Pharmaceutical Nanotechnology - Volume 11, Issue 2, 2023
Volume 11, Issue 2, 2023
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Nanoformulation-based Drug Delivery System for Viral Diseases
Viral diseases are one of the major causes of mortality worldwide. The emergence of pandemics because of the COVID virus creates a dire need for an efficient mechanism to combat the disease. Viruses differ from other pathogenic infections; they render the host immune system vulnerable. One of the major challenges for developing antivirals is the resistance developed by the overuse of drugs, which is inevitable as most viral diseases require a large number of doses. Viral infection detection, prevention, and treatment have significantly benefitted from developing several innovative technologies in recent years. Nanotechnology has emerged as one of the most promising technologies because of its capacity to deal with viral infections efficiently and eradicate the lagging of conventional antiviral drugs. This review briefly presents an overview of the application of nanotechnology for viral therapy.
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Current Research on Spray-Dried Chitosan Nanocomposite Microparticles for Pulmonary Drug Delivery
More LessUsing the pulmonary route for systemic and local drug delivery is an attractive method of drug administration because it has a high alveolar surface area, abundant blood flow, a thin airblood barrier, and low metabolic activity. In recent years, the evolution of inhalable chitosan nanocomposite microparticles formulations enabled researchers to develop new pulmonary drug delivery platforms that combine the advantages of microparticles and nanoparticles using a biocompatible, biodegradable polymer with polycationic nature and inherent immunogenicity that enhances cell targeting. Therefore, this review aims to offer an overview of the recent advances in inhalable chitosan nanocomposites microparticles formulated in the previous five years in terms of primary nanoparticles manufacturing methods; namely, ionic crosslinking of chitosan using tripolyphosphate, electrospinning/electrospraying, layer-by-layer deposition, and nanospray drying; final microparticles manufacturing techniques using spray drying, nano spray drying, and supercritical assisted spray drying; in addition to the process optimization of the previously mentioned manufacturing methods. Furthermore, this review highlights using chitosan and its derivatives in primary nanoparticles preparation and as a polysaccharide to distribute the prepared nanoparticles in microparticles. Finally, this review discusses the factors affecting yield, encapsulation efficiency, in vitro aerosolization properties, size, morphological characters, in vitro release, and in vivo evaluation of inhalable chitosan nanocomposite microparticles.
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Solid Lipid Nanoparticles (SLNs): Advancements in Modification Strategies Toward Drug Delivery Vehicle
Solid lipid nanoparticles are at the cornerstone of the swiftly growing area of medical nanotechnology, having several potential functions in drug delivery, research, clinical care, and a variety of other fields. They provide the opportunity of developing novel therapies due to their unique properties, such as small particle size and being prepared from physiological biodegradable lipids. The loading of bioactive molecules into nanocarriers is a novel drug delivery prototype employed for various drug targeting levels. Hence, SLNs hold a great promise for achieving the aim of targeted and controlled drug delivery. For this reason, they have attracted the extensive attention of scientists and researchers. This review is based on recent studies and research, and here we present advantages, disadvantages, and preparation methods, several advanced modifications, targeting strategies, and recent applications of solid lipid nanocarriers in drug delivery systems.
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Magnetophoretic Intranasal Drug-loaded Magnetic Nano-aggregates as a Platform for Drug Delivery in Status Epilepticus
Authors: Ali Hemmat, Erfaneh Ghassami, Mohsen Minaiyan and Jaleh VarshosazBackground: Status epilepticus is associated with substantial morbidity and neuronal necrosis, and the duration of the seizure would affect its following complications. Eliminating the duration would have valuable outcomes; however, the presence of BBB is an obstacle. The purpose of the current study was to achieve a nose-to-brain magnetic drug delivery system to accelerate the onset of action, and to reduce the mucociliary clearance via implementing the magnetic field. Materials and Methods: The drug-entrapped magnetic nanoaggregates were prepared via a 2-step method, synthesis of the magnetic nanoparticles and drug loading. Optimization of the variables, including ammonium hydroxide:water ratio, beta-cyclodextrin%, duration of the mixing time, amount of Pluronic, and drug:magnetic nanoaggregates mass ratio was performed according to particle size, PDI, zeta potential, release profile and entrapment efficiency. The efficacy of optimized formulation was assessed in the animal model. Results: According to the analysis performed by the software, drug-to-nanoparticle ratio and the duration of mixing time were found to be significantly effective (p < 0.05) for entrapment efficiency and particle size distribution, respectively. The optimum formulation with an approximate average size of 581 nm and 61% entrapment efficiency was obtained, which released about 80% of its drug content within the first 20 minutes. The in vivo efficacy was significantly improved (p < 0.05) by administration of magnetic nanoaggregates in the presence of a simple external magnet placed on the glabellar region of the animals, compared to the control groups. Conclusion: This drug delivery system could be suggested as a fast-acting alternative for seizure cessation in status epilepticus emergencies.
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Effect of the Surfactant Charge on the Characteristics and Anticancer Effects of Docetaxel-loaded Poloxamer Polymeric Micelles
Authors: Dwianto Harry Nugraha, Kusnandar Anggadiredja and Heni RachmawatiBackground: The main problem in the use of docetaxel as a potent chemotherapeutic agent is its solubility. Practically insoluble docetaxel requires a harsh formulation with high surfactant and alcohol concentrations to comply with the product quality. However, this formulation is inconvenient for patients. Polymeric micelles using a biocompatible polymer, poloxamer, seem to be a promising approach to increase the solubility of docetaxel, avoiding the high polysorbate and alcohol contents in the commercial product and yielding similar or better anticancer effects. Objective: This study aims to investigate the effects of surfactant with three different charges on the particle size, chemical stability, in vitro drug release and anticancer efficacy of the docetaxelloaded poloxamer-based polymeric micelle formulation. Methods: The freeze drying method was used to prepare polymeric micelles of docetaxel. Dynamic light scattering was used to determine particle size. The morphology of particles was investigated using a transmission electron microscope. High Pressure Liquid Chromatography was used to measure encapsulation efficiency, drug loading, and percentage of drug released. MTT assay was used to assess the anticancer effect. Results: Nonionic and anionic surfactants tended to increase the particle size, while cationic surfactants had no effect. Furthermore, the addition of cationic surfactant increased the chemical stability of docetaxel. Poloxamer polymeric micelles have sustained drug release, and the addition of a surfactant can increase polymeric micelle drug release. All surfactant charges increased the anticancer efficacy of docetaxel compared to the commercial formulation Taxotere, except for the formulation prepared with an anionic surfactant. Conclusion: The charge of the surfactant affects the particle size, chemical stability, drug release and anticancer properties of docetaxel-loaded poloxamer polymeric micelles. Cationic surfactant formulations have shown to be promising, resulting in the most stable and highest anticancer effect.
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Biogenic Synthesis of Silver Nanoparticles using Lasiosiphon eriocephalus (Decne): In vitroAssessment of their Antioxidant, Antimicrobial and Cytotoxic Activities
Authors: Kailas D. Datkhile, Pratik P. Durgawale and Satish R. PatilIntroduction: The emergence of novel nanobiomedicine has transformed the management of various infectious as well as non-infectious diseases. Lasiosiphon eriocephalus, a medicinal plant, revealed the presence of active secondary metabolites and biological potentials. Objective: The present study was aimed to demonstrate the biosynthesis of silver nanoparticles using L. eriocephalusleaf extract (LE-AgNPs) and their biological properties, such as antioxidant, antibacterial and anticancer potential. Methods: The biosynthesized LE-AgNPs were characterized by UV-Visible spectroscopy, Scanning electron microscopy (SEM), Transmission electron microscopy (TEM), X-ray diffraction, and Fourier transform infrared spectroscopy (FTIR) analysis. The antibacterial activity was checked by minimum inhibitory concentration (MIC) and zone of inhibition assays against Gram-positive and Gram-negative bacteria. The anticancer potential of biogenic LE-AgNPs was checked by cytotoxicity and genotoxicity assay against human cervical adenocarcinoma (HeLa) and human breast adenocarcinoma (MCF-7) cells. Results: UV-visible spectroscopy confirmed the formation of silver nanoparticles by measuring the surface plasmon resonance peak of the colloidal solution at 410-440 nm. The results of SEM and TEM revealed the distribution and spherical shape of 20-50 nm sized AgNPs. XRD spectrum confirmed the characteristic peaks at the lattice planes 110, 111, 200, 220 and 311 of silver which confirmed the crystalline nature of biosynthesized LE-AgNPs. FTIR spectrum of plant extract and biogenic LE-AgNPs was recorded in between 1635-3320 cm -1 which confirmed stretching vibrations of possible functional groups C=C and O-H, responsible for the reduction of silver ions to silver nanoparticles. The in vitro antioxidant potential of LE-AgNPs was evaluated using DPPH (IC50 = 26.51 ± 1.15 μg/mL) and ABTS radical assays (IC50 =74.33 ± 2.47 μg/mL). The potential antibacterial effects of LE-AgNPs confirmed that 92.38 ± 2.70% growth inhibition occurred in E. coli in response to 0.1mg/mL concentration of LE-AgNPs followed by P. aeruginosa (75.51 ± 0.76), S. aureus (74.53 ± 1.26) and K. pneumoniae (67.4 ± 3.49). The cytotoxicity results interpreted that the biogenic silver nanoparticles exhibited strong dose and time dependent cytotoxicity effect against selected cancer cell lines where IC50 concentration of LE-AgNPs required to inhibit the growth of HeLa cells after 24 h exposure was 4.14 μg/mL and MCF7 cells 3.00 μg/mL, respectively. Significant DNA fragmentation was seen in the DNA extracted from HeLa and MCF-7 cells exposed to more than 2.5 to 10 μg/mL concentrations of LE-AgNPs. Conclusion: The overall findings from the present investigation indicated that the AgNPs synthesized using L. eriocephalusexerted strong biological potentials such as antioxidant, antimicrobial and extensive cytotoxicity and genotoxicity activities.
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Experimental Pharmacology for COVID-19 Treatment: A Geoanalytical Bibliometric Analysis
Authors: Cesar Aguado and Victor M. CastañoObjective: The objective of this study is to produce a geo-referenced map of the status of R in COVID-related studies in the world. Methods: Spatial mapping of bibliometric data of Cortellis Drug Discovery Intelligence through a spatial bibliometric model with the aid of a GIS (Geographic Information System) called ArcGIS and the software. Results: We show the countries that have the most studies related to COV ID-19 and their degree of collaboration. No drug discovery-related activity was found in South America and Africa. A geo-referenced map of the most active countries in COVID research was constructed as well as conceptual maps of the 11 most representative drugs employed for COVID treatment. Conclusion: The georeferenced conceptual maps produced in the present report allow not only to better understand the leading institutions in R in COVID-19 related drugs but also to visualize their interactions and research relationships. This could offer, in addition to a coherent, organized multinational effort, the possibility of searching for other drugs that have been employed for other diseases and that, in terms of their conceptual relations, could represent some possibilities for treating the coronavirus SARS-2.
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The Antibacterial Effect of Tetracycline-loaded Mesoporous Silica Nanoparticles in the Gingival Fluid at Implant-abutment Junction: A Randomized Clinical Trial Study
Introduction: Dental implant failure due to periodontal disease caused by anaerobic pathogens occurs, especially in the first year of implant placement. The aim of this clinical trial study was to compare the antibacterial effect of tetracycline gel and gel containing tetracyclineloaded mesoporous silica nanoparticles (MSNs) in the gingival crevice fluid of the implantabutment junction as a randomized clinical trial study. Materials and Methods: Fourteen patients applying for implants in the posterior mandibular region were included in the study. During the uncovering session, tetracycline gel and gel containing tetracycline-loaded MSNs were placed in two implants and no substance was placed in the control group. Then, in three sessions, including molding, prosthesis delivery, and one month after delivery, the patient's gingival fluid was sampled and the number of bacteria in the gingival fluid was measured by colony-forming units (CFU/mL). Results: The results of this study showed that in all three stages of sampling, the use of tetracycline gel and gel containing MSNs loaded with tetracycline significantly reduced the CFU/mL of gingival crevice fluid compared to the control group. Tetracycline-loaded MSNs gel showed significantly lower CFU/mL than tetracycline gel. The release of tetracycline from nanoparticles keep continue for a longer time compared to tetracycline gel. Conclusion: The use of nano-based delivery systems containing antibiotics inside the implant fixture can reduce the bacterial count of the implant-abutment junction and then improve implant stability.
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