Nanoemulsions and nanocapsules loaded with Melaleuca alternifolia essential oil for sepsis treatment.

Sepsis represents a complex clinical syndrome that results from a harmful host response to infection. The infections most associated with sepsis are pneumonia, intra-abdominal infection, and urinary tract infection. Tea tree oil (TTO) has shown high antibacterial activity; however, it exhibits low aqueous solubility and high volatility, which have motivated its nanoencapsulation. In this study, the performance of nanoemulsions (NE) and nanocapsules (NC) loaded with TTO was compared. These systems were prepared by spontaneous emulsification and nanoprecipitation methods, respectively. Poly-ε-caprolactone or Eudragit® RS100 were tested as polymers for NCs whereas Tween® 80 or Pluronic® F68 as surfactants in NE preparation. Pluronic® F68 and Eudragit® RS100 resulted in more homogeneous and stable nanoparticles. In accelerated stability studies at 4 and 25 °C, both colloidal suspensions (NC and NE) were kinetically stable. NCs showed to be more stable to photodegradation and less cytotoxic than NEs. After sepsis induction by the cecal ligation and puncture (CLP) model, both NE and NC reduced neutrophil infiltration into peritoneal lavage (PL) and kidneys. Moreover, the systems increased group thiols in the kidney and lung tissue and reduced bacterial growth in PL. Taken together, both systems showed to be effective against injury induced by sepsis; however, NCs should be prioritized due to advantages in terms of cytotoxicity and physicochemical stability.

Effect of Inlet Air Temperature and Quinoa Starch/Gum Arabic Ratio on Nanoencapsulation of Bioactive Compounds from Andean Potato Cultivars by Spray-Drying.

Nanoencapsulation of native potato bioactive compounds by spray-drying improves their stability and bioavailability. The joint effect of the inlet temperature and the ratio of the encapsulant (quinoa starch/gum arabic) on the properties of the nanocapsules is unknown. The purpose of this study was to determine the best conditions for the nanoencapsulation of these compounds. The effects of two inlet temperatures (96 and 116 °C) and two ratios of the encapsulant (15 and 25% w/v) were evaluated using a factorial design during the spray-drying of native potato phenolic extracts. During the study, measurements of phenolic compounds, flavonoids, anthocyanins, antioxidant capacity, and various physical and structural properties were carried out. Higher inlet temperatures increased bioactive compounds and antioxidant capacity. However, a higher concentration of the encapsulant caused the dilution of polyphenols and anthocyanins. Instrumental analyses confirmed the effective encapsulation of the nuclei in the wall materials. Both factors, inlet temperature, and the encapsulant ratio, reduced the nanocapsules' humidity and water activity. Finally, the ideal conditions for the nanoencapsulation of native potato bioactive compounds were determined to be an inlet temperature of 116 °C and an encapsulant ratio of 15% w/v. The nanocapsules obtained show potential for application in the food industry.

Immunostimulant effects of diet supplementation with yellow (Pouteria campechiana), white (Casimiroa edulis), and black (Diospyros digyna) sapote nanocapsules on laying hens: in vitro and in vivo study.

Poultry is commonly infected by different bacteria and parasites in the environment, resulting in increased morbidity and mortality, but immunostimulants have been enhancing non-specific defense mechanisms conferring laying hens' protection. For this purpose, the pulp of yellow (Pouteria campechiana), white (Casimiroa edulis), and black (Diospyros digyna) sapotes were nanoencapsulated (YWB-SN) and evaluated in laying hens' peripheral blood leukocytes to test their addition to the experimental diets at a concentration of 0.5% (5g/kg of dry food) for 1 month (with two samples at days 15 and 30). The YWB-SN were safe when exposed to peripheral blood leukocytes (PBLs). The in vitro experiment showed that these nanocapsules enhanced reactive oxygen species production, and B-SN stimulated phagocytosis activity. Concerning the proinflammatory cytokine (TNF-α) transcription, this gene was upregulated after W-SN stimulation, while B-SN upregulated the IgG gene expression significantly. IgM was upregulated with any YBW-SN in PBLs after 24 h of stimulation. The in vivo study showed a notable B-SN immunostimulation in serum and an upregulation of TNF-α, IgM, and IgG mRNA transcription. Therefore, this study provides a new result of the yellow, white, and black sapote nanocapsules as a functional food for the poultry industry, highlighting the black sapote Diospyros digyna immunostimulant effect.

Effect of nanocapsules containing docosahexaenoic acid in mice with chronic inflammation.

BACKGROUND: Omega 3 fatty acids, such as docosahexaenoic acid (DHA) have been widely consumed as supplements to control chronic inflammation. Nanocapsules containing DHA (MLNC-DHA-a1) were developed and showed excellent stability. Thus, our objective was to evaluate the effect of MLNC-DHA-a1 nanocapsules on biomarkers of chronic inflammation. METHODS: Cells viability was determined by flow cytometry. The uptake of MLNC-DHA-a1 nanocapsules by macrophages and their polarization were determined. In vivo, LDLr(-,-) mice were fed a Western diet to promote chronic inflammation and were treated with MLNC-DHA-a1 nanocapsules, intravenously injected via the caudal vein once a week for 8 weeks. RESULTS: MLNC-DHA-a1 nanocapsules decreased the concentration of TNFα (p = 0.02) in RAW 264.7 cells compared to the non-treated group (NT), with no changes in IL-10 (p = 0.29). The nanocapsules also exhibited an increase in the M2 (F4/80+ CD206) phenotype (p < 0.01) in BMDM cells. In vivo, no difference in body weight was observed among the groups, suggesting that the intervention was well tolerated. However, compared to the CONT group, MLNC-DHA-a1 nanocapsules led to an increase in IL-6 (90.45 ×13.31 pg/mL), IL-1ß (2.76 ×1.34 pg/mL) and IL-10 (149.88 ×2.51 pg/mL) levels in plasma. CONCLUSION: MLNC-DHA-a1 nanocapsules showed the potential to promote in vitro macrophage polarization and were well-tolerated in vivo. However, they also increased systemic pro-inflammatory cytokines. Therefore, considering that this immune response presents a limitation for clinical trials, further studies are needed to identify the specific compound in MLNC-DHA-a1 that triggered the immune response. Addressing this issue is essential, as MLNC-DHA-a1 tissue target nanocapsules could contribute to reducing chronic inflammation.

Clove essential oil loaded chitosan nanocapsules on quality and shelf-life of blueberries.

In this study, the formation of clove essential oil loaded chitosan nanocapsules (CEO/CS-NCs) was achieved by the ionotropic gelation technology. The spherical shape and core-shell structure of CEO/CS-NCs were characterized by SEM, TEM, and FT-IR. CEO/CS-NCs have a reasonable encapsulation efficiency rate of 39 % and an average size of 253.63 nm. The simulated release of CEO/CS-NCs in a citric acid buffer solution shows that the nano-encapsulation technology could control the sustained release of clove essential oil (CEO). The shelf life of untreated blueberries at room temperature is only about 3 days, while CEO/CS-NCs combined with low-temperature storage can extend the shelf life to about 12 days. The quality characteristic of blueberries, including fruit firmness and moisture content, were effectively maintained, and the rotting rate of blueberries was significantly reduced with CEO/CS-NCs. As a natural preservative, CEO/CS-NCs have a good antioxidant activity close to the commercial antioxidant butylated hydroxytoluene (BHT) and a high antibacterial activity against pathogenic bacteria (PB) isolated from naturally occurring blueberries. Therefore, this study not only gives a theoretical basis for the development of CEO as a commercial preservative but also provides a practical solution to solve the protection challenge of preserving blueberries.

The Anti-Arthritic Activity of Diclofenac Lipid-Core Nanocapsules: Stereological Analysis Showing More Protection of Deep Joint Components.

Diclofenac is the most prescribed nonsteroidal anti-inflammatory drug worldwide and is used to relieve pain and inflammation in inflammatory arthritis. Diclofenac is associated with serious adverse effects, even in regular-dose regimens. Drug delivery systems can overcome this issue by reducing adverse effects and optimizing their efficacy. This study evaluated the activity of lipid-core nanocapsules loaded with diclofenac (DIC-LNCs) in an experimental model of adjuvant-induced arthritis. The diclofenac nanoformulation was obtained via self-assembly. A stereological analysis approach was applied for the morphological quantification of the volume, density, and cellular profile count of the metatarsophalangeal joints of rats. Proinflammatory cytokines and biochemical profiles were also obtained. Our results showed that the diclofenac nanocapsule DIC-LNCs were able to reduce arthritis compared with the control group and the DIC group. DIC-LNCs efficiently reduced proinflammatory cytokines, C-reactive protein, and xanthine oxidase levels. Additionally, DIC-LNCs reduced the loss of synoviocytes and chondrocytes compared with the DIC (p < 0.05) and control groups (p < 0.05). These data suggest that DIC-LNCs have anti-arthritic activity and preserve joint components, making them promising for clinical use.

Novel Oxygen- and Curcumin-Laden Ionic Liquid@Silica Nanocapsules for Enhanced Antimicrobial Photodynamic Therapy.

The efficiency of photodynamic therapy is often limited by the scarcity of oxygen at the target site. To address this problem, this work proposes the development of a new nanosystem for antimicrobial photodynamic therapy applications (aPDT) where the natural-origin photosensitizer curcumin (CUR) is immersed in an oxygen-rich environment. Inspired by the perfluorocarbon-based photosensitizer/O2 nanocarriers reported in the literature, we developed a new type of silica nanocapsule containing curcumin dissolved in three hydrophobic ionic liquids (ILs) with high oxygen dissolving capacities. The nanocapsules (CUR-IL@ncSi), prepared by an original oil-in-water microemulsion/sol-gel method, had a high IL content and exhibited clear capacities to dissolve and release significant amounts of oxygen, as demonstrated by deoxygenation/oxygenation studies. The ability of CUR-IL solutions and of CUR-IL@ncSi to generate singlet oxygen (1O2) upon irradiation was confirmed by the detection of 1O2 phosphorescence at 1275 nm. Furthermore, the enhanced capacities of oxygenated CUR-IL@ncSi suspensions to generate 1O2 upon irradiation with blue light were confirmed by an indirect spectrophotometric method. Finally, preliminary microbiological tests using CUR-IL@ncSi incorporated into gelatin films showed the occurrence of antimicrobial effects due to photodynamic inactivation, with their relative efficiencies depending on the specific IL in which curcumin was dissolved. Considering these results, CUR-IL@ncSi has the potential to be used in the future to develop biomedical products with enhanced oxygenation and aPDT capacities.

Nanotechnology Promoting the Development of Products from the Biodiversity of the Asteraceae Family.

Biodiversity is a hallmark of the Asteraceae family. Several species are known for their pharmacological potential. The search for new substances has permeated the chemistry of natural products for years. However, the development of a final product is still a challenge. Plant extracts have physicochemical characteristics that sometimes hinder administration, requiring a formulation. In this context, nanotechnology emerges as a tool to improve the pharmacokinetic parameters of several pharmacologically active substances. Nanoemulsions, liposomes, and nanoparticles are used to carry the active ingredients and thus improve therapeutic action, especially for substances with solubility and absorption problems. This paper aimed at compiling all the studies that used nanotechnology to develop formulations from species of the Asteraceae family from 2010 to 2021 in a literature review. The search showed that nanoemulsions are the most developed formulation associated with essential oils. The use of nanotechnology promoted an improvement in the pharmacokinetic parameters of active substances.

Bio-Based Nano-Enabled Cosmetic Formulations for the Treatment of Cutibacterium acnes-Associated Skin Infections.

Acne is a common chronic skin condition with serious physical and psychosocial consequences. In some cases, the appearance of pimples, whiteheads, or blackheads on the face, neck, and back may lead to scarring, disfiguring, depression, frustration, and anxiety in patients. Current treatments rely on antibiotics to eradicate Cutibacterium acnes (C. acnes), the bacterium responsible for this skin condition. However, these approaches do not scavenge the reactive oxidative species (ROS) generated during disease development and raise concerns about the increase in antimicrobial resistance. In this study, an environmentally friendly and cost-effective self-assembly nanoencapsulation technology based on zein, a bio-based hydrophobic protein, was employed to produce multifunctional essential oil (EO)-loaded nanocapsules (NCs) with superior antioxidant and bactericidal activity toward C. acnes. The NCs displayed "smart" release of the active cargo only under the conditions that were conducive to acne proliferation on skin. Once incorporated into creams, the EO-loaded NCs led to a complete inhibition of C. acnes and demonstrated the capacity to scavenge ROS, thus preventing damage to human skin cells. The in vitro permeation studies revealed that the nanoformulated EO was able to penetrate through the epidermis, indicating its potential for the treatment of skin diseases, such as acne.

Copaiba Oil-Loaded Polymeric Nanocapsules: Production and In Vitro Biosafety Evaluation on Lung Cells as a Pre-Formulation Step to Produce Phytotherapeutic Medicine.

Copaiba oil has been largely used due to its therapeutic properties. Nanocapsules were revealed to be a great nanosystem to carry natural oils due to their ability to improve the bioaccessibility and the bioavailability of lipophilic compounds. The aim of this study was to produce and characterize copaiba oil nanocapsules (CopNc) and to evaluate their hemocompatibility, cytotoxicity, and genotoxicity. Copaiba oil was chemically characterized by GC-MS and FTIR. CopNc was produced using the nanoprecipitation method. The physicochemical stability, toxicity, and biocompatibility of the systems, in vitro, were then evaluated. Β-bisabolene, cis-α-bergamotene, caryophyllene, and caryophyllene oxide were identified as the major copaiba oil components. CopNc showed a particle size of 215 ± 10 nm, a polydispersity index of 0.15 ± 0.01, and a zeta potential of -18 ± 1. These parameters remained unchanged over 30 days at 25 ± 2 °C. The encapsulation efficiency of CopNc was 54 ± 2%. CopNc neither induced hemolysis in erythrocytes, nor cytotoxic and genotoxic in lung cells at the range of concentrations from 50 to 200 µg·mL-1. In conclusion, CopNc showed suitable stability and physicochemical properties. Moreover, this formulation presented a remarkable safety profile on lung cells. These results may pave the way to further use CopNc for the development of phytotherapeutic medicine intended for pulmonary delivery of copaiba oil.

Copaiba essential oil loaded-nanocapsules film as a potential candidate for treating skin disorders: preparation, characterization, and antibacterial properties.

Infections have emerged as a novel target in managing skin and mucosa diseases. Bacterial resistance to antimicrobials and biofilm elimination from surfaces remains a challenge. Because polymeric nanocapsules (NC) can increase antimicrobial activity, this study aimed to produce and characterize NC into chitosan films (CSF). Copaiba essential oil (CO) presents antimicrobial activity and was chosen to load NC. In addition, the antibacterial activity was evaluated to obtain a new biodegradable polymeric platform system with the potential to treat topical diseases associated with bacterial infections. The CO-NC produced by nanoprecipitation presented particle size lower than 250 nm, negative charge, and encapsulation efficiency higher than 70 %. Direct incorporation of CO into CSF (CO-CSF) by casting method worsened the film's characteristics. However, incorporating CO-NC into CSF (CO-NC-CSF) avoided these drawbacks demonstrating improved physical, mechanical, morphological, and topographical properties. FTIR results demonstrated possible intermolecular interactions among the polymers and CO. The CO-NC-CSF and CO-CSF presented antibacterial properties against Staphylococcus aureus, and Pseudomonas aeruginosa, especially the formulation containing 1 % of CO. These results indicated that CO-NC-CSF is a promising candidate for treating skin disorders.

Ashwagandha-loaded nanocapsules improved the behavioral alterations, and blocked MAPK and induced Nrf2 signaling pathways in a hepatic encephalopathy rat model.

Ashwagandha (ASH), a vital herb in Ayurvedic medicine, demonstrated potent preclinical hepato- and neuroprotective effects. However, its efficacy is limited due to low oral bioavailability. Accordingly, we encapsulated ASH extract in chitosan-alginate bipolymeric nanocapsules (ASH-BPNCs) to enhance its physical stability and therapeutic effectiveness in the gastrointestinal tract. ASH-BPNC was prepared by emulsification followed by sonication. The NCs showed small particle size (< 220 nm), zeta-potential of 25.2 mV, relatively high entrapment efficiency (79%), physical stability at acidic and neutral pH, and in vitro release profile that extended over 48 h. ASH-BPNC was then investigated in a thioacetamide-induced hepatic encephalopathy (HE) rat model. Compared with free ASH, ASH-BPNC improved survival, neurological score, general motor activity, and cognitive task-performance. ASH-BPNC restored ALT, AST and ammonia serum levels, and maintained hepatic and brain architecture. ASH-BPNC also restored GSH, MDA, and glutathione synthetase levels, and Nrf2 and MAPK signaling pathways in liver and brain tissues. Moreover, ASH-BPNC downregulated hepatic NF-κB immunohistochemical expression. Moreover, the in vivo biodistribution studies demonstrated that most of the administered ASH-BPNC is accumulated in the brain and hepatic tissues. In conclusion, chitosan-alginate BPNCs enhanced the hepatoprotective and neuroprotective effects of ASH, thus providing a promising therapeutic approach for HE.

Application of the Ugi reaction for preparation of submicron capsules based on sugar beet pectin.

The Ugi four-component condensation in diluted liposomal suspensions was used to prepare pectin-based submicron capsules. A set of isocyanides and aldehydes was used to optimize the synthesis of capsule shells. Modified sugar beet pectin was selected as a natural polymer with pronounced surface activity to create a capsule shell. At first, liposomal composition was optimized in order to select suitable conditions for capsule formation. Then, the wide set of capsules constructed on modified sugar beet pectin scaffold has been synthesized. The choice was determined by level of substitution degree and possible chemical diversity of the modified surface. Detailed characterization of products has been performed for polysaccharide particles with liposomal core prepared with various processing parameters (concentration, cross-linking components, the density of linkage). The chemical structure, average size, polydispersity index, morphology, stability, and cytotoxicity of obtained particles have been investigated in dependence on the shell content. The obtained submicrometer cross-linked capsules (220-240 nm) with controlled colloidal properties showed high stability and low toxicity. Thus, the proposed carriers have a great potential as sustained drug delivery systems for different administration routes.

Thermosensitive and mucoadhesive hydrogel containing curcumin-loaded lipid-core nanocapsules coated with chitosan for the treatment of oral squamous cell carcinoma.

Buccal drug administration may be chosen as a medication route to treat various diseases for local or systemic effects. This study proposes the development of a thermosensitive hydrogel containing curcumin-loaded lipid-core nanocapsules coated with chitosan to increase mucoadhesion, circumventing several limitations of this route of administration. Hydroxypropylmethylcellulose and Poloxamer® 407 were incorporated for hydrogel production. Physicochemical characterization parameters, such as particle size distribution, mean diameter, polydispersity index, zeta potential, and morphology, were analyzed. Spherical homogeneous particles were obtained with average diameter, of 173 ± 22 nm for LNCc (curcumin lipid-core nanocapsules) and 179 ± 48 nm for CLNCc (chitosan-curcumin lipid-core nanocapsules). A PDI equal to 0.09 ± 0.02 for LNCc and 0.26 ± 0.01 for CLNCc confirmed homogeneity. Tensile analysis and washability test on porcine buccal mucosa indicated higher mucoadhesion for hydrogels in comparison to the nanocapsules in suspension, remaining on the mucous membrane up to 8 h (10.92 ± 3.95 µg of curcumin washed for H-LNCc and 28.41 ± 24.47 µg for H-CLNCc) versus the latter, which remained washed on the membrane for 90 min only (62.60 ± 4.72 µg for LNCc and 52.08 ± 1.63 µg for CLNCc). The irritant potential (IR) of the formulations was evaluated by the hen's egg chorioallantoic membrane test (HET-CAM), with no irritation phenomena observed. Formulations were tested for their efficacy in an in vitro model against oral squamous cancer cell line, showing a significant reduction in cell viability on all tested groups. These findings demonstrated that the proposed nanosystem is mucoadhesive and has potential to deliver buccal treatments.

Introducing potato starch-ecofriendly silver nanoparticles as a novel binary system for nanoencapsulation of riboflavin.

Riboflavin (Rf), an externally supplied nutrient, is highly photosensitive, and should be protected from sunlight once used in food and pharmaceutical manufacturing. The applications of encapsulated Rf have recently developed due to their therapeutic properties. In this study, the use of green silver nanoparticles (AgNPs) synthesized by Rosa damascena mill L. extract to control the encapsulation efficiency of Rf in potato starch was demonstrated for the first time. Starch/Rf, Starch/AgNPs/Rf and Starch/AgNPs nanocapsules were characterized by Fourier-transform infrared, field emission scanning electron microscopy, differential scanning calorimetry, and brunauer-Emmett-Teller techniques. The obtained results showed that the presence of AgNPs reduces Rf nanocapsules size (from 340 to 327 nm), increases the encapsulation efficiency (21.14 ± 0.62 to 92.52 ± 1.32 %) and improves the thermal stability, antibacterial and antioxidant activities. Moreover, UV-vis spectroscopy demonstrated the stronger association of AgNPs/Rf and AgNPs/Rf/Starch nanocapsules with BSA under physiological conditions.

Innovated pirfenidone loaded lecithin nanocapsules for targeting liver fibrosis: Formulation, characterization and in vivo study.

Increasing interest in developing antifibrotic therapies became a paramount priority due to the globally raised incidence of deaths secondary to hepatic cirrhosis. This work deals with the development of innovative antifibrotic pirfenidone -loaded lecithin core nanocapsules. This with the intention to target the liver and to increase the drug bioavailability, reducing drug liver toxicity, and studying the associated hepatic microenvironment changes. PFD-loaded lecithin nanocapsules (PFD-LENCs) were prepared using the natural lipoid S45 for its dual benefits of being both a lipid and an amphiphilic surfactant. The selected formulation exhibited in vitro sustained drug release up to 24 h compared to free PFD, which is consistent with the studied pharmacokinetic profile. The studied cytotoxicity of PFD as well as PFD-LENCs exhibited negligible cytotoxicity in normal oral epithelial cells. For exploring the capability of the PFD-LENCs in reaching the liver; in vivo tracing using CLSM, in vivo biodistribution to the vital organs were conducted and electron microscopic examination for depicting nanoparticles in liver tissue was performed. Results revealed the capability of the prepared fluorescent LENC2 in reaching the liver, PFD-LENCs detection in the Disse space of the liver and the significant accumulation of PFD-LENCs in liver tissue compared to the other tested organs. The assessment of the necro-inflammatory, antioxidant and the anti-fibrotic effect of PFD-LENCs (50 & 100 mg/kg) exhibited a significant decrease of liver enzymes, TNF-α, TGF-ß, Col-1, α-SMA, and TIMP-1, and a significant increase of catalase enzyme and MMP2 compared to free PFD. EM studies, revealed often detection of dendritic cells in PFD-LENCs (100 mg/kg) treated mice and abnormal collagen structure which can represent an adjunct contribution to the antifibrotic mechanism of PFD-LENCs. In conclusion, the development of this innovative PFD loaded lecithin nanocapsules achieved a targeting ability to the liver, controlled drug release, thereby increase the PFD therapeutic value in downregulating hepatic fibrosis in adjunct with the reduction of liver toxicity.

Layer-by-layer development of chitosan/alginate-based platelet-mimicking nanocapsules for augmenting doxorubicin cytotoxicity against breast cancer.

Breast carcinoma is considered one of the most invasive and life-threatening malignancies in females. Mastectomy, radiation therapy, hormone therapy and chemotherapy are the most common treatment choices for breast cancer. Doxorubicin (DOX) is one of the most regularly utilized medications in breast cancer protocols. However, DOX has showed numerous side effects including lethal cardiotoxicity. This study aims to fortify DOX cytotoxicity and lowering its side effects via its combining with the antidiabetic metformin (MET) as an adjuvant therapy, along with its effective delivery using natural platelet-rich plasma (PRP), and newly-developed PRP-mimicking nanocapsules (NCs). The PRP-mimicking NCs were fabricated via layer-by-layer (LBL) deposition of oppositely charged biodegradable and biocompatible chitosan (CS) and alginate (ALG) on a core of synthesized polystyrene nanoparticles (PS NPs) followed by removal of the PS core. Both natural PRP and PRP-mimicking NCs were loaded with DOX and MET adjuvant therapy, followed by their physicochemical characterizations including DLS, FTIR, DSC, and morphological evaluation using TEM. In-vitro drug release studies, cytotoxicity, apoptosis/necrosis, and cell cycle analysis were conducted using MCF-7 breast cancer cells. Also, an in-vivo assessment was carried out using EAC-bearing balb/c mice animal model to evaluate the effect of DOX/MET-loaded natural PRP and PRP-mimicked NCs on tumor weight, volume and growth biomarkers in addition to analyzing the immunohistopathology of the treated tissues. Results confirmed the development of CS/ALG-based PRP-mimicking NCs with a higher loading capacity of both drugs (DOX and MET) and smaller size (259.7 ± 19.3 nm) than natural PRP (489 ± 20.827 nm). Both in-vitro and in-vivo studies were in agreement and confirmed that MET synergized the anticancer activity of DOX against breast cancer. Besides, the developed LBL NCs successfully mimicked the PRP in improving the loaded drugs biological efficiency more than free drugs.

Cationic Chitosan/Pectin Polyelectrolyte Nanocapsules of Moxifloxacin as Novel Topical Management System for Bacterial Keratitis.

PURPOSE: Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). This investigation aimed to formulate MOX-loaded chitosan/pectin cationic polyelectrolyte nanocapsules (CPNCs) for the effective topical treatment of BK. METHODS: Physicochemical properties like nanocapsule size, charge, drug entrapment efficiency (EE), viscosity, pH, and in-vitro release profile of CPNCs were evaluated. The in-vitro antibacterial activity of CPNCs and marketed formulations (MFs) was studied against Staphylococcus aureus. Ex-vivo corneal permeation studies of CPNCs were evaluated with the help of a modified diffusion apparatus, which was used with goat cornea. The pharmacodynamic study was performed with optimized CPNCs on a BK-induced rabbit eye model and compared with MF. RESULTS: The optimized nanocapsules appeared as positive charge (+19.91 ± 0.66) with a nano size (242.0 ± 0.30 nm) as calculated by the dynamic light scattering method. The in-vitro release profile of CPNCs exhibited sustained release properties. The ex-vivo permeation pattern also supported the improved drug permeation through the cornea from CPNCs as compared with MF. Draize irritation studies confirmed that the prepared formulation is compatible with the corneal tissue. The in-vivo study concluded that the antibacterial activity of CPNCs was improved when evaluated with MF. CONCLUSION: The obtained results showed that CPNCs were the better choice for the management of BK therapy due to its capability to improve the corneal adhesion of CPNCs through direct interaction with the mucous membrane of the corneal tissue.

Nano-based formulations as an approach for providing a novel identity for organoselenium compounds.

The organoselenium compounds belong to a class of synthetic molecules that displays a remarkable spectrum of promising pharmacological properties. Despite the huge amount of preclinical data that supports a bright outlook for organoselenium compounds, some toxicity issues and physicochemical limitations delay the development of more advanced studies. Currently, several scientific reports demonstrated that the association of nanotechnology has emerged as an alternative to improve solubility and safety issues of these molecules as well as enhance pharmacological properties. Therefore, our main objective was to address studies that reported the development and biological evaluations of nano-based formulations to synthetic organoselenium compounds incorporation by constructing an integrative literature review. The data survey was performed using the Science Direct, PubMed, Web of Science, and SCOPUS online databases, covering studies that were published from January 2011 up to October 2021. In the last decade, there has been an exponential growth in research regarding the incorporation of synthetic organoselenium compounds into distinct nanocarrier systems such as nanocapsules, nanoemulsions, micelles, and others, reinforcing that the association of such molecules and nanotechnology is a promising alliance. The reports investigated many nanosystems containing selenium organic molecules intending oral, intravenous, and cutaneous applications. Besides that, these systems were evaluated in a variety of in vitro techniques and in vivo models, concerning their pharmacological potential, biodistribution profile, and safety. In summary, the findings indicate that the production of nano-based formulations containing organoselenium compounds either improved physicochemical and biological properties or minimize toxicological issues of compounds.

A review of nanostructured delivery systems for the encapsulation, protection, and delivery of silymarin: An emerging nutraceutical.

Silymarin exhibits biological activities that may promote human health and wellbeing, including antioxidant, antimicrobial, anti-inflammatory, and anti-cancer activities. Consequently, it has potential for application as a nutraceutical ingredient in functional foods and supplements. But its application for this purpose is currently limited by its poor water solubility, chemical stability, and bioavailability. The potential of nano-delivery systems to improve the functional performance of silymarin was reviewed in this manuscript. The formation, attributes, and applications of biopolymer-based, lipid-based, surfactant-based, and miscellaneous nanocarriers are discussed. In particular, the impact of the different delivery systems such as biopolymer-based, lipid-based delivery systems on the gastrointestinal fate of silymarin is summarized. The encapsulation in edible nanocarriers can improve the bioavailability of silymarin by enhancing its water-dispersibility, inhibiting its degradation, and increasing its absorption.These nanocarriers may therefore be utilized to incorporate this nutraceutical into functional foods and supplements in a bioavailable form.