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Nanomaterials
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Implementation of Nanomaterials for Drug Delivery
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Implementation of Nanomaterials for Drug Delivery

A special issue of Nanomaterials (ISSN 2079-4991).

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 21253

Special Issue Editor

Dr. Carly S. Filgueira

E-Mail Website
Guest Editor
Departments of Nanomedicine and Cardiovascular Surgery, Houston Methodist Research Institute (HMRI), Houston, TX, USA
Interests: alternative treatment approaches; physiological disorders; sustained release harnessing; nanotechnological approaches

Special Issue Information

Dear Colleagues,

Nanomaterials have sparked a new era of therapeutic interventions. By engineering nanomaterials, the obstacles of conventional therapeutic intervention can be surpassed through sustained release, targeted drug therapy, and local delivery to a specific site of action. Local delivery improves the bioavailability of the therapeutic and reduces off-target adverse effects. Nanomaterials, such as those composed of lipids or polymers, can be used to carry drugs. Inorganic nanomaterials, such as those made of metals, can be readily functionalized and act as therapeutic modalities through photothermal and photoacoustic properties as well as radiative enhancement effects. Nanoparticles also offer a means to transport agents to diseased cells or tissues or act as diagnostic tools. Implantable devices with specially designed nanochannels allow for controlled and sustained release of therapeutics from a drug reservoir near a target site, minimizing adverse effects associated with systemic drug exposure. This Special Issue aims to explore the use of nanomedicine and nanomaterials to enhance therapeutic delivery. In harnessing nanotechnology, which consists of small, highly tunable platforms, we can develop effective therapeutics, devices, and techniques to vastly improve drug delivery and improve therapeutic outcomes.

Dr. Carly S. Filgueira
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Nanomaterials 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 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

  • drug delivery
  • implantable devices
  • targeted therapy
  • nanocarriers
  • nanomedicine
  • site-specific drug action
  • sustained release

Published Papers (6 papers)

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Research

30 pages, 8807 KiB  
Article
Dissolution Enhancement and Controlled Release of Paclitaxel Drug via a Hybrid Nanocarrier Based on mPEG-PCL Amphiphilic Copolymer and Fe-BTC Porous Metal-Organic Framework
by Nikolaos D. Bikiaris, Nina Maria Ainali, Evi Christodoulou, Margaritis Kostoglou, Thomas Kehagias, Emilia Papasouli, Emmanuel N. Koukaras and Stavroula G. Nanaki
Nanomaterials 2020, 10(12), 2490; https://doi.org/10.3390/nano10122490 - 11 Dec 2020
Cited by 17 | Viewed by 3782
Abstract
In the present work, the porous metal-organic framework (MOF) Basolite®F300 (Fe-BTC) was tested as a potential drug-releasing depot to enhance the solubility of the anticancer drug paclitaxel (PTX) and to prepare controlled release formulations after its encapsulation in amphiphilic methoxy poly(ethylene [...] Read more.
In the present work, the porous metal-organic framework (MOF) Basolite®F300 (Fe-BTC) was tested as a potential drug-releasing depot to enhance the solubility of the anticancer drug paclitaxel (PTX) and to prepare controlled release formulations after its encapsulation in amphiphilic methoxy poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) nanoparticles. Investigation revealed that drug adsorption in Fe-BTC reached approximately 40%, a relatively high level, and also led to an overall drug amorphization as confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The dissolution rate of PTX-loaded MOF was substantially enhanced achieving a complete (100%) release within four days, while the neat drug only reached a 13% maximum rate (3–4 days). This PTX-Fe-BTC nanocomposite was further encapsulated into a mPEG-PCL matrix, a typical aliphatic amphiphilic copolyester synthesized in our lab, whose biocompatibility was validated by in vitro cytotoxicity tests toward human umbilical vein endothelial cells (HUVEC). Encapsulation was performed according to the solid-in-oil-in-water emulsion/solvent evaporation technique, resulting in nanoparticles of about 143 nm, slightly larger of those prepared without the pre-adsorption of PTX on Fe-BTC (138 nm, respectively). Transmission electron microscopy (TEM) imaging revealed that spherical nanoparticles with embedded PTX-loaded Fe-BTC nanoparticles were indeed fabricated, with sizes ranging from 80 to 150 nm. Regions of the composite Fe-BTC-PTX system in the infrared (IR) spectrum are identified as signatures of the drug-MOF interaction. The dissolution profiles of all nanoparticles showed an initial burst release, attributed to the drug amount located at the nanoparticles surface or close to it, followed by a steadily and controlled release. This is corroborated by computational analysis that reveals that PTX attaches effectively to Fe-BTC building blocks, but its relatively large size limits diffusion through crystalline regions of Fe-BTC. The dissolution behaviour can be described through a bimodal diffusivity model. The nanoparticles studied could serve as potential chemotherapeutic candidates for PTX delivery. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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25 pages, 9089 KiB  
Article
Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients
by Olga Pelikh and Cornelia M. Keck
Nanomaterials 2020, 10(11), 2323; https://doi.org/10.3390/nano10112323 - 23 Nov 2020
Cited by 32 | Viewed by 4170
Abstract
Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, [...] Read more.
Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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15 pages, 6238 KiB  
Article
Silver Nanoparticles Agglomerate Intracellularly Depending on the Stabilizing Agent: Implications for Nanomedicine Efficacy
by Marina R. Mulenos, Henry Lujan, Lauren R. Pitts and Christie M. Sayes
Nanomaterials 2020, 10(10), 1953; https://doi.org/10.3390/nano10101953 - 30 Sep 2020
Cited by 20 | Viewed by 2408
Abstract
Engineered nanoparticles are utilized as drug delivery carriers in modern medicine due to their high surface area and tailorable surface functionality. After in vivo administration, nanoparticles distribute and interact with biomolecules, such as polar proteins in serum, lipid membranes in cells, and high [...] Read more.
Engineered nanoparticles are utilized as drug delivery carriers in modern medicine due to their high surface area and tailorable surface functionality. After in vivo administration, nanoparticles distribute and interact with biomolecules, such as polar proteins in serum, lipid membranes in cells, and high ionic conditions during digestion. Electrostatic forces and steric hindrances in a nanoparticle population are disturbed and particles agglomerate in biological fluids. Little is known about the stability of nanoparticles in relation to particle surface charge. Here, we compared three different surface-stabilized silver nanoparticles (50 nm) for intracellular agglomeration in human hepatocellular carcinoma cells (HepG2). Nanoparticles stabilized with branched polyethyleneimine conferred a positive surface charge, particles stabilized with lipoic acid conferred a negative surface charge, and particles stabilized with polyethylene glycol conferred a neutral surface charge. Particles were incubated in fetal bovine serum, simulated lung surfactant fluid, and simulated stomach digestion fluid. Each nanoparticle system was characterized via microscopic (transmission electron, fluorescence, and enhanced darkfield) and spectroscopic (hyperspectral, dynamic light scattering, and ultraviolet-visible absorption) techniques. Results showed that nanoparticle transformation included cellular internalization, agglomeration, and degradation and that these changes were dependent upon surface charge and incubation matrix. Hyperspectral analyses showed that positively charged silver nanoparticles red-shifted in spectral analysis after transformations, whereas negatively charged silver nanoparticles blue-shifted. Neutrally charged silver nanoparticles did not demonstrate significant spectral shifts. Spectral shifting indicates de-stabilization in particle suspension, which directly affects agglomeration intracellularly. These characteristics are translatable to critical quality attributes and can be exploited when developing nano-carriers for nanomedicine. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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17 pages, 2254 KiB  
Article
Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile
by Haniza Hassan, Ramatu Omenesa Bello, Siti Khadijah Adam, Ekram Alias, Meor Mohd Redzuan Meor Mohd Affandi, Ahmad Fuad Shamsuddin and Rusliza Basir
Nanomaterials 2020, 10(9), 1785; https://doi.org/10.3390/nano10091785 - 09 Sep 2020
Cited by 20 | Viewed by 3825
Abstract
Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infection. Its oral bioavailability is low; therefore, frequent and high doses are prescribed for optimum therapeutic efficacy. Moreover, the current therapeutic regimen of acyclovir is associated with unwarranted adverse effects, [...] Read more.
Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infection. Its oral bioavailability is low; therefore, frequent and high doses are prescribed for optimum therapeutic efficacy. Moreover, the current therapeutic regimen of acyclovir is associated with unwarranted adverse effects, hence prompting the need for a suitable drug carrier to overcome these limitations. This study aimed to develop solid lipid nanoparticles (SLNs) as acyclovir carriers and evaluate their in vivo pharmacokinetic parameters to prove the study hypothesis. During the SLN development process, response surface methodology was exploited to optimize the composition of solid lipid and surfactant. Optimum combination of Biogapress Vegetal 297 ATO and Tween 80 was found essential to produce SLNs of 134 nm. The oral bioavailability study showed that acyclovir-loaded SLNs possessed superior oral bioavailability when compared with the commercial acyclovir suspension. The plasma concentration of acyclovir-loaded SLNs was four-fold higher than the commercial suspension. Thus, this investigation presented promising results that the method developed for encapsulation of acyclovir offers potential as an alternative pathway to enhance the drug’s bioavailability. In conclusion, this study exhibited the feasibility of SLNs as an oral delivery vehicle for acyclovir and therefore represents a new promising therapeutic concept of acyclovir treatment via a nanoparticulate drug delivery system. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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9 pages, 1459 KiB  
Article
Gold Nanoparticles Radio-Sensitize and Reduce Cell Survival in Lewis Lung Carcinoma
by Arvind Pandey, Veronica Vighetto, Nicola Di Marzio, Francesca Ferraro, Matteo Hirsch, Nicola Ferrante, Sankar Mitra, Alessandro Grattoni and Carly S. Filgueira
Nanomaterials 2020, 10(9), 1717; https://doi.org/10.3390/nano10091717 - 30 Aug 2020
Cited by 14 | Viewed by 3167
Abstract
It has been suggested that particle size plays an important role in determining the genotoxicity of gold nanoparticles (GNPs). The purpose of this study was to compare the potential radio-sensitization effects of two different sized GNPs (3.9 and 37.4 nm) fabricated and examined [...] Read more.
It has been suggested that particle size plays an important role in determining the genotoxicity of gold nanoparticles (GNPs). The purpose of this study was to compare the potential radio-sensitization effects of two different sized GNPs (3.9 and 37.4 nm) fabricated and examined in vitro in Lewis lung carcinoma (LLC) as a model of non-small cell lung cancer through use of comet and clonogenic assays. After treatment with 2Gy X-ray irradiation, both particle sizes demonstrated increased DNA damage when compared to treatment with particles only and radiation alone. This radio-sensitization was further translated into a reduction in cell survival demonstrated by clonogenicity. This work indicates that GNPs of both sizes induce DNA damage in LLC cells at the tested concentrations, whereas the 37.4 nm particle size treatment group demonstrated greater significance in vitro. The presented data aids in the evaluation of the radiobiological response of Lewis lung carcinoma cells treated with gold nanoparticles. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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17 pages, 2691 KiB  
Article
Oral Bioavailability Enhancement of Raloxifene with Nanostructured Lipid Carriers
by Aditya Murthy, Punna Rao Ravi, Himanshu Kathuria and Shrinivas Malekar
Nanomaterials 2020, 10(6), 1085; https://doi.org/10.3390/nano10061085 - 31 May 2020
Cited by 40 | Viewed by 3013
Abstract
Raloxifene hydrochloride (RLX) shows poor bioavailability (<2%), high inter-patient variability and extensive gut metabolism (>90%). The objective of this study was to develop nanostructured lipid carriers (NLCs) for RLX to enhance its bioavailability. The NLC formulations were produced with glyceryl tribehenate and oleic [...] Read more.
Raloxifene hydrochloride (RLX) shows poor bioavailability (<2%), high inter-patient variability and extensive gut metabolism (>90%). The objective of this study was to develop nanostructured lipid carriers (NLCs) for RLX to enhance its bioavailability. The NLC formulations were produced with glyceryl tribehenate and oleic acid. The particle characteristics, entrapment efficiency (EE), differential scanning calorimetry (DSC), in vitro drug release, oral bioavailability (in rats) and stability studies were performed. The optimized nanoparticles were 120 ± 3 nm in size with positive zeta potential (14.4 ± 0.5 mV); % EE was over 90% with the drug loading of 5%. The RLX exists in an amorphous form in the lipid matrix. The optimized RLX-NLC formulation showed sustained release in vitro. The RLX-NLC significantly (p < 0.05) enhanced oral bioavailability 3.19-fold as compared to RLX-free suspension in female Wistar rats. The RLX-NLC can potentially enhance the oral bioavailability of RLX. It can also improve the storage stability. Full article
(This article belongs to the Special Issue Implementation of Nanomaterials for Drug Delivery)
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