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Miconazole nitrate (MN), an antifungal drug with poor solubility, is used in the treatment of vaginal candidiasis. Conventional vaginal formulations have lower residence time and poor drug penetration resulting in the recurrence of the infection. Hence, transfersomes were formulated that would alleviate fungal infection by improving drug solubility and allowing effective permeation through the vaginal mucus and epithelium. MN-loaded transfersomes (MN-TF) were prepared by the thin film method. The optimization of the MN-TF was done by using 32 full factorial design. The Lipoid S100® and Tween 80® were selected as the phospholipid and edge activator, respectively. The responses, such as particle size, PDI, and entrapment efficiency were studied and found to be 180.70±2.11 nm, 0.293±0.012, and −13.2±1.3 mV, respectively. The optimized MN-TF was incorporated into the thermosensitive gel. The morphological study through TEM confirmed the nano size of the formulation. The FTIR study showed compatibility between the drug and excipients. The microbiological screening was performed against Candida albicans which showed a higher zone of inhibition for MN-TF than the marketed gel. The ex vivo transvaginal permeation study was done for MN-TF gel and compared with the marketed gel Daktarin®. The permeability of the MN-TF was increased by 5.8-folds as compared to the marketed gel. The HET-CAM assay for the MN-TF gel demonstrated no irritation and hence was nontoxic and safe for vaginal administration. Therefore, the MN-TF gel had sustained drug release. [ABSTRACT FROM AUTHOR]

Skin melanoma is considered the most dangerous form of skin cancer due to its association with high risk of metastasis, high mortality rate and high resistance to different treatment options. Genistein is a natural isoflavonoid with known chemotherapeutic activity. Unfortunately, it has low bioavailability due to its poor aqueous solubility and excessive metabolism. In the current study, genistein was incorporated into transferosomal hydrogel to improve its bioavailability. The prepared transferosomal formulations were characterized regarding: particle size; polydispersity index; zeta potential; encapsulation efficiency; TEM; FTIR; DSC; XRD; in vitro drug release; viscosity; pH; ex vivo anti-tumor activity on 3D skin melanoma spheroids and 1-year stability study at different storage temperatures. The optimized formulation has high encapsulation efficiency with an excellent particle size that will facilitate its penetration through the skin. The transfersomes have a spherical shape with sustained drug release profile. The anti-tumor activity evaluation of genistein transfersome revealed that genistein is a potent chemotherapeutic agent with enhanced penetration ability through the melanoma spheroids when incorporated into transfersomes. Stability study results demonstrate the high physical and chemical stability of our formulations. All these outcomes provide evidence that our genistein transferosomal hydrogel is a promising treatment option for skin melanoma. [ABSTRACT FROM AUTHOR]

Salmon calcitonin (sCT) is a peptide hormone primarily used for osteoporosis due to the ability to regulate calcium and bone metabolism. However, its therapeutic efficacy through conventional routes of administration such as injection is limited by poor bioavailability, rapid degradation, and its invasive nature. Transdermal delivery systems, such as transfersome gels, offer a promising alternative by enhancing absorption through the skin. Therefore, this study aimed to evaluate the relative bioavailability and pharmacodynamic effects of transdermally administered sCT transfersomes gel in female rats. Pharmacokinetic tests of the transfersomes gel containing sCT were conducted on female Sprague-Dawley rats. A total of 10 rats were divided into 2 groups (n = 5 each) and received a single dose of sCT (4 µg/200 g). Group 1 was treated with transdermally administered transfersomes gel, and Group 2 received subcutaneously administered injection solution. As sCT concentration versus time was calculated, area under the curve (AUC) was determined. The pharmacodynamic analysis was conducted by counting the number of osteoclasts using TRAP staining and analyzing calcium levels in rats' tibia bone using Atomic Absorption Spectroscopy (AAS). In the pharmacokinetic test of transdermally administered sCT transfersomes gel, there was an increase in relative bioavailability by 144.32% compared to the subcutaneously administered injection solution. The results of pharmacodynamic analysis showed that sCT transfersomes gel increased calcium levels in rat tibia bone and reduced the number of osteoclasts in ovariectomized (Ovx) samples. This showed that sCT transfersomes gel could improve the relative bioavailability and prevent osteoporosis in Ovx rats. [ABSTRACT FROM AUTHOR]

Fungal infections present significant clinical challenges due to their diverse types and the increasing incidence of drug-resistant strains. Traditional antifungal treatments often encounter issues with penetration, efficacy and patient compliance. The study involves a comprehensive review of the structure and mechanism of transfersomes, their advantages over conventional and other nano carriers, and the integration of herbal extracts. Key aspects include improved skin penetration, enhanced bioavailability of herbal actives, and targeted delivery to infected areas. Transfersomes demonstrate significant benefits in antifungal therapy, including higher efficacy, faster symptom relief, reduced side effects and improved patient compliance. The enhanced penetration and stability of transfersomes facilitate a more effective delivery of herbal actives, making them a superior choice for topical treatments. The study also identifies areas for future research, such as optimizing formulation processes and exploring combination therapies to maximize therapeutic outcomes. Transfersomes represent a transformative advancement in the field of topical drug delivery. Their integration with herbal medicines offers a promising approach to addressing fungal infections more effectively. Future research should focus on clinical validation and further refinement of transfersome-based formulations to fully realize their potential in enhancing the management of fungal infections and other dermatological conditions. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Alzheimer's disease is the most serious neurodegenerative disorder characterized by cognitive and memorial defects alongside deterioration in behavioral, thinking and social skills. Donepezil hydrochloride (DPZ) is one of the current two FDA-approved cholinesterase inhibitors used for the management of Alzheimer's disease. The current study aimed to formulate hyaluronic acid-coated transfersomes containing DPZ (DPZ-HA-TFS) for brain delivery through the intranasal pathway to surpass its oral-correlated GIT side effects. DPZ-HA-TFS were produced using a thin film hydration method and optimized with a 24 factorial design. The influence of formulation parameters on vesicle diameter, entrapment, cumulative release after 8 h, and ex vivo nasal diffusion after 24 h was studied. The optimal formulation was then evaluated for morphology, stability, histopathology and in vivo biodistribution studies. The optimized DPZ-HA-TFS formulation elicited an acceptable vesicle size (227.5 nm) with 75.83% entrapment efficiency, 37.94% cumulative release after 8 h, 547.49 µg/cm2 permeated through nasal mucosa after 24 h and adequate stability. Histopathological analysis revealed that the formulated DPZ-HA-TFS was nontoxic and tolerable for intranasal delivery. Intranasally administered DPZ-HA-TFS manifested significantly superior values for drug targeting index (5.08), drug targeting efficiency (508.25%) and direct nose-to-brain transport percentage (80.32%). DPZ-HA-TFS might be deemed as a promising intranasal nano-cargo for DPZ cerebral delivery to tackle Alzheimer's disease safely, steadily and in a non-invasive long-term pattern. [ABSTRACT FROM AUTHOR]

Melanin is considered the main chromophore for laser hair removal. Due to a lack of laser-absorbing chromophores, removing non-pigmented hair with laser is quite problematic with unsatisfactory outcomes. This problem could be solved by delivering more melanin to the area around the hair follicle and enhancing that area as a target for light absorption. The insolubility of Sepia melanin as an exogenous dye, in most solvents, limits its bioavailability and thus its clinical use. In our study, to overcome the solubility problems and increase the bioavailability of melanin for biomedical and cosmetic applications, natural sepia melanin was loaded in different nano-delivery systems (spanlastics and transfersomes) to be delivered to the hair follicles. The different formulations of melanin were prepared and characterized. In vivo skin deposition and histopathological studies were conducted on albino mice. Transmission electron microscopy (TEM) showed the spherical shape of the prepared vesicles with an average particle size of 252 and 262 nm and zeta potential of −22.5 and −35 mV for melanin spanlastics and melanin transfersomes, respectively. Histopathological examination of hair follicles and pilosebaceous glands for the irradiated and non-irradiated albino mice skin was studied post the application of the prepared formulations topically and subcutaneously. Qualitative statistical analysis was conducted and melanin transfersomes and melanin spanlastics showed significant damage to pilosebaceous glands and hair follicles with a p-value of 0.031 and 0.009 respectively. Melanin nanovesicles as transfersomes and spanlastics could be considered a promising approach for the removal of non-pigmented hair. [ABSTRACT FROM AUTHOR]

Abstract One of the most effective strategies to fight viruses and handle health diseases is vaccination. Recent studies and current applications are moving on antigen, DNA and RNA-based vaccines to overcome the limitations related to the conventional vaccination strategies, such as low safety, necessity of multiple injection, and side effects. However, due to the instability of pristine antigen, RNA and DNA molecules, the use of nanocarriers is required. Among the different nanocarriers proposed for vaccinal applications, three types of nanovesicles were selected and analysed in this review: liposomes, transfersomes and niosomes. PubMed, Scopus and Google Scholar databases were used for searching recent papers on the most frequently used conventional and innovative methods of production of these nanovesicles. Weaknesses and limitations of conventional methods (i.e., multiple post-processing, solvent residue, batch-mode processes) can be overcome using innovative methods, in particular, the ones assisted by supercritical carbon dioxide. SuperSomes process emerged as a promising production technique of solvent-free nanovesicles, since it can be easily scaled-up, works in continuous-mode, and does not require further post-processing steps to obtain the desired products. As a result of the literature analysis, supercritical carbon dioxide assisted methods attracted a lot of interest for nanovesicles production in the vaccinal field. However, despite their numerous advantages, supercritical processes require further studies for the production of liposomes, transfersomes and niosomes with the aim of reaching well-defined technologies suitable for industrial applications and mass production of vaccines.

Fungal infections are of major concern all over the globe, and fluconazole is the most prevalently used drug to treat it. The goal of this research work was to formulate a fluconazole-embedded transfersomal gel for the treatment of fungal infections. A compatibility study between fluconazole and soya lecithin was performed by differential scanning calorimetry (DSC). Transfersomes were formulated by a thin-film hydration technique using soya lecithin and Span 80. A central composite design was adopted to prepare different formulations. Soya lecithin and Span 80 were chosen as independent variables, and the effect of these variables was studied on in vitro drug diffusion. Formulations were evaluated for entrapment efficiency and in vitro drug diffusion. The results of in vitro drug diffusion were analyzed using the analysis of variance (ANOVA) test. Optimized formulation was prepared based on the overlay plot and evaluated by scanning electron microscopy, DSC, vesicle size, polydispersity index (PDI), zeta potential, and in vitro drug diffusion studies. An optimized formulation was loaded into xanthan gum gel base and evaluated for pH, viscosity, in vitro and ex vivo drug diffusion, and antifungal activity. DSC studies revealed compatibility between fluconazole and soya lecithin. Entrapment efficiency and in vitro drug diffusion of various formulations ranged between 89.92% ± 0.20% to 97.28% ± 0.42% and 64% ± 1.56% to 85% ± 2.05%, respectively. A positive correlation was observed between in vitro drug diffusion and Span 80; conversely, a negative correlation was noted with soya lecithin. Entrapment efficiency, particle size, zeta potential, PDI, and drug diffusion of optimized formulation were 95.0% ± 2.2%, 397 ± 2 nm,-38 ± 5 mV, 0.43%, and 81 % ± 2%, respectively. SEM images showed well-distributed spherical-shaped transfersomes. In vitro, ex vivo drug diffusion and antifungal studies were conclusive of better diffusion and enhanced antifungal potential fluconazole in transfersomal formulation. [ABSTRACT FROM AUTHOR]

One of the most effective strategies to fight viruses and handle health diseases is vaccination. Recent studies and current applications are moving on antigen, DNA and RNA-based vaccines to overcome the limitations related to the conventional vaccination strategies, such as low safety, necessity of multiple injection, and side effects. However, due to the instability of pristine antigen, RNA and DNA molecules, the use of nanocarriers is required. Among the different nanocarriers proposed for vaccinal applications, three types of nanovesicles were selected and analysed in this review: liposomes, transfersomes and niosomes. PubMed, Scopus and Google Scholar databases were used for searching recent papers on the most frequently used conventional and innovative methods of production of these nanovesicles. Weaknesses and limitations of conventional methods (i.e., multiple post-processing, solvent residue, batch-mode processes) can be overcome using innovative methods, in particular, the ones assisted by supercritical carbon dioxide. SuperSomes process emerged as a promising production technique of solvent-free nanovesicles, since it can be easily scaled-up, works in continuous-mode, and does not require further post-processing steps to obtain the desired products. As a result of the literature analysis, supercritical carbon dioxide assisted methods attracted a lot of interest for nanovesicles production in the vaccinal field. However, despite their numerous advantages, supercritical processes require further studies for the production of liposomes, transfersomes and niosomes with the aim of reaching well-defined technologies suitable for industrial applications and mass production of vaccines. [ABSTRACT FROM AUTHOR]

Background and Objectives: Doxorubicin hydrochloride (DOX-HCl), a potent and extensively utilized anticancer medication, faces limitations in skin penetration, resulting in confined effectiveness. Frequent administration leads to resistance at the site of application. This study aims to strike a balance between precision and selectivity to enhance DOX-HCl's permeation. The goal is to achieve non-invasive drug delivery that avoids issues linked with conventional therapies. This will be achieved through the utilization of patches loaded with transfersomes for drug delivery. Materials and Methods: Transferosomes were prepared through the rotary evaporation technique and optimized by Box-Behnken experimental design. The impact of phospholipid, cholesterol, and tween-80 on drug entrapment efficiency and particle size was assessed using analysis of variance. The resulting formulations underwent characterization involving particle size, zeta potential, transmission electron microscopy, and Fourier-transform infrared spectroscopy. In addition, drug entrapment efficiency, in vitro drug release patterns, ex vivo drug permeation profiles, and histopathological evaluations of the optimized formulations were conducted. Results: The particle size ranged from 53 to 168 nm, with drug entrapment efficiency ranging from 30.8 ± 0.06 to 87.90 ± 0.02%. The optimum formulation exhibited a zeta potential of -24.9 mV and achieved an approximately fourfold increase in permeation rate compared to a pure drug suspension. Histopathological studies of rat abdominal skin samples post-treatment with transferosomes patch indicate a moderate epidermal inflammation versus normal morphology for untreated skin. Conclusion: Utilizing transferosomes in transdermal drug delivery systems (TDDS) presents a promising strategy to address challenges associated with conventional therapies. By incorporating transferosomes into patches, this approach offers a multi-faceted solution to enhance non-invasive drug delivery. [ABSTRACT FROM AUTHOR]

Transdermal drug delivery has gained significant attention as a non-invasive and convenient method for administering drugs. However, the stratum corneum, the outermost layer of the skin, poses a significant barrier to drug permeation. To overcome this challenge, vesicular carriers have emerged as promising systems for enhancing drug delivery through the skin. This review highlights recent advances in the development of vesicular carriers for transdermal drug delivery. Liposomes, niosomes, transfersomes, ethosomes, and solid lipid nanoparticles are among the commonly used vesicular carriers. These carriers offer advantages such as improved drug solubility, prolonged drug release, and enhanced drug stability. Additionally, they can encapsulate a wide range of drugs, including hydrophilic and lipophilic compounds. Various strategies have been employed to optimize vesicular carriers for transdermal drug delivery. These include modifying the vesicle composition, size, and surface charge to enhance skin penetration. The incorporation of penetration enhancers, such as surfactants, has also been explored to improve drug permeation across the skin. Furthermore, advancements in nanotechnology have led to the development of novel vesicular carriers, such as nanostructured lipid carriers and elastic liposomes. These carriers offer improved drug loading capacity, sustained release profiles, and enhanced skin penetration. Moreover, the use of vesicular carriers has shown promise in delivering a wide range of therapeutic agents, including small molecules, peptides, proteins, and genetic material. The ability to encapsulate and deliver these diverse drug entities opens new possibilities for transdermal drug delivery in various therapeutic areas. [ABSTRACT FROM AUTHOR]

This study investigates the encapsulation of bakuchiol, a renowned compound for hyperpigmentation treatment, utilizing transfersomes as a delivery system. The transfersomes were fabricated using the thin-film hydration technique and subjected to thorough characterization across various parameters. The resulting transfersome formulation, after optimization, demonstrated notably high encapsulation efficiencies, with bakuchiol registering at 86.7±3.6%, accompanied by a narrow particle size distribution (179.9 ± 5.4 nm). In vitro release studies unveiled cumulative release percentages of 71.98±6.52% for bakuchiol over a 24-hour period. Ex vivo permeation studies further affirmed heightened retention of bakuchiol within the skin layers compared to control group. Stability assessments indicated that the optimized transfersome remained stable at 5°C for at least 90 days. These findings underscore the remarkable potential of transfersomes in facilitating the delivery of bakuchiol, offering a compelling and viable alternative for hyperpigmentation formulations. [ABSTRACT FROM AUTHOR]

Photoaging of skin tissue can result from exposure to ultraviolet B (UVB) radiation. This study developed two nanocarriers Centella asiatica (CA) transfersomes (TF) and Bergamot essential oil (BEO) nanoemulsions (NE) combined in a gel formulation as a drug delivery system, in order to study whether they could synergize to prevent UVB radiation and provide anti-photoaging effects. Nanoencapsulation of CA-TF and BEO-NE were examined for their quality by characterizing their physicochemical properties. An in vivo study evaluated topically applied CA-TF and BEO-NE combination gels biological effect on BALB/c mice before UVB radiation (840 mJ/cm2) for two weeks. Particle size analysis of developed nanocarriers exhibited monodispersed pattern with an average particle size and zeta potential of around 9.64 ± 0.35 nm and −39.86 ± 1.33 mV, respectively. In vivo experiments showed that topically applied CA-TF and BEO-NE combination gel significantly prevented UVB-induced wrinkle formation and skin erythema and inhibited histological damage, including epidermal hyperplasia, collagen fibers, and the destruction of elastic fibers. Additionally, the CA-TF and BEO-NE combination gel reduced UVB-induced oxidative stress by increasing superoxide dismutase (SOD) activity and suppressed lipid peroxidation by decreasing malondialdehyde (MDA) expression as well as inhibiting the expression of UVB-induced pro-inflammatory cytokines include tumor necrosis factor α (TNF-α) and interleukin 6 (IL-6). Moreover, the CA-TF and BEO-NE combination gel increased the type I collagen expression, restoring UVB-induced collagen production and density. Therefore, nanoencapsulation CA-TF and BEO-NE combination gel could synergistically prevent UVB-induced oxidative stress and inflammatory responses.

The melanoma is the most dangerous kind of skin cancer begins in the melanocytes, or cells that make melanin, the pigment that gives your skin its color. Due to the need of local effect topical administration of anticancer drugs could be the best option for clinical therapy. Present study aimed to formulate transfersomes to enhance the skin penetration of rutin (Rtn). Rutin loaded transfersomes (RtnTFs) were formulated by employing central composite design (CCD) of experiment and comprising of various ratios of phospholipid 90H and sodium deoxycholate as independent variables. The assessment of critical parameters suggested higher encapsulation of Rtn and improved stability of formulation with significant drug release (P

Transdermal administration techniques have gained popularity due to their advantages over oral and parenteral methods. Noninvasive, self-administered delivery devices improve patient compliance and control drug release. Transdermal delivery devices struggle with the skin's barrier function. Molecules over 500 Da and ionized compounds don't pass through skin. Few medications can be given this way. Encapsulating pharmaceuticals in transfersomes is one solution. Bilayered liposomes encapsulate lipophilic, hydrophilic, and amphiphilic drugs with better penetration efficiencies than standard liposomes. Transfersomes are elastic in nature, allowing them to flex and squeeze through pores substantially smaller than their size while remaining whole. This article describes the concept of transfersomes, their mode of action, several techniques of manufacture and characterization, and factors influencing their properties, as well as their latest applications in the transdermal administration of pharmaceuticals. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Copyright of Al-Mustansiriyah Journal for Pharmaceutical Sciences is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Rheumatoid arthritis restricts the physical ability of patients and increases the disease burden; therefore, research has always been focused on evaluating better therapeutic options. The present research aimed to design Continentalic acid (CA)–loaded transfersomes (CA-TF) embedded in Carbopol gel containing permeation enhancer (PE) for the treatment of rheumatoid arthritis. CA-TF was developed via a modified thin film hydration method and incorporated into Carbopol 934 gel containing Eucalyptus oil (EO) as PE. The fabricated CA-TF showed particle size of < 140 nm with spherical geometry, optimal encapsulation efficiency (EE), and sustained drug release pattern. CA-TF-gel along with PE (CA-TF-PE-gel) showed better ex vivo skin penetration than plain CA gel and CA-TF-gel without PE. In vivo evaluation supported improved therapeutic outcomes of CA-TF-PE-gel in terms of behavioral findings, arthritic index, and histological findings whereas biochemical assays and pro-inflammatory cytokines (TNF-α and IL-1β) showed a significant decrease in their levels. Furthermore, immunohistochemistry assay for Nrf2 and HO-1 signaling pathways showed significant improvement in the expression of the Nrf2, and HO-1 proteins to depict improvement in arthritic condition in the animal model. CA-TF-PE-gel significantly delivered CA to the diseased target site via a topical route with promising therapeutic outcomes displayed in the CFA-induced arthritic model. [ABSTRACT FROM AUTHOR]

In this work, a propranolol hydrochloride (PRH) transfersomes loaded cutaneous hydrogel patch was developed for topical drug delivery in the affected area of infantile haemangioma. Sodium cholate was used as the edge activator to prepare the transfersomes. Based on the central composite design, transfersomes hydrogel patch formulation was optimised with 48 h cumulative penetration and time lag as response values. Particle sizes and morphology of the prepared transfersomes were assessed. They were loaded in a cutaneous hydrogel patch, after which their skin permeation abilities were evaluated, and histopathological effects were investigated using guinea pigs. Moreover, in vivo pharmacokinetics studies were performed in rats. The transfersomes system had a encapsulation efficiency of 81.84 ± 0.53%, particle size of 186.8 ± 3.38 nm, polydispersity index of 0.186 ± 0.002, and a zeta potential of −28.6 ± 2.39 mV. Transmission electron microscopy images revealed sphericity of the particles. The ex vivo drug's penetration of the optimised transfersomes hydrogel patch was 111.05 ± 11.97 μg/cm2 through rat skin within 48 h. Assessment of skin tissue did not reveal any histopathological alterations in epidermal and dermal cells. Pharmacokinetic studies showed that skin Cmax (68.22 μg/cm2) and AUC0–24 (1007.33 μg/cm2 × h) for PRH transfersomes hydrogel patch were significantly higher than those of commercially available oral dosage form and hydrogel patch without transfersomes. These findings imply that the transfersomes hydrogel patch can prolong drug accumulation in the affected skin area, and reduce systemic drug distribution via the blood stream. The hydrogel patch-loaded PRH transfersomes is a potentially useful drug formulation for infantile haemangioma. [ABSTRACT FROM AUTHOR]

AbstractTransfersome has been developed to enhance dermal delivery of amniotic mesenchymal stem cell metabolite products (AMSC-MP). AMSC-MP contains many growth factors for managing skin aging, thus improving the quality of an adjusted life year. This study aims to determine the effect of surfactant types acting as the edge activator on transfersome-loading AMSC-MP. Transfersome was prepared by thin-layer hydration method and composed of l-α-phosphatidylcholine as a phospholipid and three types of surfactants, namely; cationic (stearylamine), anionic (sodium cholate), and nonionic surfactant (Tween 80) at a weight ratio of 85:15, respectively. Transfersomes were evaluated for physical characteristics, penetration, effectiveness, and safety. The results showed that sodium cholate, an anionic surfactant, produced the smallest transfersome particle size, i.e., 144.2 ± 3.2 nm, among all formulas. Trans-SA containing stearylamine had a positive charge of 41.53 ± 6.03 mV compared to Trans-SC and Trans-TW, whose respective charges were –56.9 ± 0.55 mV and –41.73 ± 0.86 mV. The small particle size and low negative value of zeta potential enabled high dermal penetration by transfersomes containing AMSC-MP, while the positive charge of stearylamine hindered its penetration of deeper skin layers. Trans-SC and Trans-TW produced higher collagen density values at 77.11 ± of 4.15% and 70.05 ± of 6.95%, than that of Trans-SA. All the AMSC-MP transfersomes were relatively safe with 0.5–1.0 macrophage cell numbers invaded the dermis per field of view. In conclusion, sodium cholate, an anionic surfactant, demonstrated considerable capacity as the edge activator of transfersome-loading AMSC-MP for skin anti-aging therapy.

Transdermal delivery systems have gained popularity as a non-invasive method of drug administration that offers several advantages over other routes of drug delivery. They are noninvasive and self-administered delivery system which improves patient compliance and provide a controlled release of the drug. The greatest challenge of transdermal delivery systems is that in which the outermost layer of skin acts as a barrier function for transfer of therapeutic agent into the body. Molecules with high molecular weights do not pass through the skin. Therefore, only a limited number of drugs are administered by this route. So encapsulating the drugs in transfersomes is one of the best approaches to overcome this problem. Transferosomes are lipid based vesicular drug delivery systems which have a unique composition that allows them to overcome the limitation of conventional drug delivery system. They are composed of phospholipids and surfactants, which provide them with the ability to encapsulate both hydrophilic and hydrophobic drugs. They penetrate through stratum corneum by either intracellular route or the transcellular route by the generation of natural osmotic gradient. Compared to conventional drug delivery systems, transferosomes offer several advantages like avoidance of first pass metabolism, increasing bioavailability of drugs. Due to its high deformability it enhances the penetration of intact vesicles. Transferosomes vary from other conventional vesicles due to their softer, better adjustable and ultra deformable artificial membranes. This review summarizes the concept of transfersomes, including their structure, formation mechanism of action, different methods of preparation, advantages, limitations along with applications. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Purpose: The present study aimed to develop, statistically optimize, and characterize hydroquinone-loaded transfersomes (HQ-TFs) for effective topical delivery by mitigating the problems associated with HQ. Methods: HQ-TFs were prepared by the thin-film hydration method and characterized for particle size, zeta potential (ZP), entrapment efficiency (EE), in vitro drug release, and skin penetration potential. The optimized hydroquinone-loaded transfersome (OPT-HQ-TF) was incorporated in a gel and evaluated for ex vivo skin permeation and deposition profile, in vitro antioxidant activity, in vitro cytotoxicity study, in vitro tyrosinase inhibition assay, and dermal skin irritation study. Results: The OPT-HQ-TF showed a particle size of 210 nm, ZP of − 15.10 mV, and EE% of 67.61. The cumulative drug release % from transfersomal formulations ranged from 54.39 ± 1.92 to 76.05 ± 1.18%. The fluorescence microscopy investigation revealed the penetration of transfersomes into deeper skin layers. The skin permeation and deposition studies indicated that the OPT-HQ-TF gel improved permeation and drug retention in the skin compared to the HQ plain gel. The antioxidant assay revealed that HQ retained its antioxidant activity after encapsulation. The cytotoxicity study demonstrated that the OPT-HQ-TF gel significantly decreased the cytotoxicity towards L-929 mouse fibroblast. The tyrosinase inhibition assay specified that the OPT-HQ-TF gel has the potential to treat hyperpigmentation. The dermal skin irritation study indicated that the OPT-HQ-TF gel is safe and non-irritant. Conclusion: The present study findings suggested the potential application of deformable nanovesicles as an innovative topical drug delivery system of HQ in the treatment of hyperpigmentation. [ABSTRACT FROM AUTHOR]

Transfersomes have been highlighted as an interesting nanotechnology-based approach to facilitate the skin delivery of bioactive compounds. Nevertheless, the properties of these nanosystems still need to be improved to enable knowledge transfer to the pharmaceutical industry and the development of more efficacious topical medicines. Quality-by-design strategies, such as Box–Behnken factorial design (BBD), are in line with the current need to use sustainable processes to develop new formulations. Thus, this work aimed at optimizing the physicochemical properties of transfersomes for cutaneous applications, by applying a BBD strategy to incorporate mixed edge activators with opposing hydrophilic–lipophilic balance (HLB). Tween® 80 and Span® 80 were used as edge activators and ibuprofen sodium salt (IBU) was selected as the model drug. After the initial screening of the IBU solubility in aqueous media, a BBD protocol was implemented, and the optimized formulation displayed appropriate physicochemical properties for skin delivery. By comparing the optimized transfersomes to equivalent liposomes, the incorporation of mixed edge activators was found to be beneficial to upgrade the storage stability of the nanosystems. Furthermore, their cytocompatibility was shown by cell viability studies using 3D HaCaT cultures. Altogether, the data herein bode well for future advances in the use of mixed edge activators in transfersomes for the management of skin conditions. [ABSTRACT FROM AUTHOR]

The aim of this study was to develop paroxetine (PXT) loaded nanotransferosomal gel (PXT-NTFG) for intranasal brain delivery. The process involved fabricating PXT-NTFs (paroxetine-loaded nanotransferosomes) through a thin film hydration method and optimizing them based on parameters such as particle size (PS), zeta potential (ZP), polydispersity index (PDI), and entrapment efficiency (EE). The optimized PXT-NTFs exhibited uniform morphology with a PS of 158.30 ± 2.73 nm, low PDI (0.142 ± 0.072), high ZP (21.00 ± 0.75 mV), and excellent EE (88.09 ± 3.40 %). Characterization through various techniques confirmed the incorporation of PXT into the nanotransferosomes and its conversion to amorphous state. Moreover, PXT-NTFG was formulated with suitable viscosity and mucoadhesive properties. In vitro release studies demonstrated sustained drug release from PXT-NTFG at different pH levels as compared to PXT-NTFs and NTF dispersion. Similarly, ex vivo experiments showed 4 folds enhanced drug permeation from PXT-NTFG when compared with PXT conventional gel. Stability studies indicated that the optimized PXT-NTFs remained stable for four months at 4°C and 25°C. Additionally, improved behavioral outcomes, increased neuronal survival rates, and upregulated brain-derived neurotrophic factor (BDNF) expression was observed in lipopolysaccharide (LPS) induced depressed Sprague-Dawley rats after treatment with PXT-NTFG as compared to PXT-dispersion treated and untreated LPS-control groups. Notably, the formulation led to a significant reduction in brain and plasma TNF-α levels. In conclusion, intranasal PXT-NTFG is a promising formulation with sustained drug release, improved brain targeting and enhanced antidepressant activity. • Paroxetine-loaded nano-transferosomes (PXT-NTFs) were prepared and loaded into gel • PXT-NTFG was intended for brain delivery via Intranasal route • PXT-NTFG established sustained release and improved permeation of PXT • In vivo depression model of PXT-NTFG demonstrated improved behavioral outcomes • Abridged brain and plasma TNF-α levels, indicated reduced inflammation in the CNS [ABSTRACT FROM AUTHOR]

Methotrexate is the treatment of choice for rheumatoid arthritis, having significant side effects on oral administration, prompting researchers to consider transdermal administration. Transfersomes can overcome the challenges of transdermal administration of drugs because of their deformable nature, allowing for greater skin penetration than other formulations. However, due to an enormous number of product and process variables, the manufacturing of transfersomes proved a pain. The goal of the research study was to use a Plackett‐Burman design to evaluate an important product and process variables connected with the preparation of methotrexate transfersomes. The influence of six product and process variables on %entrapment efficiency and vesicle deformability was investigated and according to p‐values, and the Pareto chart, the concentration of lipid, edge activator, and methotrexate were found critical variables influencing vesicle features having positive and negative effects on variables. In the future, experimental design may be used to optimize these critical parameters for further exploration in the development of methotrexate transfersomes. [ABSTRACT FROM AUTHOR]

Transfersome has been developed to enhance dermal delivery of amniotic mesenchymal stem cell metabolite products (AMSC-MP). AMSC-MP contains many growth factors for managing skin aging, thus improving the quality of an adjusted life year. This study aims to determine the effect of surfactant types acting as the edge activator on transfersome-loading AMSC-MP. Transfersome was prepared by thin-layer hydration method and composed of l-a-phosphatidylcholine as a phospholipid and three types of surfactants, namely; cationic (stearylamine), anionic (sodium cholate), and nonionic surfactant (Tween 80) at a weight ratio of 85:15, respectively. Transfersomes were evaluated for physical characteristics, penetration, effectiveness, and safety. The results showed that sodium cholate, an anionic surfactant, produced the smallest transfersome particle size, i.e., 144.2 ± 3.2 nm, among all formulas. Trans-SA containing stearylamine had a positive charge of 41.53 ± 6.03 mV compared to Trans-SC and Trans-TW, whose respective charges were -56.9 ± 0.55 mV and -41.73 ± 0.86 mV. The small particle size and low negative value of zeta potential enabled high dermal penetration by transfersomes containing AMSC-MP, while the positive charge of stearylamine hindered its penetration of deeper skin layers. Trans-SC and Trans-TW produced higher collagen density values at 77.11 ± of 4.15% and 70.05 ± of 6.95%, than that of Trans-SA. All the AMSC-MP transfersomes were relatively safe with 0.5-1.0 macrophage cell numbers invaded the dermis per field of view. In conclusion, sodium cholate, an anionic surfactant, demonstrated considerable capacity as the edge activator of transfersome-loading AMSC-MP for skin anti-aging therapy. [ABSTRACT FROM AUTHOR]

Hyperhidrosis is a condition in which the cholinergic receptors on the eccrine glands are overstimulated, resulting in excessive sweating. It is considered a serious cosmetic and psychological problem that affects the patient's quality of life. Searching for novel treatment modalities is required to minimize the side effects and to attain better patient satisfaction. Photodynamic therapy (PDT), using eosin as a photosensitizer, is developed as a promising modality of the treatment of palmar and axillary hyperhidrosis. In this study, we treated six cases suffering palmar hyperhidrosis by applying the fractional CO2 laser prior to PDT session. For PDT, a hydrogel of eosin loaded in a transfersomes as a nano-delivery carrier was applied for 5 min, followed by irradiation by intense pulsed light (IPL). The prepared transfersomes loaded by eosin were spherical in shape with encapsulation efficiency of 33 ± 3.5%, particle size 305.5 ± 5.7 nm, average zeta potential of − 54 ± 7.6 mV with 80 ± 4% of the loaded eosin was released after 3 h. Two cases achieved 90% improvement after four sessions, three patients needed six sessions to show 75% improvement, while one patient showed only 25% improvement after six sessions. This resulted in shortening the time of PS application and decreasing the number of sessions required to achieve acceptable improvement. More clinical studies on large number of patients are required to optimize the results. [ABSTRACT FROM AUTHOR]

Burn injuries can have a lasting effect on people's quality of life, as they negatively impact their physical and mental health. Then, they are likely to suffer psychological problems as a result. A serious problem is that deep burns are more challenging to treat due to their slow healing rate and susceptibility to microbial infection. Conventional topical medications used for burn treatment are sometimes ineffective because they cannot optimize their ability of transcutaneous absorption at the targeted site and accelerate healing. However, nanotechnology offers excellent prospects for developing current medical wound therapies and is capable of addressing issues such as low drug stability, water solubility, permeability, and bioavailability. The current review focuses on lipid-based vesicles (vesiculosomes) as an example of advanced delivery systems, showing their potential clinical applications in burn wound management. Vesiculosomes may help overcome impediments including the low bioavailability of active agents, offering the controlled release of drugs, increased drug stability, fewer side effects, and reduced dosing frequency, which will ultimately improve therapeutic efficacy and patient compliance. We discuss the application of various types of vesiculosomes such as liposomes, niosomes, ethosomes, cubosomes, transfersomes, and phytosomes in burn healing therapy, as these demonstrate superior skin penetration compared to conventional burn topical treatment. We also highlight their noteworthy uses in the formulation of natural products and discuss the current status as well as future perspectives of these carriers in burn management. Furthermore, the burn treatment options currently available in the market are also summarized. [ABSTRACT FROM AUTHOR]

Ellagic acid (EA) has long been recognized as a very active antioxidant, anti-inflammatory, and antimicrobial agent. However, its low bioavailability has often hampered its applications in health-related fields. Here, we report a phospholipid vesicle-based controlled release system for EA, involving the exploitation of chestnut wood mud (CWM), an industrial by-product from chestnut tannin production, as a largely available and low-cost source of this compound. Two kinds of CWM with different particle size distributions, indicated as CWM-A and CWM-B (<100 and 32 µm, respectively), containing 5 ± 1% w/w EA, were incorporated into transfersomes. The latter were small in size (~100 nm), homogeneously dispersed, and negatively charged. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing/antioxidant power (FRAP) assays indicated up to three-fold improvement in the antioxidant properties of CWM upon incorporation into transfersomes. The kinetics of EA released under simulated physiological conditions were evaluated by UV-Vis spectroscopy and HPLC analysis. The best results were obtained with CWM-B (100% of EA gradually released after 37 days at pH 7.4). A stepwise increase in the antioxidant properties of the released material was also observed. Cell-based experiments confirmed the efficacy of CWM-B transfersomes as antioxidant agents in contrasting photodamage. [ABSTRACT FROM AUTHOR]

Yasmeen Ezzeldeen,1 Shady Swidan,1,2 Aliaa ElMeshad,3,4 Aya Sebak5 1Department of Pharmaceutics, Faculty of Pharmacy, The British University in Egypt (BUE), El-Sherouk City, Cairo, 11837, Egypt; 2The Center for Drug Research and Development (CDRD), Faculty of Pharmacy, The British University in Egypt, El-Sherouk City, Cairo, 11837, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt; 4Department of Bio Nano, Faculty of Nanotechnology for Postgraduate Studies, Cairo University, El-Sheikh Zayed, Giza, 12588, Egypt; 5Department of Pharmaceutical Technology, Faculty of Pharmacy and Biotechnology, German University in Cairo (GUC), Cairo, EgyptCorrespondence: Shady Swidan Tel +20 10-0221-1048Email shady.swidan@bue.edu.egAliaa ElMeshad Tel +20 10-0010-1551Email aliaa.elmeshad@pharma.cu.edu.egBackground: Honokiol (HK) is a natural bioactive compound with proven antineoplastic properties against melanoma. However, it shows very low bioavailability when administered orally. Alternatively, topical administration may offer a promising route. The objective of the current study was to fabricate HK transfersomes (HKTs) for topical treatment of melanoma. As an ultradeformable carrier system, transfersomes can overcome the physiological barriers to topical treatment of melanoma: the stratum corneum and the anomalous tumor microenvironment. Moreover, the immunomodulatory and stemness-regulation roles of HKTs were the main interest of this study.Methods: TFs were prepared using the modified scalable heating method. A three-factor, three-level Box–Behnken design was utilized for the optimization of the process and formulation variables. Intracellular uptake and cytotoxicity of HKTs were evaluated in nonactivated and stromal cell–activated B16F10 melanoma cells to investigate the influence of the complex tumor microenvironment on the efficacy of HK. Finally, ELISA and Western blot were performed to evaluate the expression levels of TGF-β and clusters of differentiation (CD47 and CD133, respectively).Results: The optimized formula exhibited a mean size of 190 nm, highly negative surface charge, high entrapment efficiency, and sustained release profile. HKTs showed potential to alleviate the immunosuppressive characteristics of B16F10 melanoma in vitro via downregulation of TGF-β signaling. In addition, HKTs reduced expression of the “do not eat me” signal — CD47. Moreover, HKTs possessed additional interesting potential to reduce the expression of the stem-like cell marker CD133. These outcomes were boosted upon combination with metformin, an antihyperglycemic drug recently reported to possess different functions in cancer, while combination with collagenase, an extracellular matrix–depleting enzyme, produced detrimental effects.Conclusion: HKTs represent a promising scalable formulation for treatment of the aggressive B16F10 melanoma, which is jam-packed with immunosuppressive and stem-like cell markers.Keywords: honokiol, melanoma, transfersomes, heating method, tumor microenvironment, immunosuppressive, stem-like cell

[Display omitted] Vitamin B12 (cyanocobalamin) deficiency is a widespread condition because of its different aetiologies, like malabsorption syndrome or lifestyles as strict veganism that is increasing its incidence and prevalence in developed countries. It has important haematological consequences that require pharmacological treatment. Current therapy consists of oral or parenteral supplements of cyanocobalamin; however, the oral route is discarded for malabsorption syndrome patients and the parenteral route is not well accepted generally. Topical treatments have been suggested as an alternative, but the molecular weight and hydrophilicity of cyanocobalamin limits its diffusion through the skin. Lipid vesicles can allow the transdermal absorption of molecules > 500 Da. The aim of this work was to use different ultraflexible lipid vesicles (transfersomes and ethosomes) to enhance cyanocobalamin transdermal delivery. Vesicles were characterized and lyophilised for long-term stability. The ability to deliver cyanocobalamin through the skin was assessed in vitro using full-thickness porcine skin in Franz diffusion cells. As expected, the best transdermal fluxes were provided by ultraflexible vesicles, in comparison to a drug solution. Moreover, the pre-treatment of the skin with a solid microneedle array boosts the amount of drug that could potentially reach the systemic circulation. [ABSTRACT FROM AUTHOR]

The prime objective of this study was to develop amphotericin B (AMB) and rifampicin (RIF) co-loaded transfersomal gel (AMB-RIF co-loaded TFG) for effective treatment of cutaneous leishmaniasis (CL). AMB-RIF co-loaded TF was prepared by the thin-film hydration method and was optimized based on particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (%EE), and deformability index. Similarly, AMB-RIF co-loaded TFG was characterized in terms of rheology, spread ability, and pH. In vitro, ex vivo, and in vivo assays were performed to evaluate AMB-RIF co-loaded TF as a potential treatment option for CL. The optimized formulation had vesicles in nanosize range (167 nm) with suitable PDI (0.106), zeta potential (− 19.05 mV), and excellent %EE of RIF (66%) and AMB (85%). Moreover, it had appropriate deformability index (0.952). Additionally, AMB-RIF co-loaded TFG demonstrated suitable rheological behavior for topical application. AMB-RIF co-loaded TF and AMB-RIF co-loaded TFG showed sustained release of the incorporated drugs as compared to AMB-RIF suspension. Furthermore, RIF permeation from AMB-RIF co-loaded TF and AMB-RIF co-loaded TFG was enhanced fivefold and threefold, whereas AMB permeation was enhanced by eightfold and 6.6-fold, respectively. The significantly different IC50, higher CC50, and FIC50 (p < 0.5) showed synergistic antileishmanial potential of AMB-RIF co-loaded TF. Likewise, reduced lesion size and parasitic burden in AMB-RIF co-loaded TF–treated mouse group further established the antileishmanial effect of the optimized formulation. Besides, AMB-RIF co-loaded TFG showed a better safety profile. This study concluded that TFG may be a suitable carrier for co-delivery of AMB-RIF when administered topically for the treatment of CL. [ABSTRACT FROM AUTHOR]

Phyllanthus emblica Linn. (PE) has been used to promote hair growth for decades. In this study, dried PE fruit powder was extracted, tested for biological activities, and loaded into transfersomes for hair follicle targeting. Before lyophilization, PE fruit powder was extracted using 2 solvent systems, water and 30% ethanol. The PE 30% ethanolic extract had higher antioxidant activity and total phenolic content than the PE aqueous extract. However, the cytotoxicity of the PE 30% ethanolic extract was higher than that of PE aqueous extract. As a result, the PE aqueous extract was analyzed using ultra-performance liquid chromatography and found that the major component of the PE aqueous extract was gallic acid. Afterward, the PE aqueous extract was tested for its potential to activate the expression of genes involved in hair growth promotion in human keratinocytes. At a non-toxic concentration (10 μg/mL), this extract promoted various growth factors comparable to 1% minoxidil. PE-loaded transfersomes were prepared to deliver the PE aqueous extract to the hair follicle. The particle size and polydispersity index of PE-loaded transfersomes were 228 nm and 0.25, respectively. After 3 months of storage, the particle size at 4°C and 30°C was 218 nm and 241 nm, respectively, which was comparable to its initial size. However, at 40°C, the particle size dramatically increased (315 nm). The fluorescent agent, rhodamine B, was used to evaluate the potential of transfersomes to target hair follicles. Rhodamine B transfersomes had better penetration and accumulation in hair follicles than rhodamine B solution. To conclude, the PE aqueous extract, mainly composed of gallic acid, can activate hair growth gene expression. The extract can be loaded into hair follicles targeting transfersomes. Thus, PE-loaded transfersomes are a promising delivery system for hair follicle targeting to promote hair growth. [ABSTRACT FROM AUTHOR]

Background: Ultraviolet B (UVB) radiation induces physiological and morphological photoaging of the skin resulting in wrinkles, and loss of elasticity. This study analyzed nanoencapsulation of a gel combination of Centella asiatica (CA) transfersomes and rosemary essential oil (REO) nanoemulsion with lipid-based nanocarriers for the ability of both biological compounds to synergistically prevent UVB radiation, along with ameliorative and anti-aging effects. Methods: To ensure the quality, lipid-based nanocarriers of transfersomes and nanoemulsion were characterized based on physicochemical properties such as particle size distribution, polydispersity index, zeta potential. In vivo studies were used to determine the biological effects of a gel combination of CA transfersomes, and REO nanoemulsion applied topically two weeks before UVB radiation (840 mJ/cm 2) in BALB/c hairless mice. Results: Results showed that the optimum lipid-based nanocarriers had a particle size of 43.97 ± 5.6 nm, a polydispersity index of 0.64 ± 0.01, and a zeta potential of -10.91 ± 1.99 mV. In vivo experiments revealed that topical application of a gel combination of CA transfersomes and REO nanoemulsion significantly ameliorated wrinkle formation, epidermal hyperplasia, and collagen fiber arrangement caused by UVB exposure. Further, the gel combining CA transfersomes and REO nanoemulsion suppressed lipid peroxidation by decreasing the expression of malondialdehyde (MDA) and collagen destruction by inhibiting matrix metalloproteinase-9 (MMP-9) expression. Moreover, the gel combination of CA transfersomes and REO nanoemulsion upregulated type I collagen through activation of the transforming growth factor-β (TGF-β)/Smad pathway, thereby recovering the density of collagen fiber reduced by UVB radiation. Conclusions: Overall, these data indicate that topical application of a gel combination of CA transfersomes and REO nanoemulsion could act synergistically and potentially prevents oxidative stress and collagen degradation in the skin from UVB-induced photoaging.

Current cannabidiol (CBD) formulations are challenged with unpredictable release and absorption. Rational design of a rectal colloid delivery system can provide a practical alternative. In this study the inherent physiochemical properties of transferosomes were harnessed for the development of a nano-sized transfersomes to yield more stable release, absorption, and bioavailability of CBD as a rectal colloid. Transfersomes composed of soya lecithin, cholesterol, and polysorbate 80 were synthesized via thin film evaporation and characterized for size, entrapment efficiency (%), morphology, CBD release, ex vivo permeation, and physicochemical stability. The optimized formulation for rectal delivery entrapped up to 80.0 ± 0.077% of CBD with a hydrodynamic particle size of 130 nm, a PDI value of 0.285, and zeta potential of −15.97 mV. The morphological investigation via SEM and TEM revealed that the transfersomes were spherical and unilamellar vesicles coinciding with the enhanced ex vivo permeation across the excised rat colorectal membrane. Furthermore, transfersomes improved the stability of the encapsulated CBD for up to 6 months at room temperature and showed significant promise that the transfersomes promoted rectal tissue permeation with superior stability and afforded tunable release kinetics of CBD as a botanical therapeutic with inherent poor bioavailability. [ABSTRACT FROM AUTHOR]

The extract of Teucrium marum L. (Lamiaceae) was obtained using the aerial parts of the plant, by means of a maceration process. Verbascoside, caffeic acids derivatives and flavonols were the main components contained in the extract as detected using high-performance liquid chromatography coupled with diode array detector (HPLC–DAD) as an analytical method. The extract was successfully incorporated into hyalurosomes, which were further enriched by adding a water cosolvent (glycerol) and a surfactant (Tween 80), thus obtaining glycerohyalurosomes. Liposomes, transfersomes and glycerosomes were prepared as well and used as comparisons. All vesicles were small, as the mean diameter was never higher than ~115 nm, thus ideal for topical application and stable on storage, probably thanks to the highly negative surface charge of the vesicles (~−33 mV). The cryo-TEM images confirmed the formation of close-packed, oligolamellar and multicompartment hyalurosomes and glycerohyalurosomes in which around 95% of the used extract was retained, confirming their ability to simultaneously load a wide range of molecules having different chemical natures. Moreover, the extract, when loaded in hyalurosomes and glycerohyalurosomes was able to counteract the damages induced in the fibroblasts by hydrogen peroxide to a better extent (viability~110%) than that loaded in the other vesicles (viability~100%), and effectively promoted their proliferation and migration ensuring the healing of the wound performed in a cell monolayer (scratch assay) during 48 h of experiment. Overall in vitro results confirmed the potential of glycerohyalurosomes as delivery systems for T. marum extract for the treatment of skin lesions connected with oxidative stress. [ABSTRACT FROM AUTHOR]

Purpose: Recombinant human epidermal growth factor (rhEGF) is a 6045-Da peptide that promotes the cell growth process, and it is also used for cosmetic purposes as an anti-aging compound. However, its penetration into skin is limited by its large molecular size. This study aimed to prepare rhEGF-loaded transfersomal emulgel with enhanced skin penetration compared with that of non-transfersomal rhEGF emulgel. Methods: Three transfersome formulations were prepared with different ratios between the lipid vesicle (phospholipid and surfactant) and rhEGF (200:1, 133:1, and 100:1) using a thin-film hydration-extrusion method. The physicochemical properties of these transfersomes and the percutaneous delivery of the transfersomal emulgel were evaluated. Long-term and accelerated stability studies were also conducted. Results: The 200:1 ratio of lipid to drug was optimal for rhEGF-loaded transfersomes, which had a particle size of 128.1 ± 0.66 nm, polydispersity index of 0.109 ± 0.004, zeta potential of −43.1 ± 1.07 mV, deformability index of 1.254 ± 0.02, and entrapment efficiency of 97.77% ± 0.09%. Transmission electron microscopy revealed that the transfersomes had spherical and unilamellar vesicles. The skin penetration of rhEGF was enhanced by as much as 5.56 fold by transfersomal emulgel compared with that of non-transfersomal emulgel. The stability study illustrated that the rhEGF levels after 3 months were 84.96–105.73 and 54.45%–66.13% at storage conditions of 2°C–8°C and 25°C ± 2°C/RH 60% ± 5%, respectively. Conclusion: The emulgel preparation containing transfersomes enhanced rhEGF penetration into the skin, and skin penetration was improved by increasing the lipid content.

Oral cancer is one of the most common malignancies with an increased rate of incidence. 5-Fluorouracil (5FU) is an effective chemotherapeutic indicated for oral cancer treatment. Etodolac (Et), a cyclooxygenase-2 inhibitor, can be used as an adjuvant agent to sensitize cancer cells to chemotherapy. The aim of this work was to prepare and characterize 5FU and Et dual drug–loaded transfersomes to treat oral cancer. Transfersomes were prepared by thin-film hydration method and characterized for the average particle size and zeta-potential using dynamic light scattering and scanning electron microscopy techniques. The prepared transfersomes were further characterized for their drug loading, entrapment efficiencies using amicon centrifuge tubes and drug release behavior using cellulose membrane. The synergistic activity of dual drug–loaded transfersomes was studied in FaDu oral cancer cells. Results showed that the average particle size, polydispersity index, and zeta potential were 91±6.4 nm, 0.28±0.03, and (−)46.9±9.5 mV, respectively, for 5FU- and Et (1:1)-loaded transfersomes. The highest encapsulation efficiency achieved was 36.9±3.8% and 79.8±6.4% for 5FU and Et (1:1), respectively. Growth inhibition studies in FaDu cells using different concentrations of 5FU and Et showed a combination index of 0.36, indicating a synergistic effect. The FaDu cell uptake of drug-loaded transfersomes was significantly (p<0.05) greater than that of free drugs. The transfersome hydrogel made of HPMC (2% w/w) showed similar flux, lag time, and permeation coefficient as that of drug-loaded transfersomes across excised porcine buccal tissue. In conclusion, 5FU and Et transfersome hydrogel can be developed for localized delivery to treat oral cancer. [ABSTRACT FROM AUTHOR]