RESUMEN
One of the most effective strategies to fight viruses and handle health diseases is vaccination. Recent studies and current applications are moving on antigen, DNA and RNA-based vaccines to overcome the limitations related to the conventional vaccination strategies, such as low safety, necessity of multiple injection, and side effects. However, due to the instability of pristine antigen, RNA and DNA molecules, the use of nanocarriers is required. Among the different nanocarriers proposed for vaccinal applications, three types of nanovesicles were selected and analysed in this review: liposomes, transfersomes and niosomes. PubMed, Scopus and Google Scholar databases were used for searching recent papers on the most frequently used conventional and innovative methods of production of these nanovesicles. Weaknesses and limitations of conventional methods (i.e., multiple post-processing, solvent residue, batch-mode processes) can be overcome using innovative methods, in particular, the ones assisted by supercritical carbon dioxide. SuperSomes process emerged as a promising production technique of solvent-free nanovesicles, since it can be easily scaled-up, works in continuous-mode, and does not require further post-processing steps to obtain the desired products. As a result of the literature analysis, supercritical carbon dioxide assisted methods attracted a lot of interest for nanovesicles production in the vaccinal field. However, despite their numerous advantages, supercritical processes require further studies for the production of liposomes, transfersomes and niosomes with the aim of reaching well-defined technologies suitable for industrial applications and mass production of vaccines.
Asunto(s)
Liposomas , Vacunas , Liposomas/química , Dióxido de Carbono/química , Solventes , ADN , ARNRESUMEN
OBJECTIVE: Zinc Oxide nanoparticles (ZnO NPs) are used widely in nowadays personal care products, especially sunscreens, as a protector against UV irradiation. Yet, they have some reports of potential toxicity. Silica is widely used to cage ZnO NPs to reduce their potential toxicity. Vitamin C derivative, Magnesium Ascorpyl Phosphate (MAP), is a potent antioxidant that can efficiently protect human skin from harmful impacts of UV irradiation and oxidative stress. The combination of silica coated ZnO NPs and MAP nanovesicles could have potential synergistic protective effect against skin photodamage. METHODS: Silica coated ZnO NPs and MAP nanovesicles (ethosomes and niosomes) were synthesized, formulated, and evaluated as topical gels. These gel formulations were evaluated in mice for their photoprotective effect against UV irradiation through histopathology and immuno-histochemistry study. Split-face clinical study was conducted to compare the effect of application of silica coated ZnO NPs either alone or combined with MAP nanovesicles. Their photoprotective action was evaluated, using Antera 3D® camera, for melanin level, roughness index and wrinkles depth. RESULTS: Silica coated ZnO NPs when combined with MAP nanovesicles protected mice skin from UV irradiation and decreased the expression of the proinflammatory cytokines, NF-κB. Clinically, silica coated ZnO NPs, alone or combined with MAP nanovesicles, could have significant effect to decrease melanin level, roughness index and wrinkles depth with higher effect for the combination. CONCLUSION: A composite of silica coated ZnO NPs and MAP nanovesicles could be a promising cosmetic formulation for skin protection against photodamage signs such as hyperpigmentation, roughness, and wrinkles.
Asunto(s)
Ácido Ascórbico , Dióxido de Silicio , Piel , Protectores Solares , Rayos Ultravioleta , Óxido de Zinc , Óxido de Zinc/química , Óxido de Zinc/farmacología , Óxido de Zinc/administración & dosificación , Animales , Dióxido de Silicio/química , Rayos Ultravioleta/efectos adversos , Ratones , Humanos , Ácido Ascórbico/química , Ácido Ascórbico/farmacología , Ácido Ascórbico/administración & dosificación , Ácido Ascórbico/análogos & derivados , Protectores Solares/química , Protectores Solares/farmacología , Protectores Solares/administración & dosificación , Piel/efectos de los fármacos , Piel/efectos de la radiación , Piel/metabolismo , Femenino , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/administración & dosificación , Nanopartículas/química , Envejecimiento de la Piel/efectos de los fármacos , Envejecimiento de la Piel/efectos de la radiación , Masculino , Adulto , Persona de Mediana EdadRESUMEN
Exploitation of machine learning in predicting performance of nanomaterials is a rapidly growing dynamic area of research. For instance, incorporation of therapeutic cargoes into nanovesicles (i.e., entrapment efficiency) is one of the critical parameters that ensures proper entrapment of drugs in the developed nanosystems. Several factors affect the entrapment efficiency of drugs and thus multiple assessments are required to ensure drug retention, and to reduce cost and time. Supervised machine learning can allow for the construction of algorithms that can mine data available from earlier studies to predict performance of specific types of nanoparticles. Comparative studies that utilize multiple regression algorithms to predict entrapment efficiency in nanomaterials are scarce. Herein, we report on a detailed methodology for prediction of entrapment efficiency in nanomaterials (e.g., niosomes) using different regression algorithms (i.e., CatBoost, linear regression, support vector regression and artificial neural network) to select the model that demonstrates the best performance for estimation of entrapment efficiency. The study concluded that CatBoost algorithm demonstrated the best performance with maximum R2 score (0.98) and mean square error (< 10-4). Among the various parameters that possess a role in entrapment efficiency of drugs into niosomes, the results obtained from CatBoost model revealed that the drug:lipid ratio is the major contributing factor affecting entrapment efficiency, followed by the lipid:surfactant molar ratio. Hence, supervised machine learning may be applied for future selection of the components of niosomes that achieve high entrapment efficiency of drugs while minimizing experimental procedures and cost.
Asunto(s)
Liposomas , Nanoestructuras , Aprendizaje Automático , Algoritmos , LípidosRESUMEN
Several edible plants contain flavonoids, including myricetin (Myr), which perform a wide range of biological activities. Myr has antitumor properties against various tumor cells. In this study Myr-loaded PEGylated niosomes (Myr-PN) were prepared and their anti-cancer activities were evaluated inâ vitro. Myr-PNs were prepared as a tool for drug delivery to the tumor site. Myr-PN was characterized in terms of size, zeta potential, and functional groups using dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), and field emission scanning electron microscopy (SEM). The Myr-PN size was 241â nm with a polydispersity index (PDI) of 0.20, and zeta potential -32.7±6.6â mV. Apoptotic properties of Myr-PN against normal and cancer cell lines were determined by flow cytometry and real-time quantitative PCR. Cancer cells showed higher cytotoxicity when treated with Myr-PN compared with normal cells, indicating that the synthesized nanoparticles pose no adverse effects. Apoptosis was induced in cells treated with 250â µg/mL of Myr-PN, in which 45.2 % of cells were arrested in subG1, suggesting that Myr-PN can induce apoptosis. In vitro, the synthesized Myr-PN demonstrated potent anticancer properties. Furthermore, more research should be conducted inâ vitro and inâ vivo to study the more details of Myr-PN anti-cancer effects.
Asunto(s)
Liposomas , Neoplasias , Humanos , Sistemas de Liberación de Medicamentos , Neoplasias/tratamiento farmacológico , Flavonoides/química , PolietilenglicolesRESUMEN
Doxorubicin (DOX) is widely used against solid tumors. Niosomes are self-assembled nanocarriers of non-ionic surfactants. DOX loaded into cationic niosomes (DOX-Nio) was prepared via thin film hydration method. DOX-Nio was then decorated with a hyaluronic acid (DOX-HA-Nio) via electrostatic interaction. DOX-Nio and DOX-HA-Nio displayed a particle size of 120.0±1.02 and 182.9±2.3â nm, and charge of + 35.5±0.15 and -15.6±0.25â mV, respectively, with PDI < 0.3. DOX-HA-Nio showed a good stability regarding size and charge over 4â weeks at 4 °C and maintain their integrity after lyophilization. HPLC results showed a 94.1±4.2 % encapsulation efficiency of DOX with good entrapment and slow, prolonged DOX release even after 48â hrs. Cell viability assay showed an IC50 of 14.26â nM for the DOX-HA-Nio against MCF-7â cell line with micromolar IC50 results against CD-44 negative cell lines (NIH/3T3). DOX-HA-Nio was proven to be an effective, targeted nanocarrier for DOX against MCF-7â cell line.
Asunto(s)
Neoplasias de la Mama , Humanos , Femenino , Neoplasias de la Mama/tratamiento farmacológico , Liposomas , Ácido Hialurónico , Doxorrubicina/farmacología , Células MCF-7RESUMEN
OBJECTIVE: The present study aimed to assess the radioprotective effect of nanoniosomes loaded by Mentha Pulegium essential oil (MPEO-N nanoparticles) as a natural antioxidant on human peripheral blood mononuclear cells (PBMCs). SIGNIFICANCE: Despite the applications and advantages of ionizing radiation, there are many radiation risks to biological systems that are necessary to be reduced as much as possible. METHODS: MPEO-N nanoparticles were prepared by the lipid thin film hydration method, and its physicochemical characteristics were analyzed. PBMCs were then irradiated with X-ray using a 6 MV linear accelerator at two radiation doses in the presence of nontoxic concentrations of MPEO-N nanoparticles (IC10). After 48 and 72 h of incubation, the radioprotective effect was investigated by measuring survival, apoptosis, and necrosis of PBMCs, using MTT assay and flow cytometry analysis. KEY FINDINGS: The hydrodynamic diameter and zeta potential of nanoniosomes were 106.0 ± 4.69 nm and -15.2 ± 0.9 mV, respectively. The mean survival percentage of PBMCs showed a significant increase only at a radiation dose of 200 cGy compared with the control group. The percentages of apoptosis and necrosis of cells in the presence of MPEO-N nanoparticles at both radiation doses and incubation periods (48 and 72 h) demonstrated a significant reduction compared with the control. CONCLUSION: MPEO-N nanoparticles as a natural antioxidant, exhibited a favorable radioprotective effect by a significant reduction in the percentage of apoptosis and necrosis of irradiated PBMCs.
Asunto(s)
Mentha pulegium , Aceites Volátiles , Humanos , Aceites Volátiles/farmacología , Antioxidantes/farmacología , Leucocitos Mononucleares , Radiación Ionizante , NecrosisRESUMEN
AIMS: There are around 24 distinct lipid vesicles described in the literature that are similar to vesicular systems such as liposomes. Liposome-like structures are formed by combining certain amphiphilic lipids with a suitable stabiliser. Since their discovery and classification, self-assembled liposome-like structures as active drug delivery vehicles captured researchers' curiosity. METHODOLOGY: This comprehensive study included an in-depth literature search using electronic databases such as PubMed, ScienceDirect and Google Scholar, focusing on studies on liposome and liposomes like structure, discussed in literature till 2024, their sizes, benefits, drawback, method of preparation, characterisation and pharmaceutical applications. RESULTS: Pharmacosomes, cubosomes, ethosomes, transethosomes, and genosomes, all liposome-like structures, have the most potential due to their smaller size with high loading capacity, ease of absorption, and ability to treat inflammatory illnesses. Genosomes are futuristic because of its affinity for DNA/gene transport, which is an area of focus in today's treatments. CONCLUSION: This review will critically analyse the composition, preparation procedures, drug encapsulating technologies, drug loading, release mechanism, and related applications of all liposome-like structures, highlighting their potential benefits with enhanced efficacy over each other and over traditional carriers by paving the way for exploring novel drug delivery systems in the Pharma industry.
Asunto(s)
Portadores de Fármacos , Liposomas , Liposomas/química , Portadores de Fármacos/química , Humanos , Sistemas de Liberación de Medicamentos , AnimalesRESUMEN
BACKGROUND: Periodontal diseases may benefit more from topical treatments with nanoparticles rather than systemic treatments due to advantages such as higher stability and controlled release profile. This study investigated the preparation and characterization of thermosensitive gel formulations containing clindamycin-loaded niosomes and solid lipid nanoparticles (SLNs) loaded with fluconazole (FLZ), as well as their in vitro antibacterial and antifungal effects in the treatment of common microorganisms that cause periodontal diseases. METHODS: This study loaded niosomes and SLNs with clindamycin and FLZ, respectively, and assessed their loading efficiency, particle size, and zeta potential. The particles were characterized using a variety of methods such as differential scanning calorimetry (DSC), dynamic light scattering (DLS), and Transmission Electron Microscopy (TEM). Thermosensitive gels were formulated by combining these particles and their viscosity, gelation temperature, in-vitro release profile, as well as antibacterial and antifungal effects were evaluated. RESULTS: Both types of these nanoparticles were found to be spherical (TEM) with a mean particle size of 243.03 nm in niosomes and 171.97 nm in SLNs (DLS), and respective zeta potentials of -23.3 and -15. The loading rate was 98% in niosomes and 51% in SLNs. The release profiles of niosomal formulations were slower than those of the SLNs. Both formulations allowed the release of the drug by first-order kinetic. Additionally, the gel formulation presented a slower release of both drugs compared to niosomes and SLNs suspensions. CONCLUSION: Thermosensitive gels containing clindamycin-loaded niosomes and/or FLZ-SLNs were found to effectively fight the periodontitis-causing bacteria and fungi.
Asunto(s)
Clindamicina , Fluconazol , Geles , Liposomas , Nanopartículas , Tamaño de la Partícula , Enfermedades Periodontales , Clindamicina/administración & dosificación , Clindamicina/uso terapéutico , Nanopartículas/química , Fluconazol/administración & dosificación , Fluconazol/farmacología , Enfermedades Periodontales/tratamiento farmacológico , Antifúngicos/administración & dosificación , Antifúngicos/farmacología , Antibacterianos/administración & dosificación , Antibacterianos/farmacología , Microscopía Electrónica de Transmisión , Temperatura , Rastreo Diferencial de Calorimetría , Candida albicans/efectos de los fármacos , Viscosidad , Lípidos/química , HumanosRESUMEN
Paraquat (PQ) herbicide poisoning is a severe medical problem in developing countries without suitable therapy. This study aimed to investigate the effects of crocin (CCN) and nano crocin (NCCN) on PQ -induced toxicity in the MRC-5 cell line. The results showed that the particle size of NCCN was 140.3 ± 18.0 nm, and the zeta potential of the optimal crocin-loaded niosomes was 23.4 ± 2.8 mV. The NCCN was more effective than CCN in the inhibition of PQ-induced toxicity. Treatment of the MRC-5 cells leads to a decrease in ROS and an increase in SOD, CAT, GPX, and TAC levels in PQ-CCN and PQ-NCCN groups compared with the PQ group. These changes tended to be positively associated with the NCCN compared to CCN. Overall, NCCN was more effective than crocin in treating PQ-induced toxicity in vitro and deserved further preclinical consideration.
RESUMEN
OBJECTIVE: This investigation aimed to explore the potential of non-ionic surfactant based niosomal vesicles encapsulating tenoxicam (TN; anti-rheumatic drug) for the treatment of rheumatic diseases. MATERIAL AND METHODS: Mechanical dispersion technique with controlled pressure was employed to prepare different niosomal formulations. The effects of different ratios of surfactant (span-60), lipid, and sodium deoxycholate on noisome's physicochemical properties have been examined. Moreover, inhibition of TNF-α in lipopolysaccharide-activated cultured Human leukemia monocytic (THP-1) cells were demonstrated to assess the in vitro inflammation profile. Finally, the optimized niosomal formulation (TN3) was prepared in gel matrix consist of carbopol 934 (termed as TN34) and stability was also tested at 4±2 ÌC, 25±2 ÌC, 37±2 ÌC and 45±2 ÌC for 6 months. RESULTS: The optimized niosomal formulation exhibited a small vesicle size (165±14nm) and high drug encapsulation (79.64±1.5%). Niosomal gel formulation TN34 showed pH (6.7), viscosity (6810±3.34 cps), spreadability (19.11±1.87gm.cm/sec) and also displayed sustained release pattern of drug release (98.16±0.07% TN released from gel matrix in 24h) in vitro release study. TN34 exhibited substantial anti-inflammatory response, with â¼75% inhibition of TNF-α in 48h. Stability investigation revealed that refrigerator temperature is most suitable for the storage of niosomal gel. CONCLUSION: Transdermal niosomal formulation displayed promising potential in the treatment of rheumatic diseases.
RESUMEN
AIM: The aim of this study was to investigate the potential cardioprotective and anti-cancer effects of carvedilol (CAR) either free or as loaded nano-formulated with or without doxorubicin (DOX) in solid Ehrlich carcinoma (SEC)-bearing mice. It focused on assessment of cardiac damage, drug resistance, apoptosis, oxidative stress status, angiogenesis and proliferation. METHODS: CAR was loaded into poly-D,L lactic-co-glycolic acid)PLGA(or Niosomes. SEC was induced in female albino mice as an experimental model of breast cancer. Seventy-two mice were randomly divided into 9 equal groups (Normal control, Untreated-SEC, SEC + DOX, SEC + CAR-free, SEC + CAR-PLGA, SEC + CAR-Niosomes, SEC + DOX + CAR-free, SEC + DOX + CAR-PLGA and SEC + DOX + CAR-Niosomes). Tumor volume and survival rate were recorded. On day 28 from tumor inoculation, mice were sacrificed, and blood samples were collected for determination of serum lactate dehydrogenase (LDH) and creatine kinase-MB (CK-MB). One part from tumor tissues was prepared for assessment of multidrug resistance protein-1 (MDR-1), caspase-3, reduced glutathione (GSH) and malondialdehyde (MDA), while the other part was processed for histopathological examination and immunohistochemical expression of vascular endothelial growth factor (VEGF) and Ki-67. RESULTS: There was non-significant difference between CAR-free, CAR-PLGA and CAR-Niosomes as anticancer either alone or when combined with DOX. However, CAR-free demonstrated potential cardioprotective effects against cardiac damage mediated by cancer or DOX that have been enhanced using CAR-PLGA or CAR-Niosomes, but that of Niosomes outperformed them both. CONCLUSION: CAR could be used as an adjuvant therapy with DOX, especially when nanoformualted with PLGA and even better with Niosomes, without compromising its cytotoxicity against cancer cells and preventing its cardiotoxic impacts.
Asunto(s)
Carcinoma , Nanopartículas , Ratones , Femenino , Animales , Carvedilol/farmacología , Liposomas , Factor A de Crecimiento Endotelial Vascular , Doxorrubicina/farmacología , Carcinoma/tratamiento farmacológico , Ácido LácticoRESUMEN
Development of nanocarriers has opened new avenues for the delivery of therapeutics of various pharmacological activities with improved targeting properties and reduced side effects. Niosomes, non-ionic-based vesicles, have drawn much interest in various biomedical applications, owing to their unique characteristics and their ability to encapsulate both hydrophilic and lipophilic cargoes. Niosomes share structural similarity with liposomes while overcoming limitations associated with stability, sterilization, and large-scale production of liposomes. Different methods for preparation of niosomes have been described in the literature, each having its own merits and a great impact on the sizes and characteristics of the formed niosomes. In this article, procedures involved in the thin-film hydration method, a commonly used method for the preparation of niosomes, are described in detail, while highlighting precautions that should be considered for consistent and reproducible construction of niosomes.
Asunto(s)
Sistemas de Liberación de Medicamentos , Liposomas , Sistemas de Liberación de Medicamentos/métodos , Liposomas/química , Tamaño de la Partícula , Tensoactivos/químicaRESUMEN
Gradually, loss of skin elasticity and elastic properties occurs after 30 years of age and will be associated with several changes, including creating wrinkles, skin laxity (sagging skin), and skin blemishes. In general, people all over the world are looking for ways to keep their facial skin young over time. There are several strategies to skin rejuvenate, including invasive and non-invasive methods. However, invasive methods have less popularity than non-invasive methods due to their need for specialist physicians (medical expertise), localized neuropathic pains for patients, the prevalence and incidence of skin infections, and high-cost clinical services. In the meantime, skin hydration is one of the simplest non-invasive methods for skin rejuvenation, and HA, with anti-aging and skin collagen-stimulating properties, has been introduced as a natural skin moisturizing agent. Therefore, since this composition maintains facial skin moisture and radiance, and improves its elasticity, it has always been considered by experts and specialist physicians. On the other hand, due to its lipophilic properties, hydrophilic macromolecules containing HA cannot pass through the stratum corneum. However, they have temporary and superficial softening effects on the skin. Hence, some nanocarriers have been suggested to overcome this problem and develop the properties and positive influences of HA on skin rejuvenation. Therefore, the present study aimed to introduce some new non-invasive approaches in facial skin rejuvenation, including applying liposomes, niosomes, ethosomes, and ionic liquids, to transport HA into the inner and deeper layers of the skin, including Dermis. In this review article, we examine non-invasive methods using nanoparticles to deliver HA to the epidermis and dermis of the skin for skin rejuvenation.
Asunto(s)
Ácido Hialurónico , Envejecimiento de la Piel , Humanos , Rejuvenecimiento , Piel , CaraRESUMEN
Combination therapy has been considered one of the most promising approaches for improving the therapeutic effects of anticancer drugs. This is the first study that uses two different antioxidants in full-characterized niosomal formulation and thoroughly evaluates their synergistic effects on breast cancer cells. In this study, in-silico studies of hydrophilic and hydrophobic drugs (ascorbic acid: Asc and curcumin: Cur) interactions and release were investigated and validated by a set of in vitro experiments to reveal the significant improvement in breast cancer therapy using a co-delivery approach by niosomal nanocarrier. The niosomal nanoparticles containing surfactants (Span 60 and Tween 60) and cholesterol at 2:1 M ratio were prepared through the film hydration method. A systematic evaluation of nanoniosomes was carried out. The release profile demonstrated two phases (initial burst followed by sustained release) and a pH-dependent release schedule over 72 h. The optimized niosomal preparation displayed superior storage stability for up to 2 months at 4 °C, exhibiting extremely minor changes in pharmaceutical encapsulation efficiency and size. Free dual drugs (Asc + Cur) and dual-drug loaded niosomes (Niosomal (Asc + Cur)) enhanced the apoptotic activity and cytotoxicity and inhibited cell migration which confirmed the synergistic effect of co-encapsulated drugs. Also, significant up-regulation of p53 and Bax genes was observed in cells treated with Asc + Cur and Niosomal (Asc + Cur), while the anti-apoptotic Bcl-2 gene was down-regulated. These results were in correlation with the increase in the enzyme activity of SOD, CAT, and caspase, and the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) upon treatment with the mentioned drugs. Furthermore, these anti-cancer effects were higher when using Niosomal (Asc + Cur) than Asc + Cur. Histopathological examination also revealed that Niosomal (Asc + Cur) had a lower mitosis index, invasion, and pleomorphism than Asc + Cur. These findings indicated that niosomal formulation for co-delivery of Asc and Cur would offer a promising delivery system for an effective breast cancer treatment.
Asunto(s)
Antineoplásicos , Neoplasias de la Mama , Curcumina , Humanos , Femenino , Neoplasias de la Mama/tratamiento farmacológico , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Liposomas/química , Liposomas/farmacología , Liposomas/uso terapéutico , Curcumina/farmacología , Curcumina/química , Polisorbatos/química , Polisorbatos/uso terapéuticoRESUMEN
Curcumin is a natural component extracted from the rhizomes of turmeric (Curcuma longa), a natural plat with known medicinal uses for more than 4000 years. Most turmeric therapeutic effects are attributed to curcumin, a yellow-coloured extract. Curcumin has received considerable attention due to its biological activities, such as its use in arthritis, liver and neurodegenerative diseases, obesity, and several types of cancers. Most of these curcumin therapeutic activities are related to its antioxidant and anti-inflammatory effects. However, the clinical application of curcumin is hampered by some limitations that prevent its extensive clinical application. Curcumin high hydrophobicity of curcumin and limited water solubility are among the most important limitations. This poor solubility will result in low bioavailability due to its poor absorption into plasma and the target tissues. Curcumin also has rapid metabolism, which will significantly lower its bioavailability and shorten its half-life. Moreover, curcumin is photosensitive with limited chemical stability during manufacturing and storage. These limitations have been overcome by applying nanotechnology using several types of nanoparticles (NPs). This includes using NPs such as liposomes, niosomes, gold nanoparticles, and many others to improve the curcumin solubility and bioavailability. This review focuses on the different types of NPs investigated and the outcomes generated by their use in the most recent studies in this field. To follow the latest advances in the field of site-specific drug delivery using nanomaterials, an electronic databases search was conducted using PubMed, Google scholar and Scopus using the following keywords: lipid-based nanoparticles, curcumin delivery, niosomes, and liposomes.
Asunto(s)
Curcumina , Nanopartículas del Metal , Curcumina/uso terapéutico , Liposomas , Oro , Sistemas de Liberación de MedicamentosRESUMEN
Smart pH-responsive niosomes loaded with either Oxaliplatin (Ox), Ylang ylang essential oil (Y-oil), or co-loaded with both compounds (Ox-Y) (Ox@NSs, Y@NSs, and Ox-Y@NSs, respectively) were formulated utilizing the thin film method. The developed nanocontainers had a spherical morphology with mean particle sizes lower than 170 nm and showed negative surface charges, high entrapment efficiencies, and a pH-dependent release over 24 h. The prepared pH-responsive niosomes' cytotoxicity was tested against the invasive triple-negative breast cancer (MDA-MB-231) cells, compared to free OX and Y-oil. All niosomal formulations loaded with Ox and/or Y-oil significantly improved cytotoxic activity relative to their free counterparts. The Ox-Y@NSs demonstrated the lowest IC50 (0.0002 µg/mL) when compared to Ox@NSs (0.006 µg/mL) and Y@NSs (18.39 µg/mL) or unloaded Ox (0.05 µg/mL) and Y-oil (29.01 µg/mL). In addition, the percentages of the MDA-MB-231 cell population in the late apoptotic and necrotic quartiles were profoundly higher in cells treated with the smart Ox-Y@NSs (8.38% and 5.06%) than those exposed to free Ox (7.33% and 1.93%) or Y-oil (2.3% and 2.13%) treatments. Gene expression analysis and protein assays were performed to provide extra elucidation regarding the molecular mechanism by which the prepared pH-sensitive niosomes induce apoptosis. Ox-Y@NSs significantly induced the gene expression of the apoptotic markers Tp53, Bax, and Caspase-7, while downregulating the antiapoptotic Bcl2. As such, Ox-Y@NSs are shown to activate the intrinsic pathway of apoptosis. Moreover, the protein assay ascertained the apoptotic effects of Ox-Y@NSs, generating a 4-fold increase in the relative protein quantity of the late apoptotic marker Caspase-7. Our findings suggest that combining natural essential oil with synthetic platinum-based drugs in pH-responsive nanovesicles is a promising approach to breast cancer therapy.
Asunto(s)
Antineoplásicos , Cananga , Aceites Volátiles , Neoplasias de la Mama Triple Negativas , Humanos , Oxaliplatino/farmacología , Caspasa 7 , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Liposomas , Aceites Volátiles/farmacología , Aceites de Plantas , Antineoplásicos/farmacología , Concentración de Iones de HidrógenoRESUMEN
BACKGROUND: Inflammatory autoimmune arthritis like that present in rheumatoid arthritis (RA) is treated by medications with many side effects. This study was a trial to benefit from Toxoplasma immune-modulatory effects on its host to treat arthritis in rat model resembling joints affection of RA. To avoid hazards of infection, Toxoplasma lysate antigen (TLA) was given instead of the whole infection, in addition to giving its encapsulated niosomes form, assuming that it would enhance the effect of TLA alone, to compare effects of both on disease activity with that of prednisolone. METHODS: Swiss albino rats were divided into 6 groups: normal control group and the remaining 5 groups were injected by CFA adjuvant to induce arthritis; one of those groups was the untreated model. Each of the other groups received one of the following (TLA, TLA-encapsulated niosomes, prednisolone or niosomes) for comparison of their results. Inflammatory markers measured at the end of the experiment were: interleukin 17 (IL-17), IL-10 and CRP by ELISA technique; histopathological assessment of the biopsied hind paw joints was done and also, Janus kinase 3 (JAK3) expression was assessed by immunohistochemistry. RESULTS: TLA and TLA-encapsulated niosomes both mitigated the signs of clinical and histopathological arthritis and were having anti-inflammatory effects (decreased CRP, IL-17 and JAK3 expressions, while increased IL-10 levels) with better effects in TLA-encapsulated niosomes-treated RA group, both groups' results were comparable to prednisolone. Niosomes also gave some anti-inflammatory effects but were mild in comparison to TLA and TLA-encapsulated niosomes. CONCLUSION: Vaccination with both TLA and TLA-encapsulated niosomes for the first time in adjuvant-induced arthritis ameliorated the disease through diversion of immune system and JAK3 downregulation. Both vaccinations should be further tested to evaluate the possibility of their introduction for disease treatment and in other autoimmune diseases.
Asunto(s)
Artritis Experimental , Artritis , Toxoplasma , Ratas , Animales , Interleucina-10 , Interleucina-17 , Liposomas , Janus Quinasa 3 , Regulación hacia Abajo , Antígenos de Protozoos , Vacunación , Prednisolona , Antiinflamatorios , Artritis Experimental/tratamiento farmacológicoRESUMEN
Secretory phospholipase B1 (PLB1) and biofilms act as microbial virulence factors and play an important role in pulmonary cryptococcosis. This study aims to formulate the ethanolic extract of propolis-loaded niosomes (Nio-EEP) and evaluate the biological activities occurring during PLB1 production and biofilm formation of Cryptococcus neoformans. Some physicochemical characterizations of niosomes include a mean diameter of 270 nm in a spherical shape, a zeta-potential of -10.54 ± 1.37 mV, and 88.13 ± 0.01% entrapment efficiency. Nio-EEP can release EEP in a sustained manner and retains consistent physicochemical properties for a month. Nio-EEP has the capability to permeate the cellular membranes of C. neoformans, causing a significant decrease in the mRNA expression level of PLB1. Interestingly, biofilm formation, biofilm thickness, and the expression level of biofilm-related genes (UGD1 and UXS1) were also significantly reduced. Pre-treating with Nio-EEP prior to yeast infection reduced the intracellular replication of C. neoformans in alveolar macrophages by 47%. In conclusion, Nio-EEP mediates as an anti-virulence agent to inhibit PLB1 and biofilm production for preventing fungal colonization on lung epithelial cells and also decreases the intracellular replication of phagocytosed cryptococci. This nano-based EEP delivery might be a potential therapeutic strategy in the prophylaxis and treatment of pulmonary cryptococcosis in the future.
Asunto(s)
Antifúngicos , Biopelículas , Cryptococcus neoformans , Proteínas Fúngicas , Lisofosfolipasa , Macrófagos Alveolares , Própolis , Humanos , Biopelículas/efectos de los fármacos , Línea Celular Tumoral , Criptococosis/prevención & control , Criptococosis/terapia , Cryptococcus neoformans/efectos de los fármacos , Cryptococcus neoformans/enzimología , Cryptococcus neoformans/patogenicidad , Etanol/química , Proteínas Fúngicas/antagonistas & inhibidores , Liposomas , Enfermedades Pulmonares Fúngicas/prevención & control , Enfermedades Pulmonares Fúngicas/terapia , Lisofosfolipasa/antagonistas & inhibidores , Macrófagos Alveolares/microbiología , Própolis/química , Própolis/farmacología , Virulencia/efectos de los fármacos , Factores de Virulencia/antagonistas & inhibidores , Antifúngicos/química , Antifúngicos/farmacologíaRESUMEN
Fungal skin diseases are recognized as a global burden disease that affect human quality adjusted life. Terbinafine belongs to allylamine and broad-spectrum antifungal drugs but considered practically insoluble. Different lipids/surfactant with two different molar ratios were investigated with Span 40-based niosomes; characterized for size, morphology, loading capacity (EE%), in vitro release, kinetics, and antifungal activities. Vesicle sizes (0.19-1.23 µm), EE% (25-99%), zeta potential (> -32 mV), and in vitro release rates were dependent on both lipid types and ratios. Higher ratios of Poloxamer 407 preferably formed mixed micelles rather than forming noisome bilayers. Both Compritol and Precirol were deemed to be potential alternatives to cholesterol as bilayer membrane stabilizers. Terbinafine-loaded Compritol and Precirol stabilized niosomes were successfully prepared and demonstrated superior antifungal activities in vitro (inhibition zones) using Candida albicans ATCC 60913.
Asunto(s)
Antifúngicos , Liposomas , Humanos , Antifúngicos/farmacología , Terbinafina/farmacología , Poloxámero , Tensoactivos , Tamaño de la PartículaRESUMEN
Dermal drug delivery has emerged as a promising alternative to traditional methods of drug administration due to its non-invasive nature and ease of use. However, the stratum corneum, the outermost layer of the skin, presents a significant barrier to drug penetration. Niosomes, self-assembled vesicular structures composed of nonionic surfactants and cholesterol, have been extensively investigated as a means of overcoming this barrier and improving the efficacy of dermal drug delivery. This review summarizes the current state of research on the use of niosomes in dermal drug delivery in cosmetics, with a particular focus on their formulation, characterization, and application in the delivery of various drug classes. The review highlights the advantages of niosomes over conventional drug delivery methods, including improved solubility and stability of drugs, controlled release, and enhanced skin permeation. The review also discusses the challenges associated with niosome-based drug delivery, such as their complex formulation and optimization, and the need for further studies on their long-term safety and toxicity.