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Nanotechnology in Drug Delivery

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Materials Science".

Deadline for manuscript submissions: closed (20 February 2018) | Viewed by 84668

Special Issue Editors

Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Avda. Joan XXIII, 27-31, 08028 Barcelona, Spain
Interests: colloids; micelles; layer-by-layer; liposomes; magnetic particles; drug delivery; magnetic hyperthermia; magnetic photothermia
Special Issues, Collections and Topics in MDPI journals
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Avda. Joan XXIII, 27-31, 08028 Barcelona, Spain
Interests: colloidal systems; liposomes; Langmuir–Blodgett films; membrane models; drug delivery; surfaces; magnetic nanoparticles; prussian blue nanoparticles; liposomes; magnetoliposomes
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nanotechnology creates and applies structures and systems, nanomaterials, with specific functions attributable to their size. Nanomaterials possess physicochemical properties that make them excellent candidates for biomedical applications, so in diagnostic as in therapy. In recent years, nanotechnology has shed new light on the delivering strategies, since nanotechnology offers the possibility of designing novel drugs with greater cell specificity. Nanotechnology can produce multifunctional drug carrier nanomaterials that act selectively on specific targets. Moreover, the nanomaterials can protect the drug against both inactivation and degradation. In this way, the application of nanotechnology to drug delivery will have a high clinical impact for the near future, since controlled release of drugs from nanomaterials affords opportunities in cancer therapy and in other diseases. The potential of drug delivery systems based on the use of nanomaterials stems from significant advantages such as: (1) an improved delivery of poorly water-soluble drugs; (2) a modification of the pharmacokinetics of the releasing of the drug; (3) the ability to target specific locations in the body; (4) the reduction of the quantity of drug needed to attain a particular concentration in the vicinity of the target; and (5) the reduction of the concentration of the drug at the non-target sites minimizing severe side effects. Nanomaterials can act at the tissue or cellular level. The latter implies that they can be endocytosed or phagocytosed resulting in internalization of the nanomaterials. In this process, the nanomaterials can reach beyond the cytoplasmic membrane and, in some cases, also beyond the nuclear membrane (i.e., transfection applications). Different nanomaterials can be used for drug delivery applications: dendrimers, micelles, nanoemulsions, liposomes, nanoparticulate systems, nanobottles. Such systems can be combined with hard nanoparticles, i.e., magnetic particles, and the resulting hybrid particles combine the properties of their cores with those of the soft nanomaterials that form the shell. Furthermore, nanotechnology allows to us to prepare stimuli-responsive devices that deliver a drug in spatial, temporal- and dosage-controlled fashions. Nanoscale stimuli-responsive systems are able to control drug biodistribution in response to specific stimuli. These stimuli are categorized into two main types: Exogenous (variation in temperature, magnetic field, ultrasound intensity, light or electric pulses) or endogenous (changes in pH, enzyme concentration or redox gradients). Since important intracellular environment differences in pH value, redox state, and amounts of biomolecules exist between the tumor tissues and the normal tissues, these gradients are an ideal trigger for controlled release and enhanced specificity against tumor cells. On the other hand, exogenous stimuli can be applied at the disease location for achieving the drug release.

We invite researchers to contribute original and review articles regarding the impact of nanotechnology on drug delivery. Potential topics include, but are not limited to:

·         Colloidal particles
·         Liposomes
·         Magnetoliposomes
·         Micelles
·         Polymeric micelles
·         Dendrimers
·         Micro and nanogeles
·         Nanobottles
·         Nanocapsules
·         Magnetic nanoparticles
·         Stimuli-responsive drug delivery
·         pH-responsive drug delivery
·         Temperature-responsive drug delivery
·         Magnetic-responsive drug delivery
·         Targeted delivery to the brain

Prof. Dr. Joan Estelrich
Dr. Maria Antònia Busquets
Guest Editors

Manuscript Submission Information

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Published Papers (12 papers)

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Research

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19 pages, 4500 KiB  
Article
Preparation and Characterization of Electrostatically Crosslinked Polymer–Liposomes in Anticancer Therapy
by Yi-Ting Chiang, Sih-Ying Lyu, Yu-Han Wen and Chun-Liang Lo
Int. J. Mol. Sci. 2018, 19(6), 1615; https://doi.org/10.3390/ijms19061615 - 30 May 2018
Cited by 14 | Viewed by 4030
Abstract
pH-sensitive polymer–liposomes can rapidly release their payloads. However, it is difficult to simultaneously achieve stability and pH-responsiveness in the polymer–liposomes. In this study, stable and pH-sensitive crosslinked polymer–liposomes were fabricated through electrostatic interactions. The pH-sensitive copolymer methoxy poly(ethylene glycol)-block-poly(methacrylic acid)-cholesterol (mPEG- [...] Read more.
pH-sensitive polymer–liposomes can rapidly release their payloads. However, it is difficult to simultaneously achieve stability and pH-responsiveness in the polymer–liposomes. In this study, stable and pH-sensitive crosslinked polymer–liposomes were fabricated through electrostatic interactions. The pH-sensitive copolymer methoxy poly(ethylene glycol)-block-poly(methacrylic acid)-cholesterol (mPEG-b-P(MAAc)-chol) and crosslinking reagent poly(ethylene glycol) with end-capped with lysine (PEG-Lys2) were synthesized and characterized. At physiological conditions, the pH-sensitive copolymers were anionic and interacted electrostatically with the cationic crosslinker PEG-Lys2, forming the electrostatically-crosslinked polymer–liposomes and stabilizing the liposomal structure. At pH 5.0, the carboxylic groups in mPEG-b-P(MAAc)-chol were neutralized, and the liposomal structure was destroyed. The particle size of the crosslinked polymer–liposomes was approximately 140 nm and the polymer–liposomes were loaded with the anticancer drug doxorubicin. At pH 7.4, the crosslinked polymer–liposomes exhibited good stability with steady particle size and low drug leakage, even in the presence of fetal bovine serum. At pH 5.0, the architecture of the crosslinked polymer–liposomes was damaged following rapid drug release, as observed by using transmission electron microscopy and their apparent size variation. The crosslinked polymer–liposomes were pH-sensitive within the endosome and in the human breast cancer cells MDA-MB-231, as determined by using confocal laser scanning microscopy. The intracellular drug release profiles indicated cytotoxicity in cancer cells. These results indicated that the highly-stable and pH-sensitive electrostatically-crosslinked polymer–liposomes offered a potent drug-delivery system for use in anticancer therapies. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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11 pages, 2028 KiB  
Article
Antimalarial Activity of Orally Administered Curcumin Incorporated in Eudragit®-Containing Liposomes
by Elisabet Martí Coma-Cros, Arnau Biosca, Elena Lantero, Maria Letizia Manca, Carla Caddeo, Lucía Gutiérrez, Miriam Ramírez, Livia Neves Borgheti-Cardoso, Maria Manconi and Xavier Fernàndez-Busquets
Int. J. Mol. Sci. 2018, 19(5), 1361; https://doi.org/10.3390/ijms19051361 - 04 May 2018
Cited by 46 | Viewed by 7698
Abstract
Curcumin is an antimalarial compound easy to obtain and inexpensive, having shown little toxicity across a diverse population. However, the clinical use of this interesting polyphenol has been hampered by its poor oral absorption, extremely low aqueous solubility and rapid metabolism. In this [...] Read more.
Curcumin is an antimalarial compound easy to obtain and inexpensive, having shown little toxicity across a diverse population. However, the clinical use of this interesting polyphenol has been hampered by its poor oral absorption, extremely low aqueous solubility and rapid metabolism. In this study, we have used the anionic copolymer Eudragit® S100 to assemble liposomes incorporating curcumin and containing either hyaluronan (Eudragit-hyaluronan liposomes) or the water-soluble dextrin Nutriose® FM06 (Eudragit-nutriosomes). Upon oral administration of the rehydrated freeze-dried nanosystems administered at 25/75 mg curcumin·kg−1·day−1, only Eudragit-nutriosomes improved the in vivo antimalarial activity of curcumin in a dose-dependent manner, by enhancing the survival of all Plasmodium yoelii-infected mice up to 11/11 days, as compared to 6/7 days upon administration of an equal dose of the free compound. On the other hand, animals treated with curcumin incorporated in Eudragit-hyaluronan liposomes did not live longer than the controls, a result consistent with the lower stability of this formulation after reconstitution. Polymer-lipid nanovesicles hold promise for their development into systems for the oral delivery of curcumin-based antimalarial therapies. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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14 pages, 4248 KiB  
Article
Effective Delivery of Arsenic Trioxide to HPV-Positive Cervical Cancer Cells Using Optimised Liposomes: A Size and Charge Study
by Anam Akhtar, Scarlet Xiaoyan Wang, Lucy Ghali, Celia Bell and Xuesong Wen
Int. J. Mol. Sci. 2018, 19(4), 1081; https://doi.org/10.3390/ijms19041081 - 04 Apr 2018
Cited by 19 | Viewed by 3892
Abstract
Despite the success of arsenic trioxide (ATO) in treating haematological malignancies, its potential to treat solid tumours has not been fully exploited, owing to its dose-limiting toxicity and poor pharmacokinetics. In order to overcome this hurdle, liposomal encapsulation of the drug with different [...] Read more.
Despite the success of arsenic trioxide (ATO) in treating haematological malignancies, its potential to treat solid tumours has not been fully exploited, owing to its dose-limiting toxicity and poor pharmacokinetics. In order to overcome this hurdle, liposomal encapsulation of the drug with different surface charges (neutral, negative, and positive) and sizes (100, 200 and 400 nm) were synthesised and tested on human papilloma virus (HPV)-positive HeLa and HPV-negative HT-3 cervical cancer cell lines. Two epithelial cell lines—human keratinocytes (HK) and human colon cells (CRL-1790)—were used as controls. The synthesised liposomes were tested for their physico-chemical characteristics, drug loading efficiency, and toxicity on the studied cell lines. Neutral liposomes of 100 nm in size were the chosen formulation for delivering ATO into the studied cells, as they showed the least intrinsic cytotoxicity and the highest loading efficiency. The findings demonstrated that the optimised formulation of liposomes was an effective drug delivery method for HPV-infected cervical cancer cells. Furthermore, the toxicity vs. uptake ratio was highest for HeLa cells, while a reduced or minimal toxic effect was observed for non-HPV-infected cervical cancer cells and control cells. These findings may provide a promising therapeutic strategy for effectively managing cervical cancers. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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13 pages, 7856 KiB  
Article
Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery
by Nemany Abdelhamid Nemany Hanafy, Alessandra Quarta, Marzia Maria Ferraro, Luciana Dini, Concetta Nobile, Maria Luisa De Giorgi, Sonia Carallo, Cinzia Citti, Antonio Gaballo, Giuseppe Cannazza, Rosaria Rinaldi, Gianluigi Giannelli and Stefano Leporatti
Int. J. Mol. Sci. 2018, 19(3), 748; https://doi.org/10.3390/ijms19030748 - 06 Mar 2018
Cited by 25 | Viewed by 7244
Abstract
LY2157299 (LY), which is very small molecule bringing high cancer diffusion, is a pathway antagonist against TGFβ. LY dosage can be diluted by blood plasma, can be captured by immune system or it might be dissolved during digestion in gastrointestinal tract. The aim [...] Read more.
LY2157299 (LY), which is very small molecule bringing high cancer diffusion, is a pathway antagonist against TGFβ. LY dosage can be diluted by blood plasma, can be captured by immune system or it might be dissolved during digestion in gastrointestinal tract. The aim of our study is to optimize a “nano-elastic” carrier to avoid acidic pH of gastrointestinal tract, colon alkaline pH, and anti-immune recognition. Polygalacturonic acid (PgA) is not degradable in the gastrointestinal tract due to its insolubility at acidic pH. To avoid PgA solubility in the colon, we have designed its conjugation with Polyacrylic acid (PAA). PgA-PAA conjugation has enhanced their potential use for oral and injected dosage. Following these pre-requisites, novel polymeric nano-micelles derived from PgA-PAA conjugation and loading LY2157299 are developed and characterized. Efficacy, uptake and targeting against a hepatocellular carcinoma cell line (HLF) have also been demonstrated. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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19 pages, 8673 KiB  
Article
Solid Lipid Nanoparticles Carrying Temozolomide for Melanoma Treatment. Preliminary In Vitro and In Vivo Studies
by Nausicaa Clemente, Benedetta Ferrara, Casimiro Luca Gigliotti, Elena Boggio, Maria Teresa Capucchio, Elena Biasibetti, Davide Schiffer, Marta Mellai, Laura Annovazzi, Luigi Cangemi, Elisabetta Muntoni, Gianluca Miglio, Umberto Dianzani, Luigi Battaglia and Chiara Dianzani
Int. J. Mol. Sci. 2018, 19(2), 255; https://doi.org/10.3390/ijms19020255 - 24 Jan 2018
Cited by 55 | Viewed by 6924
Abstract
Aim: To develop an innovative delivery system for temozolomide (TMZ) in solid lipid nanoparticles (SLN), which has been preliminarily investigated for the treatment of melanoma. Materials and Methods: SLN-TMZ was obtained through fatty acid coacervation. Its pharmacological effects were assessed and compared with [...] Read more.
Aim: To develop an innovative delivery system for temozolomide (TMZ) in solid lipid nanoparticles (SLN), which has been preliminarily investigated for the treatment of melanoma. Materials and Methods: SLN-TMZ was obtained through fatty acid coacervation. Its pharmacological effects were assessed and compared with free TMZ in in vitro and in vivo models of melanoma and glioblastoma. Results: Compared to the standard free TMZ, SLN-TMZ exerted larger effects, when cell proliferation of melanoma cells, and neoangiogeneis were evaluated. SLN-TMZ also inhibited growth and vascularization of B16-F10 melanoma in C57/BL6 mice, without apparent toxic effects. Conclusion: SLN could be a promising strategy for the delivery of TMZ, allowing an increased stability of the drug and thereby its employment in the treatment of aggressive malignacies. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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11 pages, 2169 KiB  
Article
Enhancement in Corneal Permeability of Dissolved Carteolol by Its Combination with Magnesium Hydroxide Nanoparticles
by Noriaki Nagai, Sakie Yamaoka, Yuya Fukuoka, Miyu Ishii, Hiroko Otake, Kazutaka Kanai, Norio Okamoto and Yoshikazu Shimomura
Int. J. Mol. Sci. 2018, 19(1), 282; https://doi.org/10.3390/ijms19010282 - 17 Jan 2018
Cited by 8 | Viewed by 3848
Abstract
We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol. The carteolol was solved in saline containing additives (0.5% methylcellulose, 0.001% benzalkonium chloride, 0.5% mannitol; CRT-solution). MH nanoparticles [...] Read more.
We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol. The carteolol was solved in saline containing additives (0.5% methylcellulose, 0.001% benzalkonium chloride, 0.5% mannitol; CRT-solution). MH nanoparticles were prepared by a bead mill method with additives. Then carteolol/MH microparticle and carteolol/MH nanoparticle fixed combinations (mCMFC and nCMFC) were prepared by mixing the CRT-solution and MH particles. The transcorneal penetration and IOP-reducing effect of carteolol was evaluated in rabbits. The mean particle size of mCMFC was 7.2 μm, and the particle size was reduced to 73.5–113.5 nm by the bead mill treatment. The MH particles in nCMFC remained in the nano size range for 8 days after preparation, and the amounts of lacrimal fluid and corneal damage were unchanged by repetitive instillation of nCMFC (twice a day for 4 weeks). The transcorneal penetration of carteolol was enhanced by the combination with MH nanoparticles, and the IOP-reducing effect of nCMFC was significantly higher than that of CRT-solution or mCMFC. In conclusion, we designed nCMFC, and showed that the high levels of dissolved carteolol can be delivered into the aqueous humor by the instillation of nCMFC. Combination with MH nanoparticles may achieve an enhancement of corneal penetration for water-soluble drugs. These findings provide significant information that can be used to design further studies aimed at developing anti-glaucoma eye drugs. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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23 pages, 6543 KiB  
Article
Biodistribution and Clearance of Stable Superparamagnetic Maghemite Iron Oxide Nanoparticles in Mice Following Intraperitoneal Administration
by Binh T. T. Pham, Emily K. Colvin, Nguyen T. H. Pham, Byung J. Kim, Emily S. Fuller, Elizabeth A. Moon, Raphael Barbey, Samuel Yuen, Barry H. Rickman, Nicole S. Bryce, Stephanie Bickley, Marcel Tanudji, Stephen K. Jones, Viive M. Howell and Brian S. Hawkett
Int. J. Mol. Sci. 2018, 19(1), 205; https://doi.org/10.3390/ijms19010205 - 10 Jan 2018
Cited by 62 | Viewed by 9770
Abstract
Nanomedicine is an emerging field with great potential in disease theranostics. We generated sterically stabilized superparamagnetic iron oxide nanoparticles (s-SPIONs) with average core diameters of 10 and 25 nm and determined the in vivo biodistribution and clearance profiles. Healthy nude mice underwent an [...] Read more.
Nanomedicine is an emerging field with great potential in disease theranostics. We generated sterically stabilized superparamagnetic iron oxide nanoparticles (s-SPIONs) with average core diameters of 10 and 25 nm and determined the in vivo biodistribution and clearance profiles. Healthy nude mice underwent an intraperitoneal injection of these s-SPIONs at a dose of 90 mg Fe/kg body weight. Tissue iron biodistribution was monitored by atomic absorption spectroscopy and Prussian blue staining. Histopathological examination was performed to assess tissue toxicity. The 10 nm s-SPIONs resulted in higher tissue-iron levels, whereas the 25 nm s-SPIONs peaked earlier and cleared faster. Increased iron levels were detected in all organs and body fluids tested except for the brain, with notable increases in the liver, spleen, and the omentum. The tissue-iron returned to control or near control levels within 7 days post-injection, except in the omentum, which had the largest and most variable accumulation of s-SPIONs. No obvious tissue changes were noted although an influx of macrophages was observed in several tissues suggesting their involvement in s-SPION sequestration and clearance. These results demonstrate that the s-SPIONs do not degrade or aggregate in vivo and intraperitoneal administration is well tolerated, with a broad and transient biodistribution. In an ovarian tumor model, s-SPIONs were shown to accumulate in the tumors, highlighting their potential use as a chemotherapy delivery agent. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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1737 KiB  
Communication
Spatiotemporal Control of Doxorubicin Delivery from “Stealth-Like” Prodrug Micelles
by Li Kong, Dimitrios Poulcharidis, Gregory F. Schneider, Frederick Campbell and Alexander Kros
Int. J. Mol. Sci. 2017, 18(10), 2033; https://doi.org/10.3390/ijms18102033 - 22 Sep 2017
Cited by 4 | Viewed by 4110
Abstract
In the treatment of cancer, targeting of anticancer drugs to the tumor microenvironment is highly desirable. Not only does this imply accurate tumor targeting but also minimal drug release en route to the tumor and maximal drug release once there. Here we describe [...] Read more.
In the treatment of cancer, targeting of anticancer drugs to the tumor microenvironment is highly desirable. Not only does this imply accurate tumor targeting but also minimal drug release en route to the tumor and maximal drug release once there. Here we describe high-loading, “stealth-like” doxorubicin micelles as a pro-drug delivery system, which upon light activation, leads to burst-like doxorbicin release. Through this approach, we show precise spatiotemporal control of doxorubicin delivery to cells in vitro. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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5307 KiB  
Article
Synthesis and Characterization of Tissue Plasminogen Activator—Functionalized Superparamagnetic Iron Oxide Nanoparticles for Targeted Fibrin Clot Dissolution
by Susanne Heid, Harald Unterweger, Rainer Tietze, Ralf P. Friedrich, Bianca Weigel, Iwona Cicha, Dietmar Eberbeck, Aldo R. Boccaccini, Christoph Alexiou and Stefan Lyer
Int. J. Mol. Sci. 2017, 18(9), 1837; https://doi.org/10.3390/ijms18091837 - 24 Aug 2017
Cited by 31 | Viewed by 7358
Abstract
Superparamagnetic iron oxide nanoparticles (SPIONs) have attracted great attention in many biomedical fields and are used in preclinical/experimental drug delivery, hyperthermia and medical imaging. In this study, biocompatible magnetite drug carriers, stabilized by a dextran shell, were developed to carry tissue plasminogen activator [...] Read more.
Superparamagnetic iron oxide nanoparticles (SPIONs) have attracted great attention in many biomedical fields and are used in preclinical/experimental drug delivery, hyperthermia and medical imaging. In this study, biocompatible magnetite drug carriers, stabilized by a dextran shell, were developed to carry tissue plasminogen activator (tPA) for targeted thrombolysis under an external magnetic field. Different concentrations of active tPA were immobilized on carboxylated nanoparticles through carbodiimide-mediated amide bond formation. Evidence for successful functionalization of SPIONs with carboxyl groups was shown by Fourier transform infrared spectroscopy. Surface properties after tPA immobilization were altered as demonstrated by dynamic light scattering and ζ potential measurements. The enzyme activity of SPION-bound tPA was determined by digestion of fibrin-containing agarose gels and corresponded to about 74% of free tPA activity. Particles were stored for three weeks before a slight decrease in activity was observed. tPA-loaded SPIONs were navigated into thrombus-mimicking gels by external magnets, proving effective drug targeting without losing the protein. Furthermore, all synthesized types of nanoparticles were well tolerated in cell culture experiments with human umbilical vein endothelial cells, indicating their potential utility for future therapeutic applications in thromboembolic diseases. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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Review

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20 pages, 2032 KiB  
Review
Protein Polymer-Based Nanoparticles: Fabrication and Medical Applications
by Kelsey DeFrates, Theodore Markiewicz, Pamela Gallo, Aaron Rack, Aubrie Weyhmiller, Brandon Jarmusik and Xiao Hu
Int. J. Mol. Sci. 2018, 19(6), 1717; https://doi.org/10.3390/ijms19061717 - 09 Jun 2018
Cited by 154 | Viewed by 11721
Abstract
Nanoparticles are particles that range in size from about 1–1000 nanometers in diameter, about one thousand times smaller than the average cell in a human body. Their small size, flexible fabrication, and high surface-area-to-volume ratio make them ideal systems for drug delivery. Nanoparticles [...] Read more.
Nanoparticles are particles that range in size from about 1–1000 nanometers in diameter, about one thousand times smaller than the average cell in a human body. Their small size, flexible fabrication, and high surface-area-to-volume ratio make them ideal systems for drug delivery. Nanoparticles can be made from a variety of materials including metals, polysaccharides, and proteins. Biological protein-based nanoparticles such as silk, keratin, collagen, elastin, corn zein, and soy protein-based nanoparticles are advantageous in having biodegradability, bioavailability, and relatively low cost. Many protein nanoparticles are easy to process and can be modified to achieve desired specifications such as size, morphology, and weight. Protein nanoparticles are used in a variety of settings and are replacing many materials that are not biocompatible and have a negative impact on the environment. Here we attempt to review the literature pertaining to protein-based nanoparticles with a focus on their application in drug delivery and biomedical fields. Additional detail on governing nanoparticle parameters, specific protein nanoparticle applications, and fabrication methods are also provided. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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19 pages, 1056 KiB  
Review
Approaches in Polymeric Nanoparticles for Vaginal Drug Delivery: A Review of the State of the Art
by Gerardo Leyva-Gómez, Elizabeth Piñón-Segundo, Néstor Mendoza-Muñoz, María L. Zambrano-Zaragoza, Susana Mendoza-Elvira and David Quintanar-Guerrero
Int. J. Mol. Sci. 2018, 19(6), 1549; https://doi.org/10.3390/ijms19061549 - 23 May 2018
Cited by 65 | Viewed by 9393
Abstract
The vagina is a region of administration with a high contact surface to obtain local or systemic effects. This anatomical area represents special interest for government health systems for different sexually transmitted infections. However, the chemical changes of the vagina, as well as [...] Read more.
The vagina is a region of administration with a high contact surface to obtain local or systemic effects. This anatomical area represents special interest for government health systems for different sexually transmitted infections. However, the chemical changes of the vagina, as well as its abundant mucus in continuous exchange, act as a barrier and a challenge for the development of new drugs. For these purposes, the development of new pharmaceutical forms based on nanoparticles has been shown to offer various advantages, such as bioadhesion, easy penetration of the mucosa, and controlled release, in addition to decreasing the adverse effects of conventional pharmaceutical forms. In order to obtain nanoparticles for vaginal administration, the use of polymers of natural and synthetic origin including biodegradable and non-biodegradable systems have gained great interest both in nanospheres and in nanocapsules. The main aim of this review is to provide an overview of the development of nanotechnology for vaginal drug release, analyzing the different compositions of polymeric nanoparticles, and emphasizing new trends in each of the sections presented. At the end of this review, a section analyzes the properties of the vehicles employed for the administration of nanoparticles and discusses how to take advantage of the properties that they offer. This review aims to be a reference guide for new formulators interested in the vaginal route. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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15 pages, 466 KiB  
Review
PEO-PPO-PEO Tri-Block Copolymers for Gene Delivery Applications in Human Regenerative Medicine—An Overview
by Ana Rey-Rico and Magali Cucchiarini
Int. J. Mol. Sci. 2018, 19(3), 775; https://doi.org/10.3390/ijms19030775 - 08 Mar 2018
Cited by 57 | Viewed by 6751
Abstract
Lineal (poloxamers or Pluronic®) or X-shaped (poloxamines or Tetronic®) amphiphilic tri-block copolymers of poly(ethylene oxide) and poly(propylene oxide) (PEO-PPO-PEO) have been broadly explored for controlled drug delivery in different regenerative medicine approaches. The ability of these copolymers to self-assemble [...] Read more.
Lineal (poloxamers or Pluronic®) or X-shaped (poloxamines or Tetronic®) amphiphilic tri-block copolymers of poly(ethylene oxide) and poly(propylene oxide) (PEO-PPO-PEO) have been broadly explored for controlled drug delivery in different regenerative medicine approaches. The ability of these copolymers to self-assemble as micelles and to undergo sol-to-gel transitions upon heating has endowed the denomination of “smart” or “intelligent” systems. The use of PEO-PPO-PEO copolymers as gene delivery systems is a powerful emerging strategy to improve the performance of classical gene transfer vectors. This review summarizes the state of art of the application of PEO-PPO-PEO copolymers in both nonviral and viral gene transfer approaches and their potential as gene delivery systems in different regenerative medicine approaches. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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