binding. Peptides are particularly susceptible to the biological environment; therefore, a p1025 peptide-loaded liquid crystalline system (LCS) consisting of tea tree oil as the oil phase, polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol as the surfactant, and water or 0.5% polycarbophil polymer dispersions as the aqueous phase was employed as a drug delivery platform. This system exhibited anticaries and bioadhesive properties and provided a protective environment to p1025 at the site of action, thereby modulating its action, prolonging its contact with the teeth, and decreasing the frequency of administration. LCSs were characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), and rheological, texture, and bioadhesive tests. PLM and SAXS revealed the presence of hexagonal liquid crystalline phases and microemulsions. Rheological analyses demonstrated that the addition of polymer dispersions favored characteristics such as shear thinning and thixotropy, hence improving buccal application. Bioadhesion tests showed that polymer dispersions contributed to the adhesion onto the teeth. Taken together, LCS could provide a novel pharmaceutical nanotechnology platform for dental caries treatment. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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4515 KiB  
Article
Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
by Roberta B. Rigon, Naiara Fachinetti, Patrícia Severino, Maria H. A. Santana and Marlus Chorilli
Molecules 2016, 21(1), 116; https://doi.org/10.3390/molecules21010116 - 20 Jan 2016
Cited by 78 | Viewed by 7841
Abstract
The aim of this study was to evaluate the skin delivery and in vitro biological activity of trans-resveratrol (RES)-loaded solid lipid nanoparticles (SLNs). The SLNs were composed of stearic acid, poloxamer 407, soy phosphatidylcholine (SPC), an aqueous phase and 0.1% RES. The [...] Read more.
The aim of this study was to evaluate the skin delivery and in vitro biological activity of trans-resveratrol (RES)-loaded solid lipid nanoparticles (SLNs). The SLNs were composed of stearic acid, poloxamer 407, soy phosphatidylcholine (SPC), an aqueous phase and 0.1% RES. The particle size, polydispersity index (PdI) and zeta potential were analyzed by dynamic light scattering (DLS). The SLNs were analyzed by scanning electron microscopy (SEM-FEG) and differential scanning calorimetry (DSC). In vitro RES-SLN skin permeation/retention assays were conducted, and their tyrosinase inhibitory activity was evaluated. An MTT reduction assay was performed on HaCat keratinocytes to determine in vitro cytotoxicity. The formulations had average diameter lower than 200 nm, the addition of SPC promoted increases in PdI in the RES-SLNs, but decreases PdI in the RES-free SLNs and the formulations exhibited zeta potentials smaller than −3 mV. The DSC analysis of the SLNs showed no endothermic peak attributable to RES. Microscopic analysis suggests that the materials formed had nanometric size distribution. Up to 45% of the RES permeated through the skin after 24 h. The RES-loaded SLNs were more effective than kojic acid at inhibiting tyrosinase and proved to be non-toxic in HaCat keratinocytes. The results suggest that the investigated RES-loaded SLNs have potential use in skin disorder therapies. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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6193 KiB  
Article
Biocompatible 3D Matrix with Antimicrobial Properties
by Alberto Ion, Ecaterina Andronescu, Dragoș Rădulescu, Marius Rădulescu, Florin Iordache, Bogdan Ștefan Vasile, Adrian Vasile Surdu, Madalina Georgiana Albu, Horia Maniu, Mariana Carmen Chifiriuc, Alexandru Mihai Grumezescu and Alina Maria Holban
Molecules 2016, 21(1), 115; https://doi.org/10.3390/molecules21010115 - 20 Jan 2016
Cited by 7 | Viewed by 6045
Abstract
The aim of this study was to develop, characterize and assess the biological activity of a new regenerative 3D matrix with antimicrobial properties, based on collagen (COLL), hydroxyapatite (HAp), β-cyclodextrin (β-CD) and usnic acid (UA). The prepared 3D matrix was characterized by Scanning [...] Read more.
The aim of this study was to develop, characterize and assess the biological activity of a new regenerative 3D matrix with antimicrobial properties, based on collagen (COLL), hydroxyapatite (HAp), β-cyclodextrin (β-CD) and usnic acid (UA). The prepared 3D matrix was characterized by Scanning Electron Microscopy (SEM), Fourier Transform Infrared Microscopy (FT-IRM), Transmission Electron Microscopy (TEM), and X-ray Diffraction (XRD). In vitro qualitative and quantitative analyses performed on cultured diploid cells demonstrated that the 3D matrix is biocompatible, allowing the normal development and growth of MG-63 osteoblast-like cells and exhibited an antimicrobial effect, especially on the Staphylococcus aureus strain, explained by the particular higher inhibitory activity of usnic acid (UA) against Gram positive bacterial strains. Our data strongly recommend the obtained 3D matrix to be used as a successful alternative for the fabrication of three dimensional (3D) anti-infective regeneration matrix for bone tissue engineering. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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1953 KiB  
Article
Peptide KSL-W-Loaded Mucoadhesive Liquid Crystalline Vehicle as an Alternative Treatment for Multispecies Oral Biofilm
by Jéssica Bernegossi, Giovana Maria Fioramonti Calixto, Paulo Ricardo da Silva Sanches, Carla Raquel Fontana, Eduardo Maffud Cilli, Saulo Santesso Garrido and Marlus Chorilli
Molecules 2016, 21(1), 37; https://doi.org/10.3390/molecules21010037 - 25 Dec 2015
Cited by 37 | Viewed by 6372
Abstract
Decapeptide KSL-W shows antibacterial activities and can be used in the oral cavity, however, it is easily degraded in aqueous solution and eliminated. Therefore, we aimed to develop liquid crystalline systems (F1 and F2) for KSL-W buccal administration to treat multispecies oral biofilms. [...] Read more.
Decapeptide KSL-W shows antibacterial activities and can be used in the oral cavity, however, it is easily degraded in aqueous solution and eliminated. Therefore, we aimed to develop liquid crystalline systems (F1 and F2) for KSL-W buccal administration to treat multispecies oral biofilms. The systems were prepared with oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20), and a 1% poloxamer 407 dispersion as the oil phase (OP), surfactant (S), and aqueous phase (AP), respectively. We characterized them using polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheology, and in vitro bioadhesion, and performed in vitro biological analysis. PLM showed isotropy (F1) or anisotropy with lamellar mesophases (F2), confirmed by peak ratio quantification using SAXS. Rheological tests demonstrated that F1 exhibited Newtonian behavior but not F2, which showed a structured AP concentration-dependent system. Bioadhesion studies revealed an AP concentration-dependent increase in the system’s bioadhesiveness (F2 = 15.50 ± 1.00 mN·s) to bovine teeth blocks. Antimicrobial testing revealed 100% inhibition of multispecies oral biofilm growth after KSL-W administration, which was incorporated in the F2 aqueous phase at a concentration of 1 mg/mL. Our results suggest that this system could serve as a potential vehicle for buccal administration of antibiofilm peptides. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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4799 KiB  
Article
Storage Stability of Kinnow Fruit (Citrus reticulata) as Affected by CMC and Guar Gum-Based Silver Nanoparticle Coatings
by Syed Wasim Ahmad Shah, Muhammad Jahangir, Muhammad Qaisar, Sher Aslam Khan, Talat Mahmood, Muhammad Saeed, Abid Farid and Muhammad Liaquat
Molecules 2015, 20(12), 22645-22661; https://doi.org/10.3390/molecules201219870 - 18 Dec 2015
Cited by 56 | Viewed by 9751
Abstract
The influence of carboxy methyl cellulose (CMC) and guargum-based coatings containing silver nanoparticles was studied on the postharvest storage stability of the kinnow mandarin (Citrus reticulata cv. Blanco) for a period of 120 days (85%–90% relative humidity) at 4 °C and 10 [...] Read more.
The influence of carboxy methyl cellulose (CMC) and guargum-based coatings containing silver nanoparticles was studied on the postharvest storage stability of the kinnow mandarin (Citrus reticulata cv. Blanco) for a period of 120 days (85%–90% relative humidity) at 4 °C and 10 °C. Physicochemical and microbiological qualities were monitored after every 15 days of storage. Overall results revealed an increase in total soluble solid (TSS), total sugars, reducing sugars and weight loss but this increase was comparatively less significant in coated fruits stored at 4 °C. Ascorbic acid, total phenolics, and antioxidant activity was significantly enhanced in coated fruits stored at 4 °C. Titratable acidity significantly decreased during storage except for coated kinnow stored at 4 °C. In control samples stored at 10 °C, high intensity of fruit rotting and no chilling injury was observed. Total aerobic psychrotrophic bacteria and yeast and molds were noticed in all treatments during storage but the growth was not significant in coated fruits at 4 °C. Kinnow fruit can be kept in good quality after coating for four months at 4 °C and for 2 months at 10 °C. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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5589 KiB  
Article
Green Chemistry Approach for Synthesis of Effective Anticancer Palladium Nanoparticles
by Sangiliyandi Gurunathan, EunSu Kim, Jae Woong Han, Jung Hyun Park and Jin-Hoi Kim
Molecules 2015, 20(12), 22476-22498; https://doi.org/10.3390/molecules201219860 - 15 Dec 2015
Cited by 89 | Viewed by 10245
Abstract
The purpose of this study was to design and synthesize Palladium nanoparticles (PdNPs) using an environmentally friendly approach and evaluate the in vitro efficacy of PdNPs in human ovarian cancer A2780 cells. Ultraviolet-Visible (UV-Vis) spectroscopy was used to monitor the conversion of Pd(II) [...] Read more.
The purpose of this study was to design and synthesize Palladium nanoparticles (PdNPs) using an environmentally friendly approach and evaluate the in vitro efficacy of PdNPs in human ovarian cancer A2780 cells. Ultraviolet-Visible (UV-Vis) spectroscopy was used to monitor the conversion of Pd(II) ions to Pd(0)NPs. X-ray diffraction (XRD) revealed the crystallinity of the as-synthesized PdNPs and Fourier transform infrared spectroscopy (FTIR) further confirmed the role of the leaf extract of Evolvulus alsinoides as a reducing and stabilizing agent for the synthesis of PdNPs. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) showed that the average size of the NPs was 5 nm. After a 24-h exposure to PdNPs, cell viability and light microscopy assays revealed the dose-dependent toxicity of the PdNPs. Furthermore, the dose-dependent cytotoxicity of the PdNPs was confirmed by lactate dehydrogenase (LDH), increased reactive oxygen species (ROS) generation, activation of PdNPs-induced autophagy, impairment of mitochondrial membrane potential (MMP), enhanced caspase-3 activity, and detection of TUNEL-positive cells. Our study demonstrates a single, simple, dependable and green approach for the synthesis of PdNPs using leaf extracts of Evolvulus alsinoides. Furthermore, the in vitro efficacy of PdNPs in human ovarian cancer cells suggests that it could be an effective therapeutic agent for cancer therapy. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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942 KiB  
Article
Production of Nanoemulsions from Palm-Based Tocotrienol Rich Fraction by Microfluidization
by Pik Seah Goh, Mei Han Ng, Yuen May Choo, Nasrulhaq Boyce Amru and Cheng Hock Chuah
Molecules 2015, 20(11), 19936-19946; https://doi.org/10.3390/molecules201119666 - 05 Nov 2015
Cited by 36 | Viewed by 6887
Abstract
In the present study, tocotrienol rich fraction (TRF) nanoemulsions were produced as an alternative approach to improve solubility and absorption of tocotrienols. In the present study, droplet size obtained after 10 cycles of homogenization with increasing pressure was found to decrease from 120 [...] Read more.
In the present study, tocotrienol rich fraction (TRF) nanoemulsions were produced as an alternative approach to improve solubility and absorption of tocotrienols. In the present study, droplet size obtained after 10 cycles of homogenization with increasing pressure was found to decrease from 120 to 65.1 nm. Nanoemulsions stabilized with Tween series alone or emulsifier blend Brij 35:Span 80 (0.6:0.4 w/w) homogenized at 25,000 psi and 10 cycles, produced droplet size less than 100 nm and a narrow size distribution with a polydispersity index (PDI) value lower than 0.2. However blend of Tween series with Span 80 produced nanoemulsions with droplet size larger than 200 nm. This work has also demonstrated the amount of tocols losses in TRF nanoemulsion stabilized Tweens alone or emulsifier blend Brij 35:Span 80 (0.6:0.4 w/w) ranged between 3%–25%. This can be attributed to the interfacial film formed surrounding the droplets exhibited different level of oxidative stability against heat and free radicals created during high pressure emulsification. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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Review

Jump to: Research

877 KiB  
Review
Nanotechnology-Based Drug Delivery Systems for Photodynamic Therapy of Cancer: A Review
by Giovana Maria Fioramonti Calixto, Jéssica Bernegossi, Laura Marise De Freitas, Carla Raquel Fontana and Marlus Chorilli
Molecules 2016, 21(3), 342; https://doi.org/10.3390/molecules21030342 - 11 Mar 2016
Cited by 381 | Viewed by 25495
Abstract
Photodynamic therapy (PDT) is a promising alternative approach for improved cancer treatment. In PDT, a photosensitizer (PS) is administered that can be activated by light of a specific wavelength, which causes selective damage to the tumor and its surrounding vasculature. The success of [...] Read more.
Photodynamic therapy (PDT) is a promising alternative approach for improved cancer treatment. In PDT, a photosensitizer (PS) is administered that can be activated by light of a specific wavelength, which causes selective damage to the tumor and its surrounding vasculature. The success of PDT is limited by the difficulty in administering photosensitizers (PSs) with low water solubility, which compromises the clinical use of several molecules. Incorporation of PSs in nanostructured drug delivery systems, such as polymeric nanoparticles (PNPs), solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), gold nanoparticles (AuNPs), hydrogels, liposomes, liquid crystals, dendrimers, and cyclodextrin is a potential strategy to overcome this difficulty. Additionally, nanotechnology-based drug delivery systems may improve the transcytosis of a PS across epithelial and endothelial barriers and afford the simultaneous co-delivery of two or more drugs. Based on this, the application of nanotechnology in medicine may offer numerous exciting possibilities in cancer treatment and improve the efficacy of available therapeutics. Therefore, the aim of this paper is to review nanotechnology-based drug delivery systems for photodynamic therapy of cancer. Full article
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
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