Search Results (218)

Therapeutic peptides have gained significant attention due to their high specificity, potency, and safety profiles in treating various diseases. However, their clinical application via the oral route remains challenging. Peptides are inherently unstable in the gastrointestinal environment, where they are rapidly degraded by proteolytic enzymes and acidic pH, leading to poor bioavailability. Additionally, their large molecular size and hydrophilicity restrict passive diffusion across the epithelial barriers of the gastrointestinal tract. These limitations have traditionally necessitated parenteral administration, which reduces patient compliance and convenience. The oral cavity, comprising the buccal and sublingual mucosa, offers a promising alternative for peptide delivery. Its rich vascularization allows for rapid systemic absorption while bypassing hepatic first-pass metabolism. Furthermore, the mucosal surface provides a relatively permeable and accessible site for drug administration. However, the oral cavities also present significant barriers: the mucosal epithelium limits permeability, the presence of saliva causes rapid clearance, and enzymes in saliva contribute to peptide degradation. Therefore, innovative strategies are essential to enhance peptide stability, retention, and permeation in this environment. Nanoparticle-based delivery systems, including lipid-based carriers such as liposomes and niosomes, as well as polymeric nanoparticles like chitosan and PLGA, offer promising solutions. These nanocarriers protect peptides from enzymatic degradation, enhance mucoadhesion to prolong residence time, and facilitate controlled release. Their size and surface properties can be engineered to improve mucosal penetration, including through receptor-mediated endocytosis or by transiently opening tight junctions. Among these, niosomes have shown high encapsulation efficiency and sustained release potential, making them particularly suitable for oral peptide delivery. Despite advances, challenges remain in translating these technologies clinically, including ensuring biocompatibility, scalable manufacturing, and patient acceptance. Nevertheless, the oral cavity’s accessibility, combined with nanotechnological innovations, offers a compelling platform for personalized, non-invasive peptide therapies that could significantly improve treatment outcomes and patient quality of life. Full article

Background/Objectives: Liposomes and niosomes are established drug delivery systems, some of which have received FDA approval and demonstrated therapeutic efficacy. This study investigates a novel niosome formulation, utilizing two natural food-derived components, as a cost-effective alternative to traditional nanocarriers. The active pharmaceutical ingredient, calcium fructoborate (CF), possesses notable anti-inflammatory properties. The study aims to evaluate the efficacy of this novel natural niosome (NN) system, in comparison to existing nanocarrier formulations, in an ischemia–reperfusion (I/R) pain model. Methods: An acute ischemia/reperfusion injury model was employed to induce pain in 36 rats. The efficacy of the following treatments was assessed: standard CF, liposomal CF, niosomal CF, and natural niosomal CF. Efficacy was determined by quantifying the treatments’ ability to mitigate inflammation and oxidative stress in the kidneys, lungs, heart, and liver, and by evaluating potential organ damage through histopathological analysis. Results: The NN treatment significantly reduced malondialdehyde (MDA) and tumor necrosis factor-alpha (TNF-α) levels in the kidneys and liver compared to the other treatments (p < 0.05). In the kidney, NN treatment also significantly decreased creatinine levels relative to the other treatments (p < 0.01). The histopathological analysis of kidney tissue revealed that NN treatment attenuated tubular dilation, interstitial inflammation, and epithelial thinning. In the heart, liposomal treatment significantly increased MDA levels (p < 0.05) and decreased sialic acid levels (p < 0.05); however, no significant differences were observed in troponin levels (p > 0.05). In the lung, no significant differences in MDA, lactate, TNF-α, or sialic acid levels were detected among the treatment groups (p > 0.05). Conclusions: The natural niosome drug delivery system demonstrates potential as a therapeutic intervention for protecting and improving kidney and liver health. While liposomal treatment exhibited some adverse effects, it effectively suppressed inflammation. This study provides a foundation for future research and positions the NN drug delivery system as a promising, cost-effective alternative for inflammation-associated pathologies. Full article

This study aimed to formulate a carrier system to improve the oral bioaccessibility of goat casein peptides (GCAPS). Goat casein was hydrolyzed with papain and subsequently purified to obtain bioactive peptide fractions (GCAPS) with potent hypoglycemic activity. On this basis, spherical GCAPS-loaded nanocarrier systems were developed, including liposomes (GCAPS-LS) and niosomes (GCAPS-NS). Among them, GCAPS-NS exhibited higher encapsulation efficiency (94.98 ± 3.01%) and a smaller particle size (89.81 ± 8.97 nm) than GCAPS-LS. FT-IR analysis confirmed successful peptide encapsulation. Simulated gastrointestinal digestion experiments demonstrated that GCAPS-NS significantly improved GCAPS retention and DPP-IV inhibition. In vivo results from high-fat diet-induced (HFD) insulin-resistant mice demonstrated that GCAPS-NS effectively ameliorated metabolic abnormalities by including adiposity, enhancing GLP-1 levels and suppressing hsCRP expression, thereby contributing to improved glycemic homeostasis. Moreover, GCAPS-NS intervention resulted in a significant enrichment of Akkermansia and a reduced Firmicutes/Bacteroidetes ratio, suggesting its beneficial role in alleviating HFD gut dysbiosis. These findings indicated that goat casein peptides held great potential as a functional food for the management of type 2 diabetes. Full article

Purple waxy corn cobs (PWCCs) represent an underutilized agricultural waste rich in anthocyanins with promising cosmeceutical potential. This study investigated niosome-based encapsulation to enhance the stability and bioactivity of PWCC anthocyanin extracts. PWCC extract was macerated in 50% ethanol. The extract exhibited a high total anthocyanin content (3.02 ± 0.81 mg C3GE/L), while cyanidin-3-glucoside identified as the major anthocyanin (1.17 ± 0.02 mg/g dry weight). Furthermore, the extracts showed strong antioxidant activities as evidence by DPPH, ABTS, and FRAP assays. The optimized niosome preparations synthesized by the probe sonication method exhibited better entrapment efficiency (80–85%), nanoscale particle size (185–296 nm), and stable zeta potential (−29 to −32 mV). TEM verification of the spherical morphology and FT-IR spectra confirmed the successful loading of anthocyanins. The thermal stability test exhibited negligible changes in the particle size and zeta potential. Furthermore, in vitro release profile followed the Higuchi model, indicating enhanced release kinetics. Biological assays demonstrated moderate UVB protection effects and potent anti-melanogenesis activity in B16F10 cells. Notably, formulation N5 exhibited the highest tyrosinase inhibition and melanin synthesis suppression. These findings indicate that niosome-based encapsulation represents a promising strategy for enhancing the stability, bioavailability, and biological efficacy of anthocyanin extracts, especially in the cosmetic and pharmaceutical industries. Full article

Background/Objectives: The study describes the elaboration and evaluation of thermosensitive niosomes intended for the systemic application of daunorubicin hydrochloride. The attained stimulus sensitivity would determine the release of the chemotherapeutic predominantly at the target site, which ensures a higher drug concentration and leads to reduced systemic toxicity. The latter is highly beneficial, as the anthracycline antibiotic is known for its dose-dependent cardiotoxic effects. Methods: Conventional and copolymer-modified niosomes were prepared via thin-film hydration and the transmembrane ammonium gradient method, allowing us to assess the impacts of copolymer type-DHP-PiPOX (1,3-dihexadecyl-propane-2-ol-poly(2-isopropyl-2-oxazoline)) or DHP-PETEGA (1,3-dihexadecyl-propane-2-ol-poly(ethoxytriethylene glycol acrylate)) and their concentrations (0.5, 1, and 2.5 mol%), as well as the method of preparation, on the main physicochemical properties of the vesicles. Niosomes were characterized in terms of their size, polydispersity index (PDI), zeta potential, entrapment efficiency, morphology, and drug release properties. Thermosensitivity was evaluated by fluorescence studies, and the antiproliferative activity of optimized formulations was assessed against the acute myelocyte leukemia-derived HL-60 cell line. Results: Daunorubicin-loaded niosomes modified with DHP-PiPOX and DHP-PETEGA at 2.5 mol% exhibited suitable physicochemical properties for systemic application, with sizes below 200 nm (155 and 158 nm respectively), low PDI values of 0.25 and 0.29, spherical morphology, and high daunorubicin entrapment efficiency (68.6 and 66.5% respectively). The vesicles showed temperature-dependent drug release properties and superior antiproliferative activity compared to the free daunorubicin (IC₅₀ values of 6.91 and 8.54 vs. 12.14). Conclusions: The obtained results indicate that the developed thermosensitive nanovesicles may serve as a suitable drug delivery system for the systemic application of daunorubicin hydrochloride. Full article

Nisin, a food preservative lantibiotic produced by Lactococcus lactis, exhibits potent antimicrobial activity against a wide range of Gram-positive pathogens, including antibiotic-resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA). This study explores the development of a novel nano drug delivery platform comprising nisin-loaded niosomes, formulated via microfluidic mixing, and integrated into fast-dissolving oral films for targeted buccal administration. Microfluidic synthesis enabled the precise control of critical parameters including the flow rate ratio, surfactant composition, and lipid concentration, resulting in uniform niosomal vesicles with optimal size distribution (100–200 nm), low polydispersity index, and high encapsulation efficiency. Span 40 and Span 60 were employed as non-ionic surfactants, stabilized with cholesterol to improve bilayer rigidity and drug retention. The encapsulated nisin demonstrated improved physicochemical stability over time and protection against proteolytic degradation, thus preserving its antimicrobial potency. The niosomal suspensions were subsequently incorporated into polymer-based oral films as a final dosage form composed of polyvinyl alcohol (PVA) as the primary film-forming polymer, polyethylene glycol 400 (PEG400) as a plasticizer, and sucralose and mint as a sweetener and flavoring agent, respectively. A disintegrant was added to accelerate film dissolution in the oral cavity, facilitating the rapid release of niosomal nisin. The films were cast and evaluated for thickness uniformity, mechanical properties, disintegration time, surface morphology, and drug content uniformity. The dried films exhibited desirable flexibility, rapid disintegration (<30 s), and consistent distribution of nisin-loaded vesicles. In vitro antimicrobial assays confirmed that the bioactivity of nisin was retained post-formulation, showing effective inhibition zones (16 mm) against Bacillus subtilis. This delivery system offers a promising platform for localized antimicrobial therapy in the oral cavity, potentially aiding in the treatment of dental plaque, oral infections, and periodontal diseases. Overall, the integration of microfluidic-synthesized nisin niosomes into oral films presents a novel, non-invasive strategy for enhancing the stability and therapeutic efficacy of peptide-based drugs in mucosal environments. Physicochemical characterization of the niosomes and niosome films was performed using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) to evaluate thermal stability and scanning electron microscopy (SEM) to assess surface morphology. In vitro peptide release studies demonstrated sustained release from both niosomal suspensions and film matrices, and the resulting data were further fitted to established kinetic models to elucidate the underlying drug release mechanisms. This delivery system offers a promising platform for localized antimicrobial therapy in the oral cavity, potentially aiding in the treatment of dental plaque, oral infections, and periodontal diseases. Overall, the integration of microfluidic-synthesized nisin niosomes into oral films presents a novel, non-invasive strategy for enhancing the stability and therapeutic efficacy of peptide-based drugs in mucosal environments. Full article

Azelaic acid (AzA), a saturated dicarboxylic acid, is indicated for the treatment of acne vulgaris, rosacea, melasma, and post-inflammatory hyperpigmentation. Its antimicrobial, anti-inflammatory, and antimelanogenic properties support its use; however, its poor aqueous solubility and limited skin permeability constrain its optimal topical delivery. This review summarizes clinical evidence and advances in formulations—including conventional vehicles, polymeric/lipid nanocarriers, and deep eutectic solvent (DES) systems—to promote more effective and well-tolerated use. Across indications, 15–20% azelaic acid (AzA) formulations produced clinically meaningful improvements with mild, transient local irritation. For acne vulgaris, reductions in inflammatory and noninflammatory lesions were comparable to those of topical retinoids/adapalene, and tolerability was superior in some studies. For rosacea, the 15% gel formulation was comparable to metronidazole in reducing papules, pustules, and erythema while maintaining negligible systemic exposure. In melasma and other dyschromias, 20% cream demonstrated efficacy similar to hydroquinone, exhibiting a favorable safety profile. Advanced delivery systems, including liposomes, niosomes/ethosomes, nanostructured lipid carriers, microemulsions, nanosponges, and DES platforms, increased AzA solubilization, cutaneous deposition, and stability. This enabled dose-sparing strategies and improved adherence. Data on AzA cocrystals and ionic salts suggest additional control over release and irritation. AzA remains a versatile and well-tolerated dermatologic agent whose performance is strongly vehicle-dependent. Rational selection and engineering of carriers, particularly DES-integrated polymeric and lipid systems, can mitigate solubility and permeability limitations, enhance skin targeting, and reduce irritation in the treatment of acne and rosacea. Full article

Niosomes are nanocarriers with a bilayer structure, consisting of a polar region and a non-polar region. This unique structure allows them to encapsulate compounds with varying polarities, addressing solubility challenges in the transport and delivery of bioactive molecules. The formation of niosomes involves key structural, geometric, and thermodynamic factors influenced by the choice of surfactants and preparation methods. These factors, including the critical packing factor and the hydrophilic–lipophilic balance (HLB), play a crucial role in determining the properties of the final niosomes. Additionally, the use of Tandford’s equations allows for the calculation of geometric parameters. These factors determine the structural integrity and functional properties of niosomes, making it possible to design functional niosomes with characteristics tailored for specific applications. This ability to design niosomes with desired properties is especially valuable in biomedical fields, where precise control over drug delivery and targeting is essential. This review highlights the importance of niosome formulation and presents examples of niosomes that have been functionalized for specific applications, including anticancer treatments, immunological treatments, and their action in the central nervous system. Full article

Ozone (O₃) occurs in nature as a chemical compound made of three oxygen atoms. It is an unstable, highly oxidative gas that rapidly decomposes into oxygen. The therapeutic use of O₃ dates back to the beginning of the 20th century and is currently based on the application of low doses, inducing a moderate oxidative stress that stimulates the antioxidant cellular defenses without causing cell damage. Low O₃ doses also induce anti-inflammatory and regenerative effects, and their anticancer potential is under investigation. In addition, the oxidative properties of O₃ make it an excellent antibacterial, antimycotic, and antiviral agent. Thanks to these properties, O₃ is currently widely used in several medical fields. However, its chemical instability represents an application limit, and ozonated oil is the only stabilized form of medical O₃. In recent years, novel O₃ formulations have been proposed for their sustained and more efficient administration, based on nanotechnology. This review offers an overview of the nanocarriers designed for the delivery of medical O₃, and of their therapeutic applications. The reviewed articles demonstrate that research is active and productive, though it is a rather new entry in the nanotechnological field. Liposomes, nanobubbles, nanoconstructed hydrogels, polymeric nanoparticles, and niosomes were designed to deliver O₃ and have been proven to exert antiseptic, anticancer, and pro-regenerative effects when administered in vitro and in vivo. Improving the therapeutic administration of O₃ through nanocarriers is a just-started challenge, and multiple prospects may be foreseen. Full article

Background/Objectives: 5-Fluorouracil (5-FU) and Irinotecan (IRT) are two of the most used chemotherapeutic agents in CRC treatment. However, achieving treatment goals has been hampered by poor drug delivery to tumor sites and associated toxicity from off-target binding to healthy cells. Though the synergism of 5-FU-IRT has provided incremental improvements in clinical outcomes, the short elimination half-life and off-target binding to healthy cells remain significant challenges. We postulated that nanoencapsulation of a combination of 5-FU and IRT in niosomes would prolong the drugs’ half-lives, while over-encapsulation lyophilized powder in Targit^® oral capsules would passively the CRC microenvironment and avoid extensive systemic distribution. Methods: Ranges of formulation and process variables were input into design of experiment (DOE Fusion One) software, to generate screening experiments. Niosomes were prepared using the thin-film hydration method and characterized by size, the polydispersity index (PDI), morphology and intrastructure, and drug loading. Blank niosomes ranged in size from 215 nm to 257 nm. Results: After loading with the 5-FU-IRT combination, the niosomes averaged 251 ± 2.20 nm with a mean PDI of 0.293 ± 0.01. The surfactant-to-cholesterol ratio significantly influenced the niosome size and the PDI. The hydrophilic 5-FU exhibited superior loading compared to the lipophilic IRT molecules, which probably competed with other lipophilic niosome components in niosomes’ palisade layers. In vitro dissolution in biorelevant media showed delayed release until lower intestinal region (IRT) or colonic region (5-FU). Conclusions: Thus, co-nanoencapsulation of 5-FU/IRT in niosomes, lyophilization, and over-encapsulation of powder in colon-specific capsules could passively target the CRC cells in the colonic microenvironment. Full article

Background: The active (remote) loading of drugs into nanoparticulate systems via the pH gradient technique has been proven highly successful in liposomes, as numerous formulations have reached the market. However, this is not the case for niosomes, as the full potential of this area remains largely undiscovered. The purpose of this research is to study the effect of different co-surfactants (Cremophor RH 40, Cremophor ELP and Solutol HS-15) on stabilising the niosomal membrane to enable the creation of a pH gradient. Methods: For visualisation of pH gradients, pH indicator bromocresol green (BCG) was used as a novel encapsulated model molecule to visually investigate the ability of niosomes to entrap drugs through active loading. Thereafter, the optimised BCG niosomal formulation was applied to encapsulate a therapeutic drug molecule, doxorubicin, via pH gradient active loading. Niosomes were formulated via thin-film hydration using Span 60, cholesterol, with or without co-surfactants. Thin films were hydrated with either Trizma buffer or HEPES buffer for BCG, or ammonium sulfate for doxorubicin. The niosomes’ outer membrane pH was adjusted via either the addition of HCl or citric acid in the case of BCG, or by passing the niosomes through a Sephadex G50 gel column, pre-equilibrated with PBS or Trizma buffer, in the case of doxorubicin. Results: Niosomes formulated with Span 60 and cholesterol could not be formed at acidic pH and thus could not create a pH gradient. All three co-surfactants, when added to Span 60 and cholesterol, stabilised the niosomes and enabled them to form a pH gradient. Niosomes (after size reduction) containing Solutol HS-15 showed significantly higher entrapment efficiency of BCG when compared to Cremophor RH 40 and Cremophor ELP (67.86% vs. 15.57% vs. 17.81%, respectively, with sizes of 159.6 nm, 177.9 nm and 219.1 nm, respectively). The use of HEPES buffer resulted in a higher EE of BCG compared to Trizma buffer (72.85% vs. 67.86%) and achieved a size of 283.4 nm. The Solutol HS-15 containing formulation has exhibited 68.28% EE of doxorubicin with ammonium sulfate as the inner buffer, while the external buffer was Trizma with a size of 241.1 nm after extrusion. Conclusions: Niosomal formulations containing Solutol HS-15 are highly promising for remote drug loading. The novel use of BCG for studying pH gradient and drug loading into niosomes has proved beneficial and successful. Full article

Meloxicam is a promising non-steroidal anti-inflammatory drug (NSAID) for acute and chronic pain prevention and treatment. Due to its poor water solubility, the clinical use of meloxicam is limited. In addition, for transdermal applications, the impermeability of the skin makes it difficult to conceive an appropriate NSAID-based delivery system that can penetrate through the skin barrier. Hydrophilic/hydrophobic gels, designed as transdermal drug delivery systems, can considerably improve other drug administration types (such as oral or intravenous), avoiding or limiting the side effects. The main purpose of this paper is to present some physicochemical and pharmaceutical considerations about meloxicam and to review the most important research concerning the gels used for the transdermal delivery of meloxicam. Thus, smart polymeric networks, semi-solid systems (lipogels, emulgels), β-cyclodextrin-based gels, liposomes (ethosomes, niosomes, flexosomes, transferosomes, menthosomes, invasomes), and nanostructured lipid carriers, with analgesic and anti-inflammatory activity, are discussed. The key objective of this study was to highlight various gel formulations with enhanced properties, which could be used in a minimally invasive manner for the sustained administration of meloxicam. Full article

Hydrophilic phytochemicals, such as flavonoids and phenolic acids, possess important biological activities, including antioxidant, anti-inflammatory, and anticancer effects. However, their application is hindered by low membrane permeability, poor chemical stability, and limited skin penetration. This review provides a comprehensive analysis of advanced delivery strategies aimed at enhancing the solubility, bioavailability, and therapeutic efficacy of selected hydrophilic compounds. Specifically, it focuses on the encapsulation of flavonoids such as quercetin, luteolin, and apigenin, as well as phenolic acids including ferulic acid, caffeic acid, and chlorogenic acid. The review discusses various nanocarrier systems: liposomes, niosomes, exosomes, and polymeric nanoparticles (e.g., nanocapsules, nanospheres) and compares their structural characteristics, preparation methods, and functional benefits. These delivery systems improve the physicochemical stability of active compounds, enable controlled and targeted release, and enhance skin and cellular absorption. Despite certain challenges related to large-scale production and regulatory constraints, such approaches offer promising solutions for the pharmaceutical and cosmetic application of hydrophilic plant-derived compounds. Full article

The development of nanocarriers for drug delivery has drawn a lot of attention due to the possibility for tailored delivery to the ill region while preserving the neighboring healthy tissue. In medicine, delivering drugs safely and effectively has never been easy; therefore, the creation of surfactant-based vesicles (niosomes) to enhance medication delivery has gained attention in the past years. Niosomes (NIOs) are versatile drug delivery systems that facilitate applications varying from transdermal transport to targeted brain delivery. These self-assembling vesicular nano-carriers are formed by hydrating cholesterol, non-ionic surfactants, and other amphiphilic substances. The focus of the review is to report on the latest NIO-type formulations which also include biopolymers from the polysaccharide class, highlighting their role in the development of these drug delivery systems (DDSs). The NIO and polysaccharide types, together with the recent pharmaceutical applications such as ocular, oral, nose-to brain, pulmonary, cardiac, and transdermal drug delivery, are all thoroughly summarized in this review, which offers a comprehensive compendium of polysaccharide-based niosomal research to date. Lastly, this delivery system’s limits and prospects are also examined. Full article

Strawberries face marketing challenges due to their short post-harvest shelf-life, largely impacted by shrivelling, weight loss, fungal decay, and mechanical damage. Neem oil (NO) is known for its shelf-life extension benefits; however, encapsulation is needed to maintain its efficacy. This study aimed to stabilize and encapsulate NO in a polymeric and lipid material to preserve the quality of strawberries stored at 4 ± 1 °C, 80 ± 2% RH for seven days. After seven days, the nanoparticle-coated fruits showed a weight loss of around 5.9% with niosomes and 8.9% with starch nanoparticles, while the control had a significant 32.45% weight loss. Additionally, both nanoparticle coatings significantly (p < 0.05) preserved fruit colour compared to the untreated control. The findings suggest that nanoparticle coatings could serve as an active agent in preserving the quality of strawberries within the food supply chain. The study provides valuable insights into post-harvest management and fruit preservation, showcasing the effectiveness of these coatings as active packaging solutions. Full article