Nebulized Hybrid Nanoarchaeosomes: Anti-Inflammatory Activity, Anti-Microbial Activity and Cytotoxicity on A549 Cells.

The properties of two hybrid nanoarchaeosomes (hybrid nanoARCs) made of archaeolipids extracted from the halophilic archaea and combining the properties of archaeolipid bilayers with metallic nanoparticles are explored here. BS-nanoARC, consisting of a nanoARC loaded with yerba mate ( extract (YME)-biogenic silver nanoparticles (BSs), and [BS + BS-nanoARC], consistent of a BS-nanoARC core covered by an outer shell of BSs, were structurally characterized and their therapeutic activities screened. By employing 109 ± 5 µg gallic acid equivalents (GAEs) and 73.

Evaluating the potential of ethyl cellulose/eudragit-based griseofulvin loaded nanosponge matrix for topical antifungal drug delivery in a sustained release pattern.

Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem.

Cholesterol nanoarchaeosomes for alendronate targeted delivery as an anti-endothelial dysfunction agent.

Sodium alendronate (ALN) is a very hydrosoluble and poorly permeable molecule used as an antiresorptive agent and with vascular anticalcifying capacity. Loaded into targeted nanovesicles, its anti-inflammatory activity may be amplified towards extra-osseous and noncalcified target cells, such as severely irritated vascular endothelium. Here cytotoxicity, mitochondrial membrane potential, ATP content, and membrane fluidity of human endothelial venous cells (HUVECs) were determined after endocytosis of ALN-loaded nanoarchaeosomes (nanoARC-Chol(ALN), made of polar lipids from : cholesterol 7:3 w/w, 166 ± 5 nm, 0.

Nanomedicines against Chagas disease: a critical review.

Chagas disease (CD) is the most important endemic parasitosis in South America and represents a great socioeconomic burden for the chronically ill and their families. The only currently available treatment against CD is based on the oral administration of benznidazole, an agent, developed in 1971, of controversial effectiveness on chronically ill patients and toxic to adults. So far, conventional pharmacological approaches have failed to offer more effective and less toxic alternatives to benznidazole.

More Than Pigments: The Potential of Astaxanthin and Bacterioruberin-Based Nanomedicines.

Carotenoids are natural products regulated by the food sector, currently used as feed dyes and as antioxidants in dietary supplements and composing functional foods for human consumption. Of the nearly one thousand carotenoids described to date, only retinoids, derived from beta carotene, have the status of a drug and are regulated by the pharmaceutical sector. In this review, we address a novel field: the transformation of xanthophylls, particularly the highly marketed astaxanthin and the practically unknown bacterioruberin, in therapeutic agents by altering their pharmacokinetics, biodistribution, and pharmacodynamics through their formulation as nanomedicines.

Cationic starch: A functionalized polysaccharide based polymer for advancement of drug delivery and health care system - A review.

Research and development in health care industry is in persistence progression. To make it more patient-friendly or to get maximum benefits from it, special attention to different advanced drug delivery system (ADDS) is employed that delivers the drug at the target site and will be able to sustain/control release of drugs. ADDS should be non-toxic, biodegradable, biocompatible along with desirable showing physicochemical and functional properties.

Inhaled lipid nanocarriers for pulmonary delivery of glucocorticoids: Previous strategies, recent advances and key factors description.

In view of the strong anti-inflammatory activity of glucocorticoids (GC) they are used in the treatment of almost all inflammatory lung diseases. In particular, inhaled GC (IGC) allow high drug concentrations to be deposited in the lung and may reduce the incidence of adverse effects associated with systemic administration. However, rapid absorption through the highly absorbent surface of the lung epithelium may limit the success of localized therapy.

Ether lipids from archaeas in nano-drug delivery and vaccination.

Archaea are microorganisms more closely related to eukaryotes than bacteria. Almost 50 years after being defined as a new domain of life on earth, new species continue to be discovered and their phylogeny organized. The study of the relationship between their genetics and metabolism and some of their extreme habitats has even positioned them as a model of extraterrestrial life forms.

Photodynamic Therapy with Nebulized Nanocurcumin on A549 Cells, Model Vessels, Macrophages and Beyond.

This study aimed to determine the damage mechanisms caused by naturally targeted nanoarchaeosomes made of diether lipids from loaded with curcumin (CUR, nATC), which mediated photodynamic therapy (PDT) on A549 cells and on THP-1-macrophages, two cell types found in airway cancers. The effect of nATC- PDT on vessels modeled with a chicken embryo chorioallantoic membrane (CAM), after dropping the formulations on its surface covered with mucins, was also determined. nATCs are known to efficiently trap CUR for at least six months, constituting easy-to-prepare, stable formulations suitable for nebulization.

anti-melanoma activity of imiquimod in ultradeformable nanovesicles.

Background: The wide spectrum of antitumoral mechanisms of imiquimod (IMQ), made it a good candidate for topical therapy of melanoma. However, physicochemical properties make IMQ formulation a difficult task. Solubility and skin penetration of IMQ are increased when loaded into ultradeformable nanovesicles.

Thymus vulgaris essential oil + tobramycin within nanostructured archaeolipid carriers: A new approach against Pseudomonas aeruginosa biofilms.

Background: Pseudomonas aeruginosa biofilms in the respiratory tract of patients with an excessive inflammatory context are difficult to eradicate. New medicines that simultaneously target biofilms and inflammation should be developed.

Hypothesis: Co-delivery of Thymus vulgaris essential oil (EOT) and tobramycin (TB) by nanostructured archaeolipids carriers (NAC) could support nebulization as well as improve EOT and TB antioxidant, anti-inflammatory and antibiofilm activity.

The Anti-Inflammatory Effect of Nanoarchaeosomes on Human Endothelial Cells.

Archaebacterias are considered a unique source of novel biomaterials of interest for nanomedicine. In this perspective, the effects of nanoarchaeosomes (ARC), which are nanovesicles prepared from polar lipids extracted from the extreme halophilic , on human umbilical vein endothelial cells (HUVEC) were investigated in physiological and under inflammatory static conditions. Upon incubation, ARC (170 nm mean size, -41 mV ζ) did not affect viability, cell proliferation, and expression of intercellular adhesion molecule-1 (ICAM-1) and E-selectin under basal conditions, but reduced expression of both molecules and secretion of IL-6 induced by lypopolysaccharide (LPS), Pam3CSK4 or .

Reparation of an Inflamed Air-Liquid Interface Cultured A549 Cells with Nebulized Nanocurcumin.

The anti-inflammatory, antifibrotic and antimicrobial activities of curcumin (CUR) are missed because of its low solubility in aqueous media, low bioavailability, and structural lability upon oral intake. Soft nanoparticles such as nanoliposomes are not efficient as CUR carriers, since crystalline CUR is expelled from them to physiological media. Nanostructures to efficiently trap and increase the aqueous solubility of CUR are needed to improve both oral or nebulized delivery of CUR.

Preclinical autophagy modulatory nanomedicines: big challenges, slow advances.

Introduction: Autophagy is a critical housekeeping pathway to remove toxic protein aggregates, damaged organelles, providing cells with bioenergetic substrates needed to survive under adverse conditions. Since altered autophagy is associated with diverse diseases, its pharmacological modulation is considered of therapeutic interest. Nanomedicines may reduce the toxicity and improve the activity of toxic autophagy modulatory drugs ().

Macrophage apoptosis using alendronate in targeted nanoarchaeosomes.

Nanoarchaeosomes are non-hydrolysable nanovesicles made of archaeolipids, naturally functionalised with ligand for scavenger receptor class 1. We hypothesized that nitrogenate bisphosphonate alendronate (ALN) loaded nanoarchaeosomes (nanoarchaeosomes(ALN)) may constitute more efficient macrophage targeted apoptotic inducers than ALN loaded nanoliposomes (nanoliposomes (ALN)). To that aim, ALN was loaded in cholesterol containing (nanoARC-chol(ALN)) or not (nanoARC(ALN)) nanoarchaeosomes.

Bacterioruberin from Haloarchaea plus dexamethasone in ultra-small macrophage-targeted nanoparticles as potential intestinal repairing agent.

Oral administration of antioxidant and anti-inflammatory drugs have the potential to improve the current therapy of inflammatory bowel disease. Success of oral treatments, however, depends on the capacity of drugs to remain structurally stable along the gastrointestinal tract, and on the feasibility of accessing the target cells. Delivering anti-inflammatory and antioxidant drugs to macrophages using targeted nanoparticles, could make treatments more efficient.

Fast Biofilm Penetration and Anti-PAO1 Activity of Nebulized Azithromycin in Nanoarchaeosomes.

Azithromycin (AZ) is a broad-spectrum antibiotic with anti-inflammatory and antiquorum sensing activity against biofilm forming bacteria such as . AZ administered by oral or parenteral routes, however, neither efficiently accesses nor remains in therapeutic doses inside pulmonary biofilm depths. Instead, inhaled nanocarriers loaded with AZ may revert the problem of low accessibility and permanence of AZ into biofilms, enhancing its antimicrobial activity.

Superoxide dismutase in nanoarchaeosomes for targeted delivery to inflammatory macrophages.

Oxidative stress plays an essential role in the pathogenesis and progression of inflammatory bowel disease. Co-administration of antioxidants and anti-inflammatory drugs has shown clinical benefits. Due to its significant reactive oxygen species (ROS) scavenging ability, great interest has been focused on superoxide dismutase (SOD) for therapeutic use.

The anti MRSA biofilm activity of Thymus vulgaris essential oil in nanovesicles.

Background: Thymus vulgaris essential oil (T) could be an alternative to classical antibiotics against bacterial biofilms, which show increased tolerance to antibiotics and host defence systems and contribute to the persistence of chronic bacterial infections.

Hypothesis: A nanovesicular formulation of T may chemically protect the structure and relative composition of its multiple components, potentially improving its antibacterial and antibiofilm activity.

Study Design: We prepared and structurally characterized T in two types of nanovesicles: nanoliposomes (L80-T) made of Soybean phosphatidylcholine (SPC) and Polysorbate 80 (P80) [SPC:P80:T 1:0.

Novel imiquimod nanovesicles for topical vaccination.

Development of needle and pain free noninvasive immunization procedures is a top priority for public health agencies. In this work the topical adjuvant activity of the immunomodulator imiquimod (IMQ) carried by ultradeformable archaeosomes (UDA) (nanovesicles containing sn-2,3 ether linked phytanyl saturated archaeolipids) was surveyed and compared with that of ultradeformable liposomes lacking archaeolipids (UDL) and free IMQ, using the model antigen ovalbumin and a seasonal influenza vaccine in Balb/c mice. UDA (250 ± 94 nm, -26 ± 4 mV Z potential) induced higher IMQ accumulation in human skin and higher production of TNF-α and IL-6 by macrophages and keratinocytes than free IMQ and UDL.

Make It Simple: (SR-A1+TLR7) Macrophage Targeted NANOarchaeosomes.

Hyperhalophilic archaebacteria exclusively produce sn2,3 diphytanylglycerol diether archaeolipids, unique structures absent in bacteria and eukaryotes. Nanovesicles made of archaeolipids known as nanoarchaeosomes (nanoARC), possess highly stable bilayers, some of them displaying specific targeting ability. Here we hypothesize that nanoARC made from archaebacteria, may constitute efficient carriers for the TLR7 agonist imiquimod (IMQ).

Nebulizing novel multifunctional nanovesicles: the impact of macrophage-targeted-pH-sensitive archaeosomes on a pulmonary surfactant.

In this study, a NE-U22 vibrating mesh Omron nebulizer was used to deliver the Lissamine™ rhodamine B 1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine triethylammonium salt (Rh-PE) and 8-hydroxypyrene-1,3,6-trisulfonic acid trisodium salt (HPTS)/p-xylene-bis-pyridinium bromide (DPX) double-labelled macrophage-targeted pH-sensitive archaeosomes (ApH, 174 ± 48 nm, -30 ± 13 mV unilamellar nanovesicles made of dioleoyl-sn-glycero-3-phosphoethanolamine: [total polar archaeolipids from the hyperhalophile archaebacteria Halorubrum tebenquichense]: cholesteryl hemisuccinate 4.2 : 2.8 : 3 w : w : w) to J774A.

Ultra-small solid archaeolipid nanoparticles for active targeting to macrophages of the inflamed mucosa.

Aim: Develop nanoparticulate agents for oral targeted delivery of dexamethasone (Dex) to macrophages of inflamed mucosa.

Materials & Methods: Solid archaeolipid nanoparticles (SAN-Dex) (compritol/Halorubrum tebenquichense polar archaeolipids/soybean phosphatidylcholine/Tween-80 4; 0.9; 0.

Topical vaccination with super-stable ready to use nanovesicles.

Ultradeformable archaeosomes (UDA) are nanovesicles made of total polar archaeolipids (TPA) from the archaea Halorubrum tebenquichense, soybean phosphatidylcholine and sodium cholate (3:3:1w/w). Fresh dispersions of UDA including different type of antigens are acknowledged as efficient topical vaccination agents. UDA dispersions however, if manufactured for pharmaceutical use, have to maintain colloidal stability upon liposomicidal processes such as sterilization and lyophilization (UDA), needed to extend shelf life during storage.