Trinitroglycerin (TNG) with remarkable angiogenic, antibacterial, and antioxidative activity is a promising candidate to govern wound healing capacity. However, its clinical administration is limited due to associated complications and NO short half-life. In the current study, TNG-loaded chitosan nanogels (TNG-Ngs) were examined in-vitro and in-vivo to gain insight into their clinical application.
View Article and Find Full Text PDFAim And Background: Trinitroglycerin (TNG) is a remarkable NO-releasing agent. Here, we synthesized TNG based on chitosan Nanogels (Ngs) for ameliorating complications associated with high-dose TNG administration.
Method: TNG-Ngs fabricated through ionic-gelation technique.
Multifunctional nanocarriers are increasingly promising for disease treatment aimed at finding effective therapy and overcoming barriers in drug delivery. Herein, valine conjugated chitosan (VLCS) was used for surface modification of nanocarriers (NCs) based on Poly (ε-caprolactone)-Poly (ethylene glycol)-Poly (ε-caprolactone) (PCL-PEG-PCL) triblock copolymers (NCs@VLCS). The nanocarriers were co-loaded with rivastigmine (RV) and quercetin (QT) to yield the final RV/QT-NCs@VLCS as a multifunctional nanocarrier for Alzheimer's disease (AD) treatment.
View Article and Find Full Text PDFJ Biomed Mater Res B Appl Biomater
September 2023
Wide availability and easy accessibility of acetaminophen oral dosage forms increase the risk of intentional poisoning or unintentional organ toxicity, leading to a wide range of liver failure, nephrotoxicity, and neurotoxicity. In this study, an attempt was made to improve oral bioavailability and reduce the toxicity of acetaminophen using nanosuspension technology. The acetaminophen nanosuspensions (APAP-NSs) were prepared by a nano-precipitation method using polyvinyl alcohol and hydroxypropylmethylcellulose as stabilizers.
View Article and Find Full Text PDFThe blood-brain barrier (BBB) acts as a physical/biochemical barrier that protects brain parenchyma from potential hazards exerted by different xenobiotics found in the systemic circulation. This barrier is created by "a lipophilic gate" as well as a series of highly organized influx/efflux mechanisms. The BBB bottleneck adversely affects the efficacy of chemotherapeutic agents in treating different CNS malignancies such as glioblastoma, an aggressive type of cancer affecting the brain.
View Article and Find Full Text PDFSonodynamic therapy (SDT) has considerably revolutionized the healthcare sector as a viable noninvasive therapeutic procedure. It employs a combination of low-intensity ultrasound and chemical entities, known as a sonosensitizer, to produce cytotoxic reactive oxygen species (ROS) for cancer and antimicrobial therapies. With nanotechnology, several unique nanoplatforms are introduced as a sonosensitizers, including, titanium-based nanomaterials, thanks to their high biocompatibility, catalytic efficiency, and customizable physicochemical features.
View Article and Find Full Text PDFTargeted delivery of neurological therapeutic to the brain has been attracting more and more attention to the treatment of central nervous system (CNS) diseases. Nonetheless, the main obstacle in this road map is the existence of a blood-brain barrier (BBB) which limits the penetration efficiency of most CNS drugs into the brain parenchyma. This present investigation describes a facile synthetic strategy to prepare a highly biocompatible calcium-doped mesoporous silica nanoparticles (MSNs) functionalized by polysorbate-80 (PS) as targeting ligand to deliver rivastigmine (RV) into the brain via crossing the BBB.
View Article and Find Full Text PDFThis study prepared a novel three-dimensional nanocomposite scaffold by the surface modification of PCL/chitosan nanofiber/net with alginate hydrogel microlayer, hoping to have the privilege of both nanofibers and hydrogels simultaneously. Bead free randomly oriented nanofiber/net (NFN) structure composed of chitosan and polycaprolactone (PCL) was fabricated by electrospinning method. The low surface roughness, good hydrophilicity, and high porosity were obtained from the NFN structure.
View Article and Find Full Text PDFIn the present study, with the aim of improving the permeability of methotrexate (MTX) to the brain, the lipophilic MTX prodrugs containing the ester functional moiety were synthesized. The chemical structure of synthesized prodrugs was characterized and confirmed by FT-IR, NMR and mass spectral studies. Based on the results of in vitro cytotoxic studies, all of the synthesized prodrugs led to decrease in the IC50 in 72 h on U87 cancer cell line and the best result was observed for dihexyl methotrexate (MTX-DH) in comparison with free MTX, which led to decrease the IC50 amount up to 6 folds.
View Article and Find Full Text PDFSilica plays an effective role in collagen creation; hence, the degradation products of silica-based materials accelerate wound healing. In this regard, chitosan/polyethylene oxide/silica hybrid nanofibers were prepared by the combining the sol-gel method with electrospinning technique to accelerate the wound healing process. Ciprofloxacin, as an antibacterial drug, was then added to the electrospinning mixture.
View Article and Find Full Text PDFMany drug molecules that are currently in the market suffer from short half-life, poor absorption, low specificity, rapid degradation, and resistance development. The design and development of lipophilic prodrugs can provide numerous benefits to overcome these challenges. Fatty acids (FAs), which are lipophilic biomolecules constituted of essential components of the living cells, carry out many necessary functions required for the development of efficient prodrugs.
View Article and Find Full Text PDFAlzheimer's disease (AD) is one of the most common types of neurodegenerative diseases which is accompanied by irreversible neuronal damage, learning difficulties, memory impairments, and cognitive disorders. The cholinergic system is destroyed during AD pathogenesis, leading to the major symptoms of the disease. Although in severe stages AD is life threatening, to date no absolute treatment has been found for this illness and some palliative options are available.
View Article and Find Full Text PDFThe objective of this study was to formulate and investigate the neuropharmacokinetics and pharmacodynamics of rivastigmine (Riv) loaded methoxy poly(ethylene glycol)--poly(ε-caprolactone) (MPEG-PCL) nanoparticles (Riv-NPs) in rats after IV administration. The MPEG-PCL was synthesized via ring-opening polymerization of ε-caprolactone by MPEG and used to prepare Riv-NPs by the nanoprecipitation method. Response surface D-optimal design was applied to optimize Riv-NPs drug delivery system.
View Article and Find Full Text PDFThe main scope of present investigation was preparation and physicochemical characterization of solid lipid nanoparticles (SLNs) loaded by α-tocopherol acetate (ATA). ATA-loaded nanoparticles were prepared by solvent injection-homogenization technique using stearic acid as the solid lipid, phosphatidylcholine as the stabilizer and finally coated by chitosan with the aim of increasing z-potential and also having a more stable nano-formulation. Then, characterization of SLNs has been conducted using dynamic light scattering (DLS), zeta potential measurement, Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).
View Article and Find Full Text PDFJ Biomed Mater Res B Appl Biomater
April 2020
The aim of the present study was to develop modified nanoemulsions to improve the oral bioavailability and pharmacokinetics of a poor water-soluble drug, repaglinide (RPG). The repaglinide-loaded nanoemulsions (RPG-NEs) were prepared from olive oil as internal phase, span 80, tween 80, and poloxamer 188 as emulsifiers, using homogenization technique. The mean droplet size, zeta potential, and entrapment efficiency of RPG-NEs were 86.
View Article and Find Full Text PDFAlzheimer's disease (AD) is one of the most common neurodegenerative diseases and is caused by accumulation of amyloid-β (Aβ) peptide and is associated with neurological abnormalities in learning and memory. The protective role of curcumin on nerve cells, along with a potent antioxidant and free radical scavenging activity, has been widely studied. However, its low bioavailability and limited transport ability across the blood-brain barrier are two major drawbacks of its application in the treatment of different neurodegenerative diseases.
View Article and Find Full Text PDFIndinavir (IDV) is a potent HIV protease inhibitor used in the treatment of human immunodeficiency virus (HIV). IDV is a weak base with limited aqueous solubility in its unprotonated form; therefore, solubility of IDV in the gastrointestinal tract fluids is the rate-limiting step of its absorption and onset of action. However, in many cases, drugs are not absorbed well in the gastrointestinal tract; polymer nanoparticles were recognized as an effective carrier system for drug encapsulation and are now studied as a vehicle for oral delivery of insoluble compounds.
View Article and Find Full Text PDFBacterial infections are the main cause of chronic infections and even mortality. In fact, due to extensive use of antibiotics and, then, emergence of antibiotic resistance, treatment of such infections by conventional antibiotics has become a major concern worldwide. One of the promising strategies to treat infection diseases is the use of nanomaterials.
View Article and Find Full Text PDFThe blood brain barrier is a major obstacle to the entry of the majority of CNS-active agents. In the present research, the potential of magnetic polymeric micelles (MPMs) for brain-targeting of naproxen was evaluated. The MPMs were made of methoxy poly(ethyleneglycol)-poly (caprolactone) copolymer and super paramagnetic iron oxide nanoparticles (SPIONs).
View Article and Find Full Text PDFDespite enormous efforts, treatment of CNS diseases remains challenging. One of the main issues causing this situation is limited CNS access for the majority of drugs used as part of the therapeutic regimens against life-threatening CNS diseases. Regarding the inarguable position of the nanocarrier systems in neuropharmacokinetic enhancement of the CNS drugs, this review discusses the latest findings on nanoemulsions (NEs) as one of the most promising candidates of this type, to overcome the challenges of CNS drug delivery.
View Article and Find Full Text PDFDrug Metab Pers Ther
February 2019
Considerable development in the application of injectable drug delivery systems for cancer therapy has occurred in the last few decades. These improvements include liposomes, lipid nanoparticles (LNPs), and other nanoparticles with or without macromolecular conjugates. For example, liposomal doxorubicin modified by poly(ethylene glycol) (Doxil) was the first liposome with anti-cancer effects which was approved by the US Food and Drug Administration, whereas Abraxane (modified albumin nanoparticles loaded by paclitaxel) was recently confirmed for the treatment of breast cancer.
View Article and Find Full Text PDFPurpose: As an anti-retroviral Protease Inhibitor (PI), Indinavir (IDV) is part of the regimen known as Highly Active Anti-Retroviral Therapy (HAART) widely used for Human Immunodeficiency Virus (HIV) infection. The drug efficiency in treatment of the brain manifestations of HIV is, however, limited which is mainly due to the efflux by P-glycoprotein (P-gp) expressed at the Blood-Brain Barrier (BBB).
Methods: To overcome the BBB obstacle, NLCs were used in this study as carriers for IDV, which were optimized through two steps: a "one-factor-at-a-time" screening followed by a systematic multiobjective optimization.
Objective: Indinavir (IDV), an antiretroviral protease inhibitor used in treatment of HIV infection, has limited entry into brain due to efflux by the P-glycoprotein presented in blood-brain barrier. The aim of present study was to develop lactoferrin-treated nanoemulsion containing indinavir (Lf-IDV-NEs) for delivery to brain.
Methods: Indinavir-loaded nanoemulsions (IDV-NEs) were prepared by high-speed homogenization method, and then lactoferrin was coupled to IDV-NEs by water soluble EDC method.
Curcumin is a multitherapeutic agent with great therapeutic potential in central nervous system (CNS) diseases. In the current study, curcumin was encapsulated in solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the purpose of increasing brain accumulation. The preparation processes have been optimized using experimental design and multiobjective optimization methods.
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