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  1. Fulltext Expanding Arsenal against Neurodegenerative Diseases Using Quercetin Based Nanoformulations: Breakthroughs and Bottlenecks
    Vishwas S, Kumar R, Khursheed R, Ramanunny AK, Kumar R, Awasthi A, et al.
    Curr Neuropharmacol, 2023;21(7):1558-1574.
    PMID: 35950245 DOI: 10.2174/1570159X20666220810105421
    Quercetin (Qu), a dietary flavonoid, is obtained from many fruits and vegetables such as coriander, broccoli, capers, asparagus, onion, figs, radish leaves, cranberry, walnuts, and citrus fruits. It has proven its role as a nutraceutical owing to numerous pharmacological effects against various diseases in preclinical studies. Despite these facts, Qu and its nanoparticles are less explored in clinical research as a nutraceutical. The present review covers various neuroprotective actions of Qu against various neurodegenerative diseases (NDs) such as Alzheimer's, Parkinson's, Huntington's, and Amyotrophic lateral sclerosis. A literature search was conducted to systematically review the various mechanistic pathways through which Qu elicits its neuroprotective actions and the challenges associated with raw Qu that compromise therapeutic efficacy. The nanoformulations developed to enhance Qu's therapeutic efficacy are also covered. Various ongoing/completed clinical trials related to Qu in treating various diseases, including NDs, are also tabulated. Despite these many successes, the exploration of research on Qu-loaded nanoformulations is limited mostly to preclinical studies, probably due to poor drug loading and stability of the formulation, time-consuming steps involved in the formulation, and their poor scale-up capacity. Hence, future efforts are required in this area to reach Qu nanoformulations to the clinical level.
    Matched MeSH terms: Nanoparticles*
  2. Next-generation viral nanoparticles for targeted delivery of therapeutics: Fundamentals, methods, biomedical applications, and challenges
    Tan JS, Jaffar Ali MNB, Gan BK, Tan WS
    Expert Opin Drug Deliv, 2023;20(7):955-978.
    PMID: 37339432 DOI: 10.1080/17425247.2023.2228202
    INTRODUCTION: Viral nanoparticles (VNPs) are virus-based nanocarriers that have been studied extensively and intensively for biomedical applications. However, their clinical translation is relatively low compared to the predominating lipid-based nanoparticles. Therefore, this article describes the fundamentals, challenges, and solutions of the VNP-based platform, which will leverage the development of next-generation VNPs.

    AREAS COVERED: Different types of VNPs and their biomedical applications are reviewed comprehensively. Strategies and approaches for cargo loading and targeted delivery of VNPs are examined thoroughly. The latest developments in controlled release of cargoes from VNPs and their mechanisms are highlighted too. The challenges faced by VNPs in biomedical applications are identified, and solutions are provided to overcome them.

    EXPERT OPINION: In the development of next-generation VNPs for gene therapy, bioimaging and therapeutic deliveries, focus must be given to reduce their immunogenicity, and increase their stability in the circulatory system. Modular virus-like particles (VLPs) which are produced separately from their cargoes or ligands before all the components are coupled can speed up clinical trials and commercialization. In addition, removal of contaminants from VNPs, cargo delivery across the blood brain barrier (BBB), and targeting of VNPs to organelles intracellularly are challenges that will preoccupy researchers in this decade.

    Matched MeSH terms: Nanoparticles*
  3. Polycaprolactone-based Nanocarriers Containing 5-fluorouracil as a Therapeutic Guided Drug Delivery Approach for Enhancing Anticancer Activity
    Mohammadian S, Khazaei M, Maghami P, Avan A, Rezaei M
    Curr Cancer Drug Targets, 2023;23(7):524-533.
    PMID: 36809944 DOI: 10.2174/1568009623666230210140212
    Nowadays, nano-platforms designed for drug delivery systems (DDSs) such as polymers, liposomes, and micelles have been demonstrated to be clinically efficient. The sustained drug release is one of the advantages of DDSs, especially polymer-based nanoparticles. The formulation could enhance the drug's durability, in which the biodegradable polymers are the most interesting building blocks of DDSs. Nano-carriers could circumvent many issues by localized drug delivery and release via certain internalization routes such as intracellular endocytosis paths and increasing biocompatibility. Polymeric nanoparticles and their nanocomposite are one of the most important classes of materials that can be used for the assembly of nanocarriers that can form complex, conjugated and encapsulated forms. The site-specific drug delivery may arise from the ability of nanocarriers to pass through the biological barrier, their specific interactions with receptors, and passive targeting. The better circulation, uptake, and stability along with targeting attributes lead to lesser side effects and damage to normal cells. Hence, in this review, the most recent achievements on polycaprolactone-based or -modified nanoparticles in drug delivery systems (DDSs) for 5-fluorouracil (5-FU) are presented.
    Matched MeSH terms: Nanoparticles*
  4. A Perspective on Therapeutic Applications and Strategies to Mitigate Toxicity of Metallic Nanoparticles
    Karuppaiah A, Selvaraj D, Sellappan M, Nagarajan A, Babu D, Rahman H, et al.
    Curr Pharm Des, 2023;29(4):239-245.
    PMID: 36624648 DOI: 10.2174/1381612829666230109111635
    Metallic nanoparticles (MNPs) have been widely used for diagnostic and therapeutic purposes in clinical practice. A number of MNP formulations are being investigated in clinical trials for various applications. This increase in the use of NPs results in higher exposure to humans, leading to toxicity issues. Hence, it is necessary to determine the possible undesirable effects of the MNPs after in-vivo application and exposure. One of the main reasons for the toxicity of MNPs is the release of their respective metallic ions throughout the body. Many research studies are in progress investigating the various strategies to reduce the toxicity of MNPs. These research studies aim to change the size, dose, agglomeration, release, and excretion rates of MNPs. In this perspective review, we discussed the possible strategies to improve the therapeutic effects of MNPs through various processes, with lessons learned from the studies involving silver nanoparticles (AgNPs). We also discussed the ways to manage the toxicity of MNPs by purification, surface functionalization, synergistic effect, and targeted therapy approach. All these strategies could reduce the dose of the MNPs without compromising their therapeutic benefits, which could decrease the toxicity of MNPs. Additionally, we briefly discussed the market and toxicology testing for FDA-regulated MNPs.
    Matched MeSH terms: Nanoparticles*; Magnetite Nanoparticles*
  5. Lopinavir-Loaded Self-Nanoemulsifying Drug Delivery System for Enhanced Solubility: Development, Characterisation and Caco-2 Cell Uptake
    Khan AA, Akhtar S, Yadav Y, Atiya A, Alelwani W, Bannunah AM, et al.
    Curr Drug Deliv, 2023;20(10):1474-1486.
    PMID: 35980056 DOI: 10.2174/1567201819666220817111054
    BACKGROUND: The antiretroviral protease inhibitor drug, lopinavir (LPV), is used to treat HIV-1 infection. LPV is known to have limited oral bioavailability, which may be attributed to its poor aqueous solubility, low efficacy and high first-pass metabolism. Self-nanoemulsifying drug delivery systems (SNEDDS) for LPV have been developed and optimised to counter the current issues.

    METHODS: The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS.

    RESULTS: The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension).

    CONCLUSION: The LPV-SNEDDS could be a potential carrier for LPV oral delivery.

    Matched MeSH terms: Nanoparticles*
  6. Fulltext Emergence of mRNA vaccines in the management of cancer
    Mohamad Razif MI, Nizar N, Zainal Abidin NH, Muhammad Ali SN, Wan Zarimi WNN, Khotib J, et al.
    Expert Rev Vaccines, 2023;22(1):629-642.
    PMID: 37401128 DOI: 10.1080/14760584.2023.2232450
    INTRODUCTION: mRNA vaccines have been developed as a promising cancer management. It is noted that specification of the antigen sequence of the target antigen is necessary for the design and manufacture of an mRNA vaccine.

    AREAS COVERED: The steps involved in preparing the mRNA-based cancer vaccines are isolation of the mRNA cancer from the target protein using the nucleic acid RNA-based vaccine, sequence construction to prepare the DNA template, in vitro transcription for protein translation from DNA into mRNA strand, 5' cap addition and poly(A) tailing to stabilize and protect the mRNA from degradation and purification process to remove contaminants produced during preparation.

    EXPERT OPINION: Lipid nanoparticles, lipid/protamine/mRNA nanoparticles, and cell-penetrating peptides have been used to formulate mRNA vaccine and to ensure vaccine stability and delivery to the target site. Delivery of the vaccine to the target site will trigger adaptive and innate immune responses. Two predominant factors of the development of mRNA-based cancer vaccines are intrinsic influence and external influence. In addition, research relating to the dosage, route of administration, and cancer antigen types have been observed to positively impact the development of mRNA vaccine.

    Matched MeSH terms: Nanoparticles*
  7. Magnetic Nanoparticle-Based Semi-automated Panning for High-Throughput Antibody Selection
    Ch'ng ACW, Konthur Z, Lim TS
    Methods Mol Biol, 2023;2702:291-313.
    PMID: 37679626 DOI: 10.1007/978-1-0716-3381-6_15
    Bio-panning is a common process involved in recombinant antibody selection against defined targets. The biopanning process aims to isolate specific antibodies against an antigen via affinity selection from a phage display library. In general, antigens are immobilized on solid surfaces such as polystyrene plastic, magnetic beads, and nitrocellulose. For high-throughput selection, semi-automated panning selection allows simultaneous panning against multiple target antigens adapting automated particle processing systems such as the KingFisher Flex. The system setup allows for minimal human intervention for pre- and post-panning steps such as antigen immobilization, phage rescue, and amplification. In addition, the platform is also adaptable to perform polyclonal and monoclonal ELISA for the evaluation process. This chapter will detail the protocols involved from the selection stage until the monoclonal ELISA evaluation with important notes attached at the end of this chapter for optimization and troubleshooting purposes.
    Matched MeSH terms: Magnetite Nanoparticles*
  8. Analyzing and mapping the research status, hotspots, and frontiers of biological wound dressings: An in-depth data-driven assessment
    Shen S, Deng L, Du Y, Gao J, Zhang C, Wang Y, et al.
    Int J Pharm, 2022 Dec 15;629:122385.
    PMID: 36375685 DOI: 10.1016/j.ijpharm.2022.122385
    Wound dressings can be applied over the wound sites to provide long-lasting wound management and improve wound healing. Biological wound dressings are superior to synthetic materials due to biodegradability and biocompatibility. These biomaterials have demonstrated huge potential in the field of wound dressings. Applying bibliometric analysis combined with results-based descriptions to characterize the research status, hotspots, and cutting-edge topics, this study is the first in-depth qualitative, quantitative, data-driven overview of biological wound dressings research in recent decades. Filtered data were used to construct co-citation, heatmaps, bi-clustering, strategy maps, and other analyses and visualization. The results show that research on biological wound dressings has progressed considerably in the last 5 years with extensive global collaboration. A clear knowledge base has been developed. Chitosan hydrogels, bacterial cellulose, active agents (silver nanoparticles, growth factors, curcumin, etc.), and electrospinning fibers stand out as research hotspots. The research frontiers include novel starting materials, precise and controlled release systems, and clinical and regenerative medicine applications. We interpreted an overview of the excavated topics and expected the findings here to provide a guide and inspire innovations for developing the next generation wound dressings.
    Matched MeSH terms: Metal Nanoparticles*
  9. Fulltext Biosynthesis of Gold Nanoparticles and Its Effect against Pseudomonas aeruginosa
    Ali SG, Jalal M, Ahmad H, Umar K, Ahmad A, Alshammari MB, et al.
    Molecules, 2022 Dec 08;27(24).
    PMID: 36557818 DOI: 10.3390/molecules27248685
    Antimicrobial resistance has posed a serious health concern worldwide, which is mainly due to the excessive use of antibiotics. In this study, gold nanoparticles synthesized from the plant Tinospora cordifolia were used against multidrug-resistant Pseudomonas aeruginosa. The active components involved in the reduction and stabilization of gold nanoparticles were revealed by gas chromatography-mass spectrophotometry(GC-MS) of the stem extract of Tinospora cordifolia. Gold nanoparticles (TG-AuNPs) were effective against P. aeruginosa at different concentrations (50,100, and 150 µg/mL). TG-AuNPs effectively reduced the pyocyanin level by 63.1% in PAO1 and by 68.7% in clinical isolates at 150 µg/mL; similarly, swarming and swimming motilities decreased by 53.1% and 53.8% for PAO1 and 66.6% and 52.8% in clinical isolates, respectively. Biofilm production was also reduced, and at a maximum concentration of 150 µg/mL of TG-AuNPs a 59.09% reduction inPAO1 and 64.7% reduction in clinical isolates were observed. Lower concentrations of TG-AuNPs (100 and 50 µg/mL) also reduced the pyocyanin, biofilm, swarming, and swimming. Phenotypically, the downregulation of exopolysaccharide secretion from P. aeruginosa due to TG-AuNPs was observed on Congo red agar plates.
    Matched MeSH terms: Metal Nanoparticles*
  10. Fulltext Synergistic Effect of Static Magnetic Fields and 3D-Printed Iron-Oxide-Nanoparticle-Containing Calcium Silicate/Poly-ε-Caprolactone Scaffolds for Bone Tissue Engineering
    Kao CY, Lin TL, Lin YH, Lee AK, Ng SY, Huang TH, et al.
    Cells, 2022 Dec 08;11(24).
    PMID: 36552731 DOI: 10.3390/cells11243967
    In scaffold-regulated bone regeneration, most three-dimensional (3D)-printed scaffolds do not provide physical stimulation to stem cells. In this study, a magnetic scaffold was fabricated using fused deposition modeling with calcium silicate (CS), iron oxide nanoparticles (Fe3O4), and poly-ε-caprolactone (PCL) as the matrix for internal magnetic sources. A static magnetic field was used as an external magnetic source. It was observed that 5% Fe3O4 provided a favorable combination of compressive strength (9.6 ± 0.9 MPa) and degradation rate (21.6 ± 1.9% for four weeks). Furthermore, the Fe3O4-containing scaffold increased in vitro bioactivity and Wharton's jelly mesenchymal stem cells' (WJMSCs) adhesion. Moreover, it was shown that the Fe3O4-containing scaffold enhanced WJMSCs' proliferation, alkaline phosphatase activity, and the osteogenic-related proteins of the scaffold. Under the synergistic effect of the static magnetic field, the CS scaffold containing Fe3O4 can not only enhance cell activity but also stimulate the simultaneous secretion of collagen I and osteocalcin. Overall, our results demonstrated that Fe3O4-containing CS/PCL scaffolds could be fabricated three dimensionally and combined with a static magnetic field to affect cell behaviors, potentially increasing the likelihood of clinical applications for bone tissue engineering.
    Matched MeSH terms: Nanoparticles*
  11. Efficacy of pentamidine-loaded chitosan nanoparticles as a novel drug delivery system for Leishmania tropica
    Khan RU, Khan M, Sohail A, Ullah R, Iqbal A, Ahmad B, et al.
    Trop Biomed, 2022 Dec 01;39(4):511-517.
    PMID: 36602209 DOI: 10.47665/tb.39.4.003
    The present study compares the in vitro effects of nanoparticles loaded pentamidine drug and conventional pentamidine on Leishmania tropica. Herein, pentamidine-loaded chitosan nanoparticles (PTN-CNPs) have been synthesized through an ionic gelation method with sodium tripolyphosphate (TPP). Next, the physical characteristics of PTN-CNPs were determined through the surface texture, zeta potential, in vitro drug release, drug loading content (DLC), and encapsulation efficacy (EE) and compared its efficacy with free pentamidine (PTN) drug against promastigotes and axenic amastigotes forms of L. tropica in vitro. The PTN-CNPs displayed a spherical shape having a size of 88 nm, an almost negative surface charge (-3.09 mV), EE for PTN entrapment of 86%, and in vitro drug release of 92% after 36 h. In vitro antileishmanial activity of PTN-CNPs and free PTN was performed against Leishmania tropica KWH23 promastigote and axenic amastigote using 3-(4, 5- dimethylthiazol-2-yl)-2, 5-diphenyletetrazolium bromide (MTT) assay. It was observed that the effect of PTN-CNPs and free PTN on both forms of the parasite was dose and time dependent. Free PTN presented low efficacy even at higher dose (40 µg/ml) with 25.6 ± 1.3 and 26.5 ±1.4 mean viability rate of the promastigotes and axenic amastigotes, respectively after 72 hrs incubation. While PTN-CNPs showed strong antileishmanial effects on both forms of parasite with 16 ± 0.4 and 19 ± 0.7 mean viability rate at the same higher concentration (40 µg/ml) after 72 hrs incubation. Half maximal inhibitory concentration (IC50) values of PTN-CNPs toward promastigotes and amastigotes were obtained as 0.1375 µg/ml and 0.1910 µg/ml, respectively. In conclusion, PTN-CNPs effectively inhibited both forms of the L. tropica; however, its effect was more salient on promastigotes. This data indicates that the PTN-CNPs act as a target drug delivery system. However, further research is needed to support its efficacy in animal and human CL.
    Matched MeSH terms: Nanoparticles*
  12. Fulltext SARS-CoV-2 detection by targeting four loci of viral genome using graphene oxide and gold nanoparticle DNA biosensor
    Babadi AA, Rahmati S, Fakhlaei R, Heidari R, Baradaran S, Akbariqomi M, et al.
    Sci Rep, 2022 Nov 12;12(1):19416.
    PMID: 36371566 DOI: 10.1038/s41598-022-23996-y
    The current COVID-19 pandemic outbreak poses a serious threat to public health, demonstrating the critical need for the development of effective and reproducible detection tests. Since the RT-qPCR primers are highly specific and can only be designed based on the known sequence, mutation sensitivity is its limitation. Moreover, the mutations in the severe acute respiratory syndrome β-coronavirus (SARS-CoV-2) genome led to new highly transmissible variants such as Delta and Omicron variants. In the case of mutation, RT-qPCR primers cannot recognize and attach to the target sequence. This research presents an accurate dual-platform DNA biosensor based on the colorimetric assay of gold nanoparticles and the surface-enhanced Raman scattering (SERS) technique. It simultaneously targets four different regions of the viral genome for detection of SARS-CoV-2 and its new variants prior to any sequencing. Hence, in the case of mutation in one of the target sequences, the other three probes could detect the SARS-CoV-2 genome. The method is based on visible biosensor color shift and a locally enhanced electromagnetic field and significantly amplified SERS signal due to the proximity of Sulfo-Cyanine 3 (Cy3) and AuNPs intensity peak at 1468 cm-1. The dual-platform DNA/GO/AuNP biosensor exhibits high sensitivity toward the viral genome with a LOD of 0.16 ng/µL. This is a safe point-of-care, naked-eye, equipment-free, and rapid (10 min) detection biosensor for diagnosing COVID-19 cases at home using a nasopharyngeal sample.
    Matched MeSH terms: Metal Nanoparticles*
  13. How far have we explored fungi to fight cancer?
    How CW, Ong YS, Low SS, Pandey A, Show PL, Foo JB
    Semin Cancer Biol, 2022 11;86(Pt 2):976-989.
    PMID: 33737109 DOI: 10.1016/j.semcancer.2021.03.009
    The use of fungal cultures have been well documented in human history. Although its used in healthcare, like penicillin and statins, have saved countless of lives, but there is still no fungal products that are specifically indicated for cancers. Research into fungal-derived materials to curb cancers in the recent decades have made a considerable progress in terms of drug delivery vehicles, anticancer active ingredients and cancer immunotherapy. Various parts of the organisms have successfully been exploited to achieve specific tasks. Apart from the identification of novel anticancer compound from fungi, its native capsular structure can also be used as drug cargo to achieve higher oral bioavailability. This review summarises the anticancer potential of fungal-derived materials, highlighting the role of capsular polysaccharides, proteins, and other structures in variety of innovative utilities to fit the current pharmaceutical technology. Many bioactive compounds isolated from fungi have also been formulated into nanoparticles to achieve greater anticancer activity. The progress of fungal compounds and their analogues in clinical trials is also highlighted. In addition, the potential of various fungal species to be developed for anticancer immunotherapy are also discussed.
    Matched MeSH terms: Nanoparticles*
  14. Low-gradient magnetic separation of magnetic nanoparticles under continuous flow: Experimental study, transport mechanism and mathematical modelling
    Tan YW, Leong SS, Lim J, Yeoh WM, Toh PY
    Electrophoresis, 2022 Nov;43(21-22):2234-2249.
    PMID: 35921231 DOI: 10.1002/elps.202200078
    Low-gradient magnetic separation (LGMS) of magnetic nanoparticles (MNPs) has been proven as one of the techniques with great potential for biomedical and environmental applications. Recently, the underlying principle of particle capture by LGMS, through a process known as magnetophoresis, under the influence of hydrodynamic effect has been widely studied and illustrated. Even though the hydrodynamic effect is very substantial for batch processes, its impact on LGMS operated at continuous flow (CF) condition remained largely unknown. Hence, in this study, the dynamical behaviour of LGMS process operated under CF was being studied. First, the LGMS experiments using poly(sodium 4-styrenesulfonate)-functionalized-MNP as modelled particle system were performed through batchwise (BW) and CF modes at different operating conditions. Here BW operation was used as a comparative study to elucidate the transport mechanism of MNP under the similar environment of CF-LGMS process, and it was found out that the convection induced by magnetophoresis (timescale effective is ∼1200 s) is only significant at far-from-magnet region. Hence, it can be deduced that forced convection is more dominant on influencing the transport behaviour of CF-LGMS (with resident time ≤240 s). Moreover, we found that the separation efficiency of CF-LGMS process can be boosted by the higher number of magnets, the higher MNP concentration and the lower flowrate of MNP solution. To better illustrate the underlying dynamical behaviour of LGMS process, a mathematical model was developed to predict its kinetic profile and separation efficiency (with average error of ∼2.6% compared to the experimental results).
    Matched MeSH terms: Magnetite Nanoparticles*
  15. Fulltext Using 157Gd doped carbon and 157GdF4 nanoparticles in proton-targeted therapy for effectiveness enhancement and thermal neutron reduction: a simulation study
    Tabbakh F, Hosmane NS, Tajudin SM, Ghorashi AH, Morshedian N
    Sci Rep, 2022 Oct 18;12(1):17404.
    PMID: 36258012 DOI: 10.1038/s41598-022-22429-0
    There are two major problems in proton therapy. (1) In comparison with the gamma-ray therapy, proton therapy has only ~ 10% greater biological effectiveness, and (2) the risk of the secondary neutrons in proton therapy is another unsolved problem. In this report, the increase of biological effectiveness in proton therapy has been evaluated with better performance than 11B in the presence of two proposed nanomaterials of 157GdF4 and 157Gd doped carbon with the thermal neutron reduction due to the presence of 157Gd isotope. The present study is based on the microanalysis calculations using GEANT4 Monte Carlo tool and GEANT4-DNA package for the strand breaks measurement. It was found that the proposed method will increase the effectiveness corresponding to the alpha particles by more than 100% and also, potentially will decrease the thermal neutrons fluence, significantly. Also, in this work, a discussion is presented on a significant contribution of the secondary alpha particles in total effectiveness in proton therapy.
    Matched MeSH terms: Nanoparticles*
  16. Fulltext Mesoporous Silica Nanoparticles Improve Oral Delivery of Antitubercular Bicyclic Nitroimidazoles
    Ang CW, Tan L, Qu Z, West NP, Cooper MA, Popat A, et al.
    ACS Biomater Sci Eng, 2022 Oct 10;8(10):4196-4206.
    PMID: 34464089 DOI: 10.1021/acsbiomaterials.1c00807
    Pretomanid and MCC7433, a novel nitroimidazopyrazinone analog, are promising antitubercular agents that belong to the bicyclic nitroimidazole family. Despite possessing high cell permeability, they suffer from poor aqueous solubility and require specialized formulations in order to be orally bioavailable. To address this limitation, we investigated the use of mesoporous silica nanoparticles (MCM-41) as drug carriers. MCM-41 nanoparticles were synthesized using a sol-gel method, and their surface was further modified with amine and phosphonate groups. A simple rotary evaporation method was used to incorporate the compounds of interest into the nanoparticles, leading to a high encapsulation efficiency of ≥86% with ∼10% loading (w/w). An overall significant improvement of solubility was also observed, and the pharmacological activity of pretomanid and MCC7433 was fully retained when tested in vitro against Mycobacterium tuberculosis using these nanocarriers. Amino-functionalized MCM-41 nanoparticles were found to enhance the systemic exposure of MCC7433 in mice (1.3-fold higher Cmax) compared to MCC7433 alone. The current work highlights the potential of using nanoparticles such as mesoporous silica as a carrier for oral delivery of poorly soluble antibacterial agents against tuberculosis.
    Matched MeSH terms: Nanoparticles*
  17. Advances and opportunities in nanoimaging agents for the diagnosis of inflammatory lung diseases
    Masanam HB, Perumal G, Krishnan S, Singh SK, Jha NK, Chellappan DK, et al.
    Nanomedicine (Lond), 2022 Oct;17(25):1981-2005.
    PMID: 36695290 DOI: 10.2217/nnm-2021-0427
    The development of rapid, noninvasive diagnostics to detect lung diseases is a great need after the COVID-2019 outbreak. The nanotechnology-based approach has improved imaging and facilitates the early diagnosis of inflammatory lung diseases. The multifunctional properties of nanoprobes enable better spatial-temporal resolution and a high signal-to-noise ratio in imaging. Targeted nanoimaging agents have been used to bind specific tissues in inflammatory lungs for early-stage diagnosis. However, nanobased imaging approaches for inflammatory lung diseases are still in their infancy. This review provides a solution-focused approach to exploring medical imaging technologies and nanoprobes for the detection of inflammatory lung diseases. Prospects for the development of contrast agents for lung disease detection are also discussed.
    Matched MeSH terms: Nanoparticles*
  18. Molecular insights and therapeutic implications of nanoengineered dietary polyphenols for targeting lung cancer: part II
    Das SS, Tambe S, Prasad Verma PR, Amin P, Singh N, Singh SK, et al.
    Nanomedicine (Lond), 2022 Oct;17(23):1799-1816.
    PMID: 36636965 DOI: 10.2217/nnm-2022-0117
    Flavonoids represent a major group of polyphenolic compounds. Their capacity to inhibit tumor proliferation, cell cycle, angiogenesis, migration and invasion is substantially responsible for their chemotherapeutic activity against lung cancer. However, their clinical application is limited due to poor aqueous solubility, low permeability and quick blood clearance, which leads to their low bioavailability. Nanoengineered systems such as liposomes, nanoparticles, micelles, dendrimers and nanotubes can considerably enhance the targeted action of the flavonoids with improved efficacy and pharmacokinetic properties, and flavonoids can be successfully translated from bench to bedside through various nanoengineering approaches. This review addresses the therapeutic potential of various flavonoids and highlights the cutting-edge progress in the nanoengineered systems that incorporate flavonoids for treating lung cancer.
    Matched MeSH terms: Nanoparticles*
  19. Fulltext Protease-targeting peptide-functionalized porous silicon nanoparticles for cancer fluorescence imaging
    Kanathasan JS, Palanisamy UD, Radhakrishnan AK, Chakravarthi S, Thong TB, Swamy V
    Nanomedicine (Lond), 2022 Sep;17(21):1511-1528.
    PMID: 36382634 DOI: 10.2217/nnm-2022-0017
    Background: Porous silicon (pSi) nanoparticles (NPs) functionalized with suitable targeting ligands are now established cancer bioimaging agents and drug-delivery platforms. With growing interest in peptides as tumor-targeting ligands, much work has focused on the use of various peptides in combination with pSi NPs for cancer theranostics. Here, the authors investigated the targeting potential of pSi NPs functionalized with two types of peptide, a linear 10-mer peptide and its branched (Y-shaped) equivalent, that respond to legumain activity in tumor cells. Results: In vitro experiments established that the linear peptide-pSi NP conjugate had better aqueous stability under tumor conditions and higher binding efficiency (p  0.05) of linear peptide-conjugated pSi NPs in the tumor site within 4 h compared with nonconjugated pSi NPs. These results suggest that the linear peptide-pSi NP formulation is a nontoxic, stable and efficient fluorescence bioimaging agent and potential drug-delivery platform.
    Matched MeSH terms: Nanoparticles*
  20. Fulltext Green Synthesis and Characterization of Silver Nanoparticles of Psidium guajava Leaf Extract and Evaluation for Its Antidiabetic Activity
    Nagaraja S, Ahmed SS, D R B, Goudanavar P, M RK, Fattepur S, et al.
    Molecules, 2022 Jul 06;27(14).
    PMID: 35889209 DOI: 10.3390/molecules27144336
    Diabetes mellitus (DM) and its complications are a severe public health concern due to the high incidence, morbidity, and mortality rates. The present study aims to synthesize and characterize silver nanoparticles (AgNPs) using the aqueous leaf extract of Psidium guajava (PGE) for investigating its antidiabetic activity. Psidium guajava silver nanoparticles (PGAg NPs) were prepared and characterized by various parameters. The in vivo study was conducted using PGE and PGAg NPs in Streptozotocin (STZ)-induced diabetic rats to assess their antidiabetic properties. STZ of 55 mg/kg was injected to induce diabetes. The PGE, PGAg NPs at a dose of 200 and 400 mg/kg and standard drug Metformin (100 mg/kg) were administered daily to diabetic rats for 21 days through the oral route. Blood glucose level, body weight changes, lipid profiles, and histopathology of the rats' liver and pancreas were examined. In the diabetic rats, PGE and PGAg NPs produced a drastic decrease in the blood glucose level, preventing subsequent weight loss and ameliorating lipid profile parameters. The histopathological findings revealed the improvements in pancreas and liver cells due to the repercussion of PGE and PGAg NPs. A compelling effect was observed in all doses of PGE and PGAg NPs; however, PGAg NPs exhibited a more promising result. Thus, from the results, it is concluded that the synthesized PGAg NPs has potent antidiabetic activity due to its enhanced surface area and smaller particle size of nanoparticles.
    Matched MeSH terms: Metal Nanoparticles*
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