Search Results (400)

Background: Various routes of drug administration are available for psoriasis treatment. However, there is an urgent need for novel and improved therapeutic options. Hence, our study aimed to develop a nanostructured lipid carrier (NLC) gel of hesperidin (HPD) using a systemic QbD approach for an effective treatment of psoriasis. Methods: Initially, HPD-NLC was optimized with independent variables (drug content, amount of liquid lipid, total lipid, and surfactant concentration) using Box–Behnken Design to assess dependent variables (particle size, size distribution, and entrapment efficiency). HPD-NLC was developed using the high-shear homogenization technique. The characteristics of nanoformulation such as particle size, morphology [transmission electron microscopy (TEM) and differential scanning calorimetry (DSC)], crystallinity [powder X-ray diffraction (XRD)], and chemical interactions [Fourier transform infrared spectroscopy (FTIR)], the drug entrapment efficiency (%EE), and the drug release were investigated. Franz-diffusion cell was utilized to perform in vitro diffusion study, and an imiquimod-induced psoriasis model was used for in vivo study. Results: The optimized HPD-NLC exhibited a spherical shape with particle size of 125.7 nm, polydispersity index (PDI) of 0.36, and entrapment efficiency of 52.26% w/w. Further, different techniques validated the reduced crystallinity of the hesperidin. The in vitro diffusion study highlighted the sustained and anomalous diffusion of the drug from NLC gel. In the in vivo study, the HPD-NLC-Gel-treated group displayed normal skin with minimal keratosis, while the drug-loaded gel group exhibited signs of hyperkeratosis and parakeratosis signs. Conclusions: HPD-NLC gel showed promising advancement in nanotechnology-based psoriasis treatment and the results of this study open the door for the application of topical HPD-NLC-Gel clinically. Full article

Objective: This study aims to develop an intranasal (IN) delivery system for glioblastoma multiforme (GBM) management using repurposed superparamagnetic iron-oxide (SPION) loaded with atorvastatin (ATO)-nanostructured lipid carrier (NLC). Methods: Emulsification and ultrasonication were used to formulate ATO-NLCs, and the best formula was loaded with SPION to make the final atorvastatin/superparamagnetic iron oxide-loaded nanostructured lipid carrier (ASN) formulation. Entrapment efficiency (EE%), particle size (PS), zeta potential (ZP), and drug release after 6 h (Q6h) were evaluated for NLCs. ASN was tested for cytotoxicity on T98G cancer cells, and the cell cycle was examined to determine cell death. Furthermore, the ability of the optimal formulation to suppress the levels of inflammatory biomarkers was investigated in Lipopolysaccharide (LPS)-induced inflammation. The brain-targeting behavior of IN-ASN was visualized in rabbits via confocal laser scanning microscopy (CLSM). Results: The optimum NLC exhibited a spherical shape, EE% of 84.0 ± 0.67%, PS of 282.50 ± 0.51 nm, ZP of −18.40 ± 0.15 mV, and Q6h of 89.23%. The cytotoxicity of ASN against cancer cells was 4.4-fold higher than ATO suspension, with a 1.3-fold increment in cell apoptosis. ASN showed significantly reduced pro-inflammatory biomarkers (IL-β, IL-6, TNF-α, TLR4, NF-қB), whereas CLSM revealed enhanced brain delivery with no observed histopathological nasal irritation. The in silico analysis demonstrated enhanced ATO-ADME (absorption, distribution, metabolism, and excretion) properties, while the network pharmacology study identified 10 target GBM genes, among which MAPK3 was the most prominent with a good binding score as elucidated by the simulated docking study. Conclusions: These findings may present ATO/SPION-NLCs as significant evidence for repurposing atorvastatin in the treatment of glioblastoma multiforme. Full article

Background/Objectives: Atorvastatin (ATR), an antihyperlipidemic drug with a potential antibacterial effect, was investigated in this study. Like other statins, ATR has been repurposed for several uses, ranging from anti-inflammatory to antimicrobial applications, and has demonstrated successful results. However, the efficacy of ATR is limited by its low solubility, indicating an opportunity for its encapsulation in a nanotechnology-based drug delivery system. Methods: Nanostructured lipid carrier (NLC) formulations were prepared using high-pressure homogenization and ultrasonication. The formulations were characterized, including their particle size, polydispersity index, zeta potential, encapsulation efficiency, and in vitro release. Antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli (E. coli), and Staphylococcus aureus (S. aureus) was evaluated using the growth curve (bacterial growth over time) and well diffusion methods (zone of inhibition and minimum inhibitory concentration (MIC) determination). The crystal violet assay was employed to assess biofilm inhibition. Results: The NLC formulations were optimized, and the size and zeta potential of the blank nanoparticles were 130 ± 8.39 nm and −35 ± 0.5 mV, respectively. In comparison, the encapsulated NLCs had a size of 142 ± 52.20 nm and a zeta potential of −31 ± 1.41 mV. The average encapsulation efficiency was 94%, and 70% of the drug was released after 24 h. The ATR-loaded NLCs showed significantly enhanced antibacterial activity by reducing the minimum inhibitory concentration by 2.5-fold for E. coli, 1.8-fold for S. aureus, and 1.4-fold for MRSA, and promoting more effective bacterial growth inhibition. Notably, biofilm inhibition was significantly improved with ATR-NLCs, achieving 80% inhibition for S. aureus, 40% for E. coli, and 30% for MRSA, compared to free ATR (p < 0.001). These findings suggest that NLC encapsulation enhances ATR’s antimicrobial efficacy and biofilm suppression. Conclusions: This study identified NLCs as successful carriers of ATR, significantly enhancing its antibacterial efficacy and biofilm inhibition capabilities. This formulation, which shows antimicrobial potential against both Gram-positive and Gram-negative bacteria, should be further studied and developed against different resistant microbial strains. Full article

Background/Objectives: Carvacrol, a monoterpenoid phenol found in essential oils, exhibits many biological activities, including anticancer properties through mechanisms such as induction of apoptosis. These properties can be enhanced if encapsulated within nanoparticles. This study focuses on producing functionalized carvacrol-loaded nanostructured lipid carriers (NLCs) applied to the treatment of breast cancer. Methods: NLCs were produced by hot emulsification with the sonication method and optimized by the Box–Behnken design, considering Precirol^® (1, 4, 7%), carvacrol (1, 5, 9%), and Tween^® (0.1, 0.5, 0.9%) as independent variables. Results: The optimized NLC containing 2% carvacrol had a particle size of 111 ± 2 nm, PdI of 0.26 ± 0.01, and zeta potential of −24 ± 0.8 mV. The solid lipid (Precirol^®) was the variable that most influenced particle size. NLCs were functionalized with Pluronic^® F68, cholesterol, chitosan, and polyethylene glycol (0.05–0.2%), with oNLC-Chol presenting the most promising results, with no significant increase in particle size (±12 nm) and high encapsulation efficiency (98%). Infrared spectra confirm effective carvacrol encapsulation, and stability tests showed no significant physicochemical changes for 120 days of storage at 4 °C. When incubated with albumin (5 mg/mL), NLCs showed overall good stability over 24 h, except for oNLC-Chol, which increased slightly in size after 24 h. In addition, oNLC increased the cytotoxic effect of carvacrol by 12-fold, resulting in an IC₅₀ of 7 ± 1 μg/mL. Conclusions: Therefore, it was possible to produce stable, homogeneous NLCs with nanometric sizes containing 2% carvacrol that displayed improved anticancer efficacy, indicating their potential as a delivery system. Full article

Lipid nanoparticles (LNs) have emerged as advanced lipid-based delivery systems, offering an effective approach for encapsulating and protecting lipid-soluble bioactive compounds, increasing their bioavailability. Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) are particularly promising for bioactive compound entrapment. However, to fully exploit their potential, it is crucial to carefully select the appropriate lipid matrices and emulsifiers. This review offers a comprehensive, up-to-date examination, considering studies published in the last 15 years, of the chemical, physical, and structural characteristics of lipids employed in LN production, focusing on the key components of the formulations: lipid matrices, emulsifiers, and bioactive compounds. In addition, it provides an in-depth analysis of production methods, drawing on insights from the latest scientific literature, and emphasizes the most important characterization techniques for LNs. Key parameters, including particle size (PS), zeta potential (ZP), crystallinity, thermal behavior, morphology, entrapment efficiency (EE), load capacity (LC), and physical stability, are discussed. Ultimately, this review aims to identify critical factors for the successful production of stable LNs that efficiently encapsulate and deliver bioactive compounds, highlighting their significant potential for applications in food systems. Full article

The cosmetic market is constantly evolving and ever-changing, particularly with the introduction and incorporation of nanotechnology-based processes into cosmetics for the production of unique formulations with both aesthetic and therapeutic benefits. There is no doubt that nanotechnology is an emerging technology for cosmetic formulations. Among the numerous cosmetic items, incorporating nanomaterials has provided a greater scope and is commonly utilized in facial masks, hair products, antiaging creams, sunscreen creams, and lipsticks. In cosmetics, nanosized materials, including lipid crystals, liposomes, lipid NPs, inorganic nanocarriers, polymer nanocarriers, solid lipid nanocarriers (SLNs), nanostructured lipid carriers (NLCs), nanofibers, nanocrystals, and nanoemulsions, have become common ingredients. The implementation of nanotechnology in the formulation of face masks will improve its efficacy. Nanotechnology enhances the penetration of active ingredients used in the preparation of face masks, such as peel-off masks and sheet masks, which results in better effects. The emphasis of this review is mainly on the formulation of cosmetic face masks, in which the impact of nanotechnology has been demonstrated to improve the product performance on the skin. Full article

Background/Objectives: Natural substances have been a widely studied source of both pharmaceutical excipients and drugs. Berberine (BRB) is a benzylisoquinoline alkaloid isolated from different plant sources. It possesses various pharmacological properties including antibacterial, antitumor, antidiabetic, neuroprotective, hepatoprotective, anti-inflammatory, antioxidant, etc. However, the limited aqueous solubility hinders its application. Nanosized drug delivery systems are an innovative approach for addressing various challenges regarding drug delivery via different routes of administration. Their utilization could improve the solubility of active constituents. Methods: A melt-emulsification and ultrasonication technique was applied for the preparation of nanostructured lipid carriers (NLCs). They were thoroughly physicochemically characterized by the means of Dynamic Light Scattering, TEM, FTIR, DSC, TGA, and In Vitro release. The In Vitro efficacy and safety were evaluated on cholangiocarcinoma, colorectal adenocarcinoma, hepatocellular carcinoma, lymphoma, fibroblast, and cardioblast cells, as well as rat liver microsomes by means of cytotoxicity assays and the comet assay. Results: The obtained nanoparticles had a spherical shape and size around 158.2 ± 1.8 nm with negative zeta potential. They revealed successful drug loading and improved dissolution of berberine in physiological conditions. The In Vitro safety studies showed that loading BRB in NLCs resulted in improved or retained cytotoxicity to tumor cell lines and reduced cytotoxicity to normal cell lines and liver microsomes. The NLC itself increased microsomal malondialdehyde (MDA) and comet formation. Conclusions: A successful preparation of NLCs with berberine is presented. The nanocarriers show favorable physicochemical and biopharmaceutical properties. The cellular experiments show that the NLC loading of berberine could improve its anticancer efficacy and safety. These findings highlight the potential applicability of berberine in gastrointestinal neoplasms and build the foundation for future practical translation. Full article

Background/Objectives: This study aims to gain insights into the antimicrobial and antiherpetic activity of hyperforin-rich Hypericum perforatum L. (HP) extract using nanostructured lipid carriers (NLCs) as delivery platforms. Methods: Two established NLC specimens, comprising glyceryl behenate and almond oil or borage oil, and their extract-loaded counterparts (HP-NLCs) were utilized. Their minimal bactericidal/fungicidal concentrations (MBC; MFC) were investigated against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 10145, Klebsiella pneumoniae ATCC 10031, and Candida albicans ATCC 10231. The anti-herpesvirus (HSV-1) potential was evaluated concerning antiviral and virucidal activity and impact on viral adsorption. Results: The borage oil-based extract-loaded nanodispersion (HP-NLC2) exhibited pronounced microbicidal activity against S. aureus (MBC 6.3 mg/mL), K. pneumoniae (MBC 97.7 µg/mL), and C. albicans (MFC < 48.8 µg/mL), unlike the almond oil-containing sample (HP-NLC1), which showed only weak inhibition of the fungal growth. HP-NLC2 was found to be less cytotoxic and to suppress HSV-1 replication slightly more than HP-NLC1, but generally, the effects were weak. Neither the empty lipid nanoparticles nor the HP extract-loaded carriers expressed activity against E. coli, P. aeruginosa, the HSV-1 extracellular virions, or viral adhesion. Conclusions: It could be concluded that both HP-NLC samples revealed only minor antiherpetic potential of the hyperforin-rich extract, but HP-NLC2 demonstrated significant antibacterial and antimycotic activity. Therefore, the latter was featured as a more convenient HP-carrier system for nano-designed dermal pharmaceutical formulations. Such a thorough investigation of hyperforin-determined anti-HSV-1 effects and antibacterial and antimycotic properties, being the first of its kind, contributes to the fundamental knowledge of HP and reveals new perspectives for the utilization, limitations, and therapeutic designation of its non-polar components. Full article

This study explores the development and characterization of lipid nanostructures (NLCs) containing natural deep eutectic solvents (NaDESs) derived from taperebá peel extract (Spondias mombin), a by-product rich in bioactive phenolic compounds, including ellagic acid and quercetin. The taperebá extract exhibited a high polyphenol content (2623 mg GAE/L) and notable antioxidant activity, as demonstrated by DPPH (258 mM TEAC/100 mL) and ABTS (495 mM TEAC/100 mL) assays. NLCs were developed using NaDESs to enhance the stability and bioavailability of the antioxidant compounds. Physicochemical characterization confirmed the formation of stable, nanometric, and monodispersed formulations with efficient encapsulation. Biological evaluation of the NLC-TAP-NaDES formulation demonstrated its remarkable capacity to mitigate oxidative stress in cells subjected to H₂O₂-induced ROS generation. Fluorescence imaging revealed a significant reduction in intracellular ROS levels in treated cells compared to untreated controls, confirming the antioxidant efficacy of the formulation. This outcome underscores the synergy between NaDESs and NLC systems in protecting and delivering phenolic compounds. This study highlights the potential of utilizing underexplored by-products, such as taperebá peels, to develop sustainable and effective antioxidant delivery systems. The NLC-TAP-NaDES platform combines nanotechnology with green chemistry principles, presenting significant implications for the treatment of oxidative stress-related conditions and broader applications in pharmaceutical and nutraceutical sciences. These findings contribute to advancing sustainable innovations in antioxidant therapies, leveraging the dual benefits of bioeconomy and high-performance nanomaterials. Full article

Edaravone is one of the treatment options for Amyotrophic Lateral Sclerosis, but its therapeutic efficacy is limited due to the incapacity to cross the blood–brain barrier, as well as its short life span and poor stability, which is ultimately caused by its tautomerism in physiological condions. This work presents an overview about the use of several nanoformulations based on polymeric, protein, lipidic, or hybrid structure as suitable and stable drug delivery systems for encapsulating edaravone. We also evaluated the functionalization of nanoparticles with pegylated chains using the polyethylene glycol or tocopherol polyethylene glycol succinate and the possibility of preparing polymeric nanoparticles at different pH (7.4, 9, and 11). Edaravone was sucessfully encapsulated in polymeric, lipid–polymer hybrid, and lipidic nanoparticles. The use of higher pH values in the synthesis of polymeric nanoparticles has led to a decrease in nanoparticle size and an increase in the percentage of encapsulation efficiency. However, the resulting nanoformulations are not stable. Only polymeric and hybrid nanoparticles showed good stability over 80 days of storage, mainly at 4 °C. Overall, the nanoformulations tested did not show cytotoxicity in the SH-SY5Y cell line except the nanostructured lipid carrier formulations that showed some cytotoxicity possibly due to lipidic peroxidation. In conclusion, this work shows that edaravone can be encapsulated in different nanocarriers that could act as an interesting alternative for the treatment of Amyotrophic Lateral Sclerosis. Full article

Objectives: This study aimed to develop hesperidin solid lipid nanoparticles (HESP-SLNs) to enhance their stability, solubility, and sustained release for wound healing; further enhancement was achieved through prepared nanostructured lipid carriers (HESP-NLCs) using Tea Tree Oil (TTO) to explore their synergistic efficacy. Methods: A factorial design of 2⁴ trials was established to evaluate the influence of lipid type (X1), lipid conc (%) (X2), surfactant type (X3), and sonication amplitude (%) (X4) of prepared HESP-SLNs on the particle size (nm) (Y1), polydispersibility index (Y2), zeta potential (Y3), and encapsulation efficiency (%) (Y4). The optimized HESP-SLNs formula was selected utilizing Design Expert^® software version 13, which was additionally enhanced by preparing TTO-loaded HESP-NLCs. In vitro release, Raman spectroscopy, and transmission electron microscopy were carried out for both lipid nanoparticles. Cytotoxicity, in vivo wound-healing assessments, and skin irritancy tests were performed to evaluate the performance of TTO-incorporated HESP-NLCs compared to HESP-SLNs. Results: The optimized formula demonstrated PS (280 ± 1.35 nm), ZP (−39.4 ± 0.92 mV), PDI (0.239 ± 0.012), and EE% (88.2 ± 2.09%). NLCs enhanced Q6% release, (95.14%) vs. (79.69%), for SLNs and showed superior antimicrobial efficacy. Both lipid nanoparticles exhibited spherical morphology and compatibility between HESP and excipients. NLCs achieved the highest wound closure percentage, supported by histological analysis and inflammatory biomarker outcomes. Cytotoxicity evaluation showed 87% cell viability compared to untreated HSF cells, and the skin irritancy test confirmed the safety of NLCs. Conclusions: TTO-loaded HESP-NLCs are promising candidates exhibiting superior wound-healing capabilities, making them a potential therapeutic option for cutaneous wound management. Full article

This research aimed to develop mucoadhesive buccal films incorporating nanostructured lipid carriers (NLCs) loaded with triamcinolone acetonide (TN-films). A Box–Behnken design was employed as a systematic approach to optimize the formulation. Key components of the NLCs—spermaceti, soybean oil, and polysorbate 80—were considered independent variables. The NLCs were prepared and size-reduced using a combination of hot homogenization and ultrasonic probe techniques. Films were cast using hydroxypropyl methylcellulose (HPMC) as the film-forming agent. The TN-films were characterized based on weight, thickness, tensile strength, elongation at break, contact angle, and surface free energy. Linear regression showed that spermaceti increased film weight and thickness, while polysorbate 80 decreased them. The mechanical strength of the films was primarily influenced by spermaceti; higher concentrations of spermaceti resulted in decreased film strength. Additionally, all independent variables contributed positively to the lipophilicity of the films. The TN-films were found to sustain drug release via a Fickian diffusion mechanism, exhibiting rapid swelling and favorable mucoadhesive properties. Moreover, the TN-films demonstrated superior drug release and permeation to pastes and films loaded with emulsions. These findings suggest that the TN-films represent a promising and effective approach for the buccal delivery of triamcinolone acetonide. Full article

Background: Phytocarriers are advanced drug delivery systems that use biocompatible and biodegradable materials to enhance the efficacy, stability, and bioavailability of natural products. The sea buckthorn (Hippophae rhamnoides L.) berry extract is rich in essential fatty acids and antioxidants, including vitamin C, vitamin E, and anthocyanins, which contribute to its wide-ranging health benefits. In this study, we assessed the morphology, intracellular delivery, and anti-inflammatory effect of sodium cholate (NaC) and sodium deoxycholate (NaDC)-based phytocarriers loaded with ethanolic extract from sea buckthorn berries (sea buckthorn carrier nanostructures, further defined as phytocarriers). Methods: Negative and electron cryo-microscopy were used to analyze hollow and loaded nanocarriers. The cyto-compatibility of nanocarriers was assessed by endpoint (LDH and MTS) and real-time cell assays, on both human fibroblasts (HS27) and human normal monocytes (SC). The anti-inflammatory effect of hollow and loaded nanocarriers was tested by multiplexing. Results: The negative and electron cryo-microscopy analyses showed that NaC-based phytocarriers were spherical, whilst NaDC-based phytocarriers were predominantly polymorphic. Moreover, the NaDC-based phytocarriers frequently formed large lipid networks or “plaques”. Although 24 h cytotoxicity testing showed both types of nanocarriers are biocompatible with human fibroblasts and monocytes, based on a long-term real-time assay, NaDC delayed fibroblast proliferation. NaC sea buckthorn phytocarriers did not impair fibroblast proliferation in the long term and they were uptaken by cells, as shown by hyperspectral microscopy. NaC nanocarriers and NaC sea buckthorn phytocarriers induced an anti-inflammatory effect, lowering IL-8 cytokine production in normal human monocytes as soon as 4 h of treatment lapsed. Conclusions: NaC-derived phytocarriers loaded with sea buckthorn alcoholic extract are a cell-compatible delivery system with anti-inflammatory properties. Full article

Naturally available antioxidants offer remarkable medicinal applications in wound healing. However, the encapsulation of these phytoactive moieties into suitable nano-scale drug delivery systems has always been challenging due to their inherent characteristics, such as low molecular weight, poor aqueous solubility, and inadequate skin permeability. Here, we provide a systematic review focusing on the major obstacles hindering the development of various lipid and polymer-based drug transporters to carry these cargos to the targeted site. Additionally, this review covers the possibility of combining the effects of a polymer and a lipid within one system, which could increase the skin permeability threshold. Moreover, the lack of suitable physical characterization techniques and the challenges associated with scaling up the progression of these nano-carriers limit their utility in biomedical applications. In this context, consistent progressive approaches for addressing these shortcomings are introduced, and their prospects are discussed in detail. Full article

Background/Objectives: Oxidative stress significantly impacts skin health, contributing to conditions like aging, pigmentation, and inflammatory disorders. Curcumin, with its potent antioxidant properties, faces challenges of low solubility, stability, and bioavailability. This study aimed to encapsulate curcumin in three lipid nanocarriers—solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and nanoemulsions (NEs)—to enhance its stability, bioavailability, and antioxidant efficacy for potential therapeutic applications in oxidative-stress-related skin disorders. Methods: The lipid nanocarriers were characterized for size, polydispersity index, ζ-potential, and encapsulation efficiency. Stability tests under various conditions and antioxidant activity assays (DPPH and FRAP methods) were conducted. Cytotoxicity in human dermal fibroblasts was assessed using MTT assays, while the expression of key antioxidant genes was evaluated in human dermal fibroblasts under oxidative stress. Skin penetration studies were performed to analyze curcumin’s distribution across the stratum corneum layers. Results: All nanocarriers demonstrated high encapsulation efficiency and stability over 90 days. NLCs exhibited superior long-term stability and enhanced skin penetration, while NE formulations facilitated rapid antioxidant effects. Antioxidant assays confirmed that curcumin encapsulation preserved and enhanced its bioactivity, particularly in NLCs. Gene expression analysis revealed upregulation of key antioxidant markers (GPX1, GPX4, SOD1, KEAP1, and NRF2) with curcumin-loaded nanocarriers under oxidative and non-oxidative conditions. Cytotoxicity studies confirmed biocompatibility across all formulations. Conclusions: Lipid nanocarriers effectively enhance curcumin’s stability, antioxidant activity, and skin penetration, presenting a targeted strategy for managing oxidative stress in skin applications. Their versatility offers opportunities for tailored therapeutic formulations addressing specific skin conditions, from chronic disorders like psoriasis to acute stress responses such as sunburn. Full article