Search Results (56)

Background/Objectives: Ultraviolet B (UVB) radiation contributes significantly to skin aging and skin disorders by promoting oxidative stress, inflammation, and collagen degradation. Natural antioxidants such as theaflavins and thearubigins from Camellia sinensis L. (black tea) have shown photoprotective effects. This study aimed to optimize the extraction of theaflavins and thearubigins from black tea leaves and evaluate the efficacy of the extract against UVB-induced damage using a transfersome-based topical formulation. Methods: Extraction of theaflavins and thearubigins was optimized via response surface methodology (Box-Behnken Design), yielding an extract rich in active polyphenols. This extract was incorporated into transfersomes that were characterized for size, polydispersity, zeta potential, storage stability, and entrapment efficiency. Human dermal fibroblasts (NHDF) were used to assess cytotoxicity, protection against UVB-induced viability loss, collagen degradation, and expression of inflammatory (IL6, COX2, iNOS) and matrix-degrading (MMP1) markers. Cellular uptake of the extract’s bioactive marker compounds was measured via LC-MS/MS. Results: The transfersomes (~60 nm) showed a good stability and a high entrapment efficiency (>85%). The transfersomes significantly protected NHDF cells from UVB-induced cytotoxicity, restored collagen production, and reduced gene expression of MMP1, IL6, COX2, and iNOS. Cellular uptake of key extract’s polyphenols was markedly enhanced by the nanoformulation compared to the free extract. Conclusions: Black tea extract transfersomes effectively prevented UVB-induced oxidative and inflammatory damage in skin fibroblasts. This delivery system enhanced bioavailability of the extract and cellular protection, supporting the use of the optimized extract in cosmeceutical formulations targeting photoaging and UV-induced skin disorders. Full article

Background/Objectives: Although androgenic alopecia is the most prevalent among non-cicatricial alopecia, it still lacks an effective and safe treatment. Dutasteride (DUT) shows promising results in hair regrowth; however, oral DUT intake causes serious sexual adverse events. Hence, we produced liposomes with different bilayer structures and evaluated the capability of such systems in increasing DUT accumulation in the hair follicles. Methods: In vitro skin penetration tests were performed with porcine ear skin, and the follicular targeting factor (Tf) was calculated as the ratio between DUT amount in HFs and DUT recovered from the sum of all skin layers. Results: While the stiffer DUT-loaded liposome was not able to target the hair follicles in 12 h (Tf = 0.15), a DUT-loaded liposome with an edge activator in its composition, i.e., transfersomes, promoted better control over DUT release and a higher Tf (0.32) (p < 0.005). Conclusions: Transfersomes present higher affinity with DUT providing a better controlled release; hence, they are a better option for DUT follicle targeting compared to liposomes. Further formulation optimizations are needed aiming to prolong such targeting effect. Full article

Gallic acid (GA) is a well-known herbal bioactive compound found in many herbs and foods like tea, wine, cashew nuts, hazelnuts, walnuts, plums, grapes, mangoes, blackberries, blueberries, and strawberries. GA has been reported for several pharmacological activities, such as antioxidant, inflammatory, antineoplastic, antimicrobial, etc. Apart from its incredible therapeutic benefits, it has been associated with low permeability and bioavailability issues, limiting their efficacy. GA belongs to BCS (Biopharmaceutics classification system) class III (high solubility and low probability). In this context, novel drug delivery approaches played a vital role in resolving these GA issues. Nanocarrier systems help improve drug moiety’s physical and chemical stability by encapsulating them into a lipidic or polymeric matrix or core system. In this regard, researchers have developed a wide range of nanocarrier systems for GA, including liposomes, transfersomes, niosomes, dendrimers, phytosomes, micelles, nanoemulsions, metallic nanoparticles, solid lipid nanoparticles (SLNs), nanoparticles, nanostructured lipid carriers, polymer conjugates, etc. In the present review, different search engines like Scopus, PubMed, ScienceDirect, and Google Scholar have been referred to for acquiring recent information on the theme of the work. Therefore, this review paper aims to emphasize several novel drug delivery systems, patents, and clinical updates of GA. Full article

Melanoma is a malignant skin cancer associated with high mortality rates and drug resistance, posing a significant threat to human health. The combination of chemotherapy and photodynamic therapy (PDT) represents a promising strategy to enhance antitumor efficacy through synergistic anti-cancer effects. Topical delivery of chemotherapeutic drugs and photosensitizers (PS) offers a non-invasive and safe way to treat melanoma. However, the effectiveness of these treatments is often hindered by challenges such as limited skin permeability and instability of the PS. In this study, transfersomes (TFS) were designed to facilitate transdermal delivery of the chemotherapeutic drug 5-Fluorouracil (5-FU) and the PS Imperatorin (IMP) for combined chemo-photodynamic therapy for melanoma. The cytotoxic and phototoxic effects of TFS-mediated PDT (TFS-UVA) were investigated in A375 cells and nude mice. The study also demonstrated that TFS-UVA generated intracellular ROS, induced G2/ M phase cell cycle arrest, and promoted cell apoptosis. In conclusion, this study indicated that 5-FU/ IMP-TFS serves as an effective transdermal therapeutic strategy for chemo-PDT in treating melanoma. Full article

Ocular drug delivery poses unique challenges due to the complex anatomical and physiological barriers of the eye. Conventional dosage forms often fail to achieve optimal therapeutic outcomes due to poor bioavailability, short retention time, and off-target effects. In recent years, vesicular drug delivery systems have emerged as promising solutions to address these challenges. Vesicular systems, such as liposome, niosome, ethosome, transfersome, and others (bilosome, transethosome, cubosome, proniosome, chitosome, terpesome, phytosome, discome, and spanlastics), offer several advantages for ocular drug delivery. These include improved drug bioavailability, prolonged retention time on the ocular surface, reduced systemic side effects, and protection of drugs from enzymatic degradation and dilution by tears. Moreover, vesicular formulations can be engineered for targeted delivery to specific ocular tissues or cells, enhancing therapeutic efficacy while minimizing off-target effects. They also enable the encapsulation of a wide range of drug molecules, including hydrophilic, hydrophobic, and macromolecular drugs, and the possibility of combination therapy by facilitating the co-delivery of multiple drugs. This review examines vesicular drug delivery systems, their advantages over conventional drug delivery systems, production techniques, and their applications in management of ocular diseases. Full article

This review focuses on nanovesicular carriers for enhanced delivery of molecules into and across the skin, from their design to recent emerging technologies. During the last four decades, several approaches have been used aiming to design new nanovesicles, some of them by altering the properties of the classic phospholipid vesicle, the liposome. Phospholipid nanovesicular systems, including the phospholipid soft vesicles as well as the non-phospholipid vesicular carries, are reviewed. The altered nanovesicles have served in the manufacture of various cosmetic products and have been investigated and used for the treatment of a wide variety of skin conditions. The evolution and recent advances of these nanovesicular technologies are highlighted in this review. Full article

Transdermal drug delivery systems offer several advantages over conventional oral or hypodermic administration due to the avoidance of first-pass drug metabolism and gastrointestinal degradation as well as patients’ convenience due to a minimally invasive and painless approach. A novel transdermal drug delivery system, comprising a combination of transfersomes with either solid silicon or solid polycarbonate microneedles has been developed for the transdermal delivery of aspirin. Aspirin was encapsulated inside transfersomes using a “thin-film hydration sonication” technique, yielding an encapsulation efficiency of approximately 67.5%. The fabricated transfersomes have been optimised and fully characterised in terms of average size distribution and uniformity, surface charge and stability (shelf-life). Transdermal delivery, enhanced by microneedle penetration, allows the superior permeation of transfersomes into perforated porcine skin and has been extensively characterised using optical coherence tomography (OCT) and transmission electron microscopy (TEM). In vitro permeation studies revealed that transfersomes enhanced the permeability of aspirin by more than four times in comparison to the delivery of unencapsulated “free” aspirin. The microneedle-assisted delivery of transfersomes encapsulating aspirin yielded 13-fold and 10-fold increases in permeation using silicon and polycarbonate microneedles, respectively, in comparison with delivery using only transfersomes. The cytotoxicity of different dose regimens of transfersomes encapsulating aspirin showed that encapsulated aspirin became cytotoxic at concentrations of ≥100 μg/mL. The results presented demonstrate that the transfersomes could resolve the solubility issues of low-water-soluble drugs and enable their slow and controlled release. Microneedles enhance the delivery of transfersomes into deeper skin layers, providing a very effective system for the systemic delivery of drugs. This combined drug delivery system can potentially be utilised for numerous drug treatments. Full article

Urticaria is an autoimmune disease and many patients are suffering from it. This research aims to investigate the development and characterization of an Ebastine-loaded transfersomal nanogel for the enhancement of bioavailability in the treatment of urticaria. The flexible transfersomes, consisting of the drug Ebastine, soya lecithin, and edge activator Tween 80, were prepared using the thin-film hydration method. The transfersomal nanogel was formulated by using the dispersion method and a suitable concentration of the gelling agent Carbopol 934. The transfersomes and their gel were evaluated for various parameters. The Ebastine-loaded transfersomes showed the highest entrapment efficiency, up to 79.92%. The polydispersity index (PDI) of the transfersomes was determined to be 0.103, and the zeta potential was determined to be −18.9 mV, indicating that the formulation was stable. The drug content of the transfersome gel was found to be 83.67%. The transfersomal gel formed using 1% Carbopol 934 showed the best results, showing in vitro release for up to 8 h and following a zero-order kinetic model. As per the microbial studies conducted, the Ebastine transfersomal gel has a good anti-microbial effect against S. aureus. These vesicular transfersomes are more flexible than other vesicular systems, making them excellent for skin penetration. In the future, this will be the best possible approach for the delivery of drugs via the transdermal route. Full article

Psychiatric and neurodegenerative disorders are amongst the most prevalent and debilitating diseases, but current treatments either have low success rates, greatly due to the low permeability of the blood–brain barrier, and/or are connected to severe side effects. Hence, new strategies are extremely important, and here is where liposome-derived nanosystems come in. Niosomes, transfersomes, and ethosomes are nanometric vesicular structures that allow drug encapsulation, protecting them from degradation, and increasing their solubility, permeability, brain targeting, and bioavailability. This review highlighted the great potential of these nanosystems for the treatment of Alzheimer’s disease, Parkinson’s disease, schizophrenia, bipolar disorder, anxiety, and depression. Studies regarding the encapsulation of synthetic and natural-derived molecules in these systems, for intravenous, oral, transdermal, or intranasal administration, have led to an increased brain bioavailability when compared to conventional pharmaceutical forms. Moreover, the developed formulations proved to have neuroprotective, anti-inflammatory, and antioxidant effects, including brain neurotransmitter level restoration and brain oxidative status improvement, and improved locomotor activity or enhancement of recognition and working memories in animal models. Hence, albeit being relatively new technologies, niosomes, transfersomes, and ethosomes have already proven to increase the brain bioavailability of psychoactive drugs, leading to increased effectiveness and decreased side effects, showing promise as future therapeutics. Full article

Background: Phloretin (Phl) is a flavonoid compound that contains multiple phenolic hydroxyl groups. It is found in many plants, such as apple leaves, lychee pericarp, and begonia, and has various biological activities, such as antioxidant and anticancer effects. The strong hydrogen bonding between Phl molecules results in poor water solubility and low bioavailability, and thus the scope of the clinical application of Phl is limited. Therefore, it is particularly important to improve the water solubility of Phl for its use to further combat or alleviate skin aging and oxidative damage and develop antioxidant products for the skin. The purpose of this study was to develop and evaluate a phloretin transfersome gel (PTG) preparation for transdermal drug delivery to improve the bioavailability of the drug and delay aging. Methods: Phloretin transfersomes (Phl-TFs) were prepared and optimized by the thin-film dispersion–ultrasonication method. Phl-TFs were characterized by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD). The Log P method was used to determine the solubility of the Phl-TFs. The skin penetration ability of the prepared PTG was evaluated using the Franz diffusion cell method. In addition, the in vivo pharmacokinetics of PTG were studied in rats, and an antioxidant activity investigation was conducted using a D-gal rat model. Results: Phl-TFs were successfully prepared with a Soybean Phosphatidylcholine (SPC)/CHOL ratio of 2.7:1 w/v, a phloretin concentration of 1.3 mg/mL, a hydration time of 46 min, an ultrasound time of 5 min, and an ultrasound power of 180 W. The Log P was 2.26, which was significantly higher than that of phloretin (p < 0.05, paired t test). The results of the in vitro penetration test demonstrated that the cumulative skin penetration of the Phl-TFs after 24 h was 842.73 ± 20.86 μg/cm². The data from an in vivo pharmacokinetic study showed that the C_max and AUC of PTG were 1.39- and 1.97-fold higher than those of the phloretin solution gel (PSG), respectively (p < 0.05, paired t test). The experimental results in aging rats showed that PTG had a better antioxidant effect. Conclusions: Phl-TFs and PTG preparations with a good shape, safety, and stability were successfully prepared. In vivo pharmacokinetics and preliminary antioxidant experiments further verified the transdermal penetration and antioxidant activity of the phloretin transdermal drug delivery preparation, providing an experimental basis for its further development. Full article

The purpose of this study was to evaluate L-cysteine-modified transfersomes as the topical carrier for enhanced epidermal delivery of podophyllotoxin (POD). L-cysteine-deoxycholic acid (LC-DCA) conjugate was synthesized via an amidation reaction. POD-loaded L-cysteine-modified transfersomes (POD-LCTs) were prepared via a thin membrane dispersion method and characterized for their particle size, zeta potential, morphology, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and in vitro release. Subsequently, in vitro skin permeation and retention, fluorescence distribution in the skin, hematoxylin–eosin staining and in vivo skin irritation were studied. The POD-LCTs formed spherical shapes with a particle size of 172.5 ± 67.2 nm and a zeta potential of −31.3 ± 6.7 mV. Compared with the POD-Ts, the POD-LCTs provided significantly lower drug penetration through the porcine ear skin and significantly increased the skin retention (p < 0.05). Meaningfully, unlike the extensive distribution of the POD-loaded transfersomes (POD-Ts) throughout the skin tissue, the POD-LCTs were mainly located in the epidermis. Moreover, the POD-LCTs did not induce skin irritation. Therefore, the POD-LCTs provided an enhanced epidermal delivery and might be a promising carrier for the topical delivery of POD. Full article

Raman spectroscopy was used to detect low quantities of Vismodegib in the skin after its topical application via transfersomes. Vismodegib is a novel antineoplastic drug approved for oral administration for treatment of basal cell carcinoma. Transfersomes loaded with Vismodegib were prepared by thin film resuspension and extrusion, and were characterized physicochemically. Transfersomes were applied to human and pig skin specimens using the Saarbrücken penetration model. The skin was then sectioned by tape stripping, followed by penetration assessment by UV-Vis spectroscopy and Raman spectroscopy in a confocal Raman microscope. Raman signals from Vismodegib and transfersomes were recovered from skin sections, showing a similar distribution in the stratum corneum obtained by the other techniques. On the other hand, pig and human skin showed differences in their penetration profiles, proving their lack of equivalence for assessing the performance of these transfersomes. Raman spectroscopy appears as a potential non-invasive, direct tool for monitoring hard-to-detect molecules in a complex environment such as the skin. Full article

In this study, elastic nanovesicles, constructed of phospholipids optimized by Quality by Design (QbD), release 6-gingerol (6-G), a natural chemical that may alleviate osteoporosis and musculoskeletal-related pain. A 6-gingerol-loaded transfersome (6-GTF) formulation was developed using a thin film and sonication approach. 6-GTFs were optimized using BBD. Vesicle size, PDI, zeta potential, TEM, in vitro drug release, and antioxidant activity were evaluated for the 6-GTF formulation. The optimized 6-GTF formulation had a 160.42 nm vesicle size, a 0.259 PDI, and a −32.12 mV zeta potential. TEM showed sphericity. The 6-GTF formulation’s in vitro drug release was 69.21%, compared to 47.71% for the pure drug suspension. The Higuchi model best described 6-G release from transfersomes, while the Korsmeyer–Peppas model supported non-Fickian diffusion. 6-GTF had more antioxidant activity than the pure 6-G suspension. The optimized transfersome formulation was converted into a gel to improve skin retention and efficacy. The optimized gel had a spreadability of 13.46 ± 4.42 g·cm/s and an extrudability of 15.19 ± 2.01 g/cm². The suspension gel had a 1.5 μg/cm²/h ex vivo skin penetration flux, while the 6-GTF gel had 2.71 μg/cm²/h. Rhodamine B-loaded TF gel reached deeper skin layers (25 μm) compared to the control solution in the CLSM study. The gel formulation’s pH, drug concentration, and texture were assessed. This study developed QbD-optimized 6-gingerol-loaded transfersomes. 6-GTF gel improved skin absorption, drug release, and antioxidant activity. These results show that the 6-GTF gel formulation has the ability to treat pain-related illnesses effectively. Hence, this study offers a possible topical treatment for conditions connected to pain. Full article

Transfersomes are deformable vesicles that can transport drugs across difficult-to-permeate barriers in human tissues. In this work, nano-transfersomes were produced for the first time by a supercritical CO₂ assisted process. Operating at 100 bar and 40 °C, different amounts of phosphatidylcholine (2000 and 3000 mg), kinds of edge activators (Span^® 80 and Tween^® 80), and phosphatidylcholine to edge activator weight ratio (95:5, 90:10, 80:20) were tested. Formulations prepared using Span^® 80 and phosphatidylcholine at an 80:20 weight ratio produced stable transfersomes (−30.4 ± 2.4 mV ζ-potential) that were characterized by a mean diameter of 138 ± 55 nm. A prolonged ascorbic acid release of up to 5 h was recorded when the largest amount of phosphatidylcholine (3000 mg) was used. Moreover, a 96% ascorbic acid encapsulation efficiency and a quasi-100% DPPH radical scavenging activity of transfersomes were measured after supercritical processing. Full article

Several studies have demonstrated the effectiveness of plant extracts against various diseases, especially skin disorders; namely, they exhibit overall protective effects. The Pistachio (Pistacia vera L.) is known for having bioactive compounds that can effectively contribute to a person’s healthy status. However, these benefits may be limited by the toxicity and low bioavailability often inherent in bioactive compounds. To overcome these problems, delivery systems, such as phospholipid vesicles, can be employed. In this study, an essential oil and a hydrolate were produced from P. vera stalks, which are usually discarded as waste. The extracts were characterized by liquid and gas chromatography coupled with mass spectrometry and formulated in phospholipid vesicles intended for skin application. Liposomes and transfersomes showed small size (<100 nm), negative charge (approximately −15 mV), and a longer storage stability for the latter. The entrapment efficiency was determined via the quantification of the major compounds identified in the extracts and was >80%. The immune-modulating activity of the extracts was assayed in macrophage cell cultures. Most interestingly, the formulation in transfersomes abolished the cytotoxicity of the essential oil while increasing its ability to inhibit inflammatory mediators via the immunometabolic citrate pathway. Full article