Search Results (107)

Artocarpin, a prenylated flavonoid isolated from Artocarpus altilis heartwood, has emerged as a promising multi-targeted bioactive compound for combating UV-induced skin aging. This review provides a comprehensive overview of the molecular mechanisms and photoprotective efficacy of artocarpin across in vitro, in vivo and clinical study, based on the peer-reviewed literature published between 2012 and 2025, retrieved from PubMed, Scopus, and Web of Science. Delivery strategies designed to overcome the inherent physicochemical limitations of artocarpin on skin penetration are also discussed. Artocarpin demonstrates antioxidant effects through both direct free radical scavenging and activation of the Nrf2-ARE pathway, providing sustained cellular defense. Its anti-inflammatory properties target multiple signaling cascades, including the NF-κB and MAPK pathways, effectively mitigating UV-induced inflammatory response. The compound maintains dermal matrix homeostasis by inhibiting matrix metalloproteinase-1 (MMP-1) expression while preserving collagen synthesis and fibroblast mechanical function. Additionally, artocarpin exhibits selective apoptosis modulation, being cytoprotective in normal keratinocytes while acting as pro-apoptotic in damaged or abnormal cells, thereby supporting tissue homeostasis. It also inhibits melanogenesis through anti-inflammatory mechanisms rather than direct tyrosinase inhibition. Furthermore, artocarpin has been shown to induce autophagic cell death in certain cell lines; however, its role in UV-induced skin damages remains to be clarified. Despite these promising biological activities, the poor water solubility (<0.1 mg/mL) and high lipophilicity (log P ≈ 5) of artocarpin significantly limit its skin penetration. Lipid-based delivery systems, including liposomes, transfersomes, ethosomes, and nanostructured lipid carriers (NLCs), are presented as effective strategies to enhance transepidermal delivery, with each system offering distinct mechanistic advantages. Further investigations should prioritize the safety of artocarpin within each delivery system, as well as the synergistic co-encapsulation with complementary natural antioxidants to simultaneously target multiple mechanisms involved in UV-induced skin damage, thereby broadening its application in the cosmeceutical industry. Full article

Background: Hydrolyzed collagen peptides (HCP) are widely used as bioactive ingredients in anti-aging and skin rejuvenation formulations due to their role in supporting skin hydration, elasticity, and extracellular matrix integrity. However, their high hydrophilicity limits effective incorporation into lipid-based systems, and restricts controlled release from formulations. Objective: In this study, ethosomal nanocarriers were designed as a phospholipid–ethanol-based system to promote favorable molecular interactions with hydrophilic peptides, aiming to enhance the encapsulation, stability, and controlled release of HCP for dermocosmetic applications. Methods: HCP-loaded ethosomes were prepared using phospholipid (Lipoid P75) and ethanol and optimized by varying high-pressure homogenization cycles. Physicochemical properties, including vesicle size, distribution uniformity, zeta potential, pH, and long-term stability, were monitored for up to 180 days. Vesicle morphology and peptide–lipid interactions were characterized using cryo-scanning electron microscopy and FTIR spectroscopy. Encapsulation efficiency was determined by ultrafiltration, while cytocompatibility was assessed in HaCaT keratinocyte cells. In vitro release behavior was investigated using Franz diffusion cells and compared with aqueous HCP solutions. Results: All formulations exhibited nanoscale size distribution and high colloidal stability, with negative zeta potentials ranging from −42.9 to −76.7 mV. The optimized formulation demonstrated sustained encapsulation efficiency (73% after 180 days) and preservation of peptide structure, as confirmed by FTIR, indicating effective chemical stabilization within the ethosomal matrix. Cytotoxicity studies confirmed good skin cell compatibility. In vitro release studies revealed a controlled and prolonged release profile from ethosomal carriers compared with free HCP solutions, suggesting improved topical bioavailability of collagen peptides. Conclusions: To the best of our knowledge, this work provides one of the first systematic investigations of optimized ethosomal systems for the stabilization of hydrophilic collagen peptides as anti-aging dermocosmetic ingredients. These findings demonstrate that optimized HCP-loaded ethosomes represent a promising ingredient formulation platform enabling bioactive preservation, formulation stability, and controlled topical performance for collagen-based skin rejuvenation applications. Full article

Background/Objectives: Brimonidine tartrate (BRT), a selective α2-adrenergic receptor agonist, is commonly used in the treatment of glaucoma. However, conventional eye drop formulations suffer from poor ocular bioavailability and rapid elimination. This study aimed to develop and evaluate BRT-loaded ethosomes as a nanocarrier-based alternative to enhance intraocular delivery and therapeutic efficacy. Methods: Ethosomes were prepared using the thin-film hydration method and optimized via central composite design. The optimized formulation was subjected to physicochemical characterization, in vitro release testing, and ocular irritation assessment using the Hen egg test—chorioallantoic membrane (HET-CAM) model. Additionally, the intraocular pressure (IOP)-lowering efficacy of the formulation was evaluated in a rat glaucoma model. Results: The optimized ethosomal formulation exhibited favorable physicochemical properties, including a mean particle size of 122.6 ± 0.7 nm, zeta potential of −1.8 ± 0.9 mV, and encapsulation efficiency of 87.33 ± 0.04%. In vitro release data followed Higuchi kinetics. HET-CAM analysis indicated non-irritancy. In vivo, the ethosomal BRT formulation achieved comparable IOP-lowering effects to the marketed eye drops at one-third of the dose. Conclusions: The developed BRT-loaded ethosomal system demonstrated promising physicochemical stability, sustained release, and therapeutic potential. These findings suggest that ethosomes may offer a safe and effective strategy for enhancing the ocular delivery of BRT in glaucoma therapy. Full article

The effectiveness of transdermal drug delivery is restricted by the barrier properties of the stratum corneum. Ethosomes, as vesicular carriers, offer a promising approach to enhance dermal bioavailability. This study aimed to optimize ethosome composition and preparation parameters to improve physicochemical stability and performance. The influence of alcohols (ethyl, n-butyl, n-propyl, isopropyl, tert-butyl), glycols (propylene glycol, ethylene glycol, 1,3-butanediol), and surfactants (Tween 80, Mirasoft^® SL L60) was systematically investigated. Stability was evaluated through zeta potential (ZP), polydispersity index (PDI), and hydrodynamic diameter (D_h). The effects of phospholipid concentration and homogenization were also assessed. SEM imaging confirmed the spherical morphology of vesicles. The optimal formulation comprised 30% (w/w) ethanol, 2.5% (w/w) phospholipid, 10% (w/w) ethylene glycol, and 1.25% (w/w) Tween 80. A comparable mixed-surfactant system (0.625% w/w; 60% Tween 80 and 40% Mirasoft^® SL L60) exhibited similar stability, indicating that glycolipid-based biosurfactants can reduce conventional surfactant requirements. Homogenization significantly enhanced colloidal stability, lowering PDI from 0.366 to 0.083 and D_h from 254 nm to 156 nm, evidencing decreased aggregation and improved size uniformity. Overall, formulation composition and processing conditions critically determine ethosome stability and transdermal delivery efficiency. Full article

Nanoparticle-based transdermal drug delivery systems (TDDS) have emerged as a revolutionary approach for antiparasitic therapy, addressing key challenges such as poor bioavailability, systemic toxicity, and drug resistance. This review highlights the advancements in nanotechnology-driven TDDS for combating zoonotic parasitic diseases, including leishmaniasis, malaria, and infections treated by broad-spectrum drugs like ivermectin and albendazole. By leveraging nanocarriers such as liposomes, nanoemulsions, and microneedles, which enhance skin permeation, enable controlled drug release, and improve targeting specificity. For instance, deformable transfersomes and ethosomes achieve high transdermal efficiency without chemical adjuvants, while microneedle arrays physically bypass the stratum corneum for precise delivery. Furthermore, sustained-release hydrogels and stimuli-responsive nanoparticles optimize therapeutic efficacy and reduce adverse effects. Despite promising results, clinical translation faces challenges in manufacturing scalability, long-term safety, and accessibility in resource-limited settings. Future directions include bioinspired nanocarriers, artificial intelligence (AI)-driven design, and integration with global health initiatives like “One Health”, all aimed at ensuring equitable implementation. This review highlights the transformative potential of nanotechnology in achieving sustainable antiparasitic solutions for zoonotic diseases. Full article

Lipid-based nanocarriers are ideal drug delivery systems for transdermal administration due to their biocompatibility and biodegradability. Their lipophilicity and/or similarity to the natural lipids of the epidermis enable intermolecular interactions with the lipid membrane and therefore result in effective passage through the skin. The purpose of this review is to focus on lipid-based drug delivery nanoplatforms administered via the transdermal route by summarizing the most recent developments with the intention of fast clinical translation. Liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), ethosomes, and transfersomes exhibit ideal physicochemical characteristics and encapsulation efficiency to enhance the effectiveness of the incorporated Active Pharmaceutical Ingredients (APIs). The state of the art for fabricating transcutaneous lipid drug delivery nanoparticles and the strategies for overcoming the current obstacles, as well as the added value of novel formulations, will be discussed within the scope of Quality by Design applications. The limitations and challenges that still exist will also be considered. 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

Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, and clinically significant drug–drug interactions, partly mediated by modulation of P-glycoprotein and cytochrome P450 3A4 metabolism. This review explores advanced delivery strategies designed to overcome these limitations. We critically evaluate lipid-based systems, such as solid lipid nanoparticles, liposomes, transferosomes, ethosomes, and cubosomes; polymer-based nanoparticles; microneedles; and implants, including drug-eluting stents. These systems ensure targeted delivery, improve pharmacokinetics, and reduce toxicity. Additionally, we discuss chemical derivatization approaches, such as prodrugs, codrugs, and strategic ring modifications (A-, B-, and C-rings), aimed at optimizing both the efficacy and safety profile of colchicine. Combinatorial nanoformulations that enable the co-delivery of colchicine with synergistic agents, such as glucocorticoids and statins, as well as theranostic platforms that integrate therapeutic and diagnostic functions, are also considered. These innovative delivery systems and derivatives have the potential to transform colchicine therapy by broadening its clinical applications while minimizing adverse effects. Future challenges include scalable manufacturing, long-term safety validation, and the translation of research into clinical practice. Full article

Transdermal drug delivery (TDD) is an increasingly important non-invasive method for administering active pharmaceutical ingredients (APIs) through the skin barrier, offering advantages such as improved therapeutic efficacy and reduced systemic side effects. As demand increases for patient-friendly and minimally invasive treatment options, TDD has attracted substantial attention in research and clinical practice. This review summarizes recent advances enhancing skin permeability through chemical enhancers (e.g., ethanol, fatty acids, terpenes), physical (e.g., iontophoresis, microneedles, sonophoresis), and nanotechnological methods (e.g., liposomes, ethosomes, solid lipid nanoparticles, and transferosomes). A comprehensive literature analysis, including scientific publications, regulatory guidelines, and patents, was conducted to identify innovative methods and materials used to overcome the barrier properties of the stratum corneum. Special emphasis was placed on in vitro, ex vivo, and in vivo evaluation techniques for such as Franz diffusion cells for assessing drug permeation and skin interactions. The findings highlight the importance of active physical methods, passive nanostructured systems, and chemical penetration enhancers. In conclusion, integrating multiple analytical techniques is essential for the rational design and optimization of effective transdermal drug delivery systems. Full article

The new generation of food packaging should not only be biodegradable, but also provide additional protective properties for packaged products, extending their shelf life. In this paper, we present the results of research on cast-extruded poly(butylene succinate) (PBS) films coated with hydroxypropyl methylcellulose (HPMC) modified with CO₂ extract from sea buckthorn (ES) or its ethosomes (ET) at amounts of 1 or 5 pph per HPMC. In addition, the developed films were exposed to accelerated aging (UV radiation and elevated temperature) to determine its effect on the films’ properties. Based on SEM, it can be concluded that accelerated aging results in the uncovering of the extract and ethosomes from the coating’s bulk. GPC showed a decrease in the molecular weight of PBS after treatment, additionally amplified by the presence of HPMC. However, the addition of ES or ET in low concentrations reduced the level of polyester degradation. The presence of the modified coating and its treatment increased the oxygen barrier (a decrease from 324 cm³/m² × 24 h for neat PBS to 208 cm³/m² × 24 h for the coated and modified PBS ET5). Despite the presence of colored extract or ethosomes in the coating, the color differences compared with neat PBS were imperceptible (ΔE < 1). The addition of 5 pph of sea buckthorn extract or its ethosomes in combination with accelerated aging resulted in the complete inhibition of the growth of E. coli and S. aureus, which was not observed in non-aged samples. The results obtained demonstrate an improvement in bioactive properties and protection against the negative effects of UV radiation on the film due to the presence of ET or ES in the coating. The developed systems could be used in the food industry as active packaging. 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

Background/Objectives: Treatment options for androgenic alopecia are still very limited and lack long-term efficacy. Dutasteride (DUT) has gained interest as a potent inhibitor of 5α-reductase, allowing for spaced applications, but DUT oral intake can cause serious adverse effects. Herein, we developed, characterized, and assessed the potential of DUT-loaded ethosomes with increasing ethanolic concentrations for hair follicle (HF) targeting to treat androgenic alopecia, hypothesizing that ethanol’s interaction with HFs’ sebum might increase DUT targeting to the HFs. Methods: Ethosomes were obtained using the water-dropping method. After a hydrodynamic size screening, a 30% ethanol concentration was fixed. Ethosomes with 30% ethanol were also prepared and had their ethanolic content removed by rotary evaporation for the evaluation of ethanol in targeting DUT to the HFs. The targeting factor (Tf) was calculated as the ratio between the DUT amount in HFs and the total DUT amount recovered from all skin layers after in vitro porcine skin penetration tests for 12 and 24 h. Results: The ethanolic concentration affected the vesicles’ size and the targeting potential. While the dried ethosomes could not increase DUT accumulation in the HFs at both time points (Tf: 0.27 in 12 h and Tf: 0.28 in 24 h), the presence of 30% ethanol in the vesicles increased the Tf from 0.28 (12 h) to 0.34 (24 h), significantly superior (p < 0.05) than the dried ethosome and control (Tf: 0.24) in 24 h. Conclusion: Ethosomes with a 30% ethanolic concentration were slightly more efficient in targeting HFs for dutasteride delivery. Full article

The topical administration of drugs on the skin by nanovesicular systems can represent a tool to treat skin pathologies. The study of nanovesicle biodistribution after skin administration is crucial to understanding their transdermal potential. A formative study enabled us to investigate the influence of some methods in the production of nanovesicles based on phosphatidylcholine, differing in their ethanol amount. Particularly, both liposomes and ethosomes produced by different methods, i.e., microfluidics and solvent injection, were considered. The evaluation of size distribution, shape and internal morphology was performed using photon correlation spectroscopy, cryogenic electron microscopy, hyperspectral dark-field microscopy and small-angle X-ray scattering. Transmission electron microscopy was then used to observe and compare the transdermal passage of selected liposomes and ethosomes applied to human skin explants in a bioreactor. The mean diameters of nanovesicles prepared by the ethanol injection method were smaller with respect to those obtained by microfluidics, measuring roughly 140 and 230 nm, respectively. The uni- or multilamellar ultrastructure of the vesicles was influenced by the solvent injection procedure. Ultrastructural analysis of skin penetration revealed (i) the ability of intact vesicles to cross the different skin layers, with ethosomes produced by the water injection method showing greater transdermal potential and (ii) the role of ethanol as a penetration enhancer. Full article

Salak peel extract has various biological properties befitting cosmeceutical applications; however, their practical uses are still limited due to their low water solubility and stability. Encapsulation technology was employed to alleviate these issues. In this work, we presented a simple method to prepare ethosome-encapsulated salak peel extract using green solvents (ethanol and water). For this purpose, we used 95% ethanol to extract salak peel and explored its activities. Results showed that, in addition to anti-oxidant, the extract also showed anti-tyrosinase, anti-inflammatory, and anti-bacterial (against S. aureus) activities. These activities indicate its potential uses in cosmeceutical applications. We further encapsulated the extract in ethosomes using a stirrer and green solvents for the preparation methods. The yielded ethosomes exhibited a size range of 120 to 205 nm, polydispersity index (PDI) of 0.15 to 0.25, and zeta potential of −35 to −60 mV depending on the amount of L-α-phosphatidylcholine used. The highest encapsulation efficiency was approximately 30%. The antiradical capacity and anti-inflammatory activities of salak peel extract were also found to be maintained after the encapsulation process. An in vitro biocompatibility study of the extract after encapsulation was also performed. The results not only indicated good biocompatibility, but also the potential skin-rejuvenating ability of salak peel ethosomes. A stability study was also performed, and the results suggested that these ethosomes were stable at different conditions. With further investigation, salak peel ethosomes, as presented here, can be suitable for cosmeceutical applications. Full article

Background: Methicillin-resistant Staphylococcus aureus (MRSA) considered under the category of serious threats by the Centers for Disease Control and Prevention (CDC), urges for new antibiotics or alternate strategies to control MRSA. Methods: Ethosome-like liposomes have been developed and characterized using dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). Liposomes were confirmed for antibiotics infusion by encapsulation efficiency and release kinetics as well. Further, the antimicrobial potential of liposomes was checked by determination of minimum inhibitory concentrations (MICs), crystal violet assay, and live/dead biofilm eradication assay. Results: The specially designed liposomes consist of amphiphilic molecules, tocopherol, conjugated with ampicillin and, another antibiotic amikacin, loaded in the core. The developed liposomes exhibited good encapsulation efficiency, and sustained release while serving as ideal antibiotic carriers for advanced efficacy along with anti-inflammatory benefits from tocopherol. Conclusively, newly designed liposomes displayed potential antimicrobial activity against MRSA and its complex biofilms. Conclusions: Overall, dual antibiotic-encapsulated liposomes demonstrate the potential to eradicate MRSA and its mature biofilms by dual-targeted action. This could be developed as an efficient anti-infective agent and delivery vehicle for conventional antibiotics to combat MRSA. Full article