Protection of hair color with pomegranate peel extract-loaded liposomal formulation: Preparation, characterization, and ex-vivo activity studies.

BACKGROUND: Pomegranate peel extract is known as a powerful antioxidant and due to preventing oxidation, it can reduce color change of dyed hair after washing. Liposomes are vesicular systems that include lipids and can form a film on hair fibers. Delivery system and active agent have a synergistic effect on protecting hair color and reducing dyeing frequency. AIMS: This study aimed to prepare liposomes suspension as an innovative formulation of pomegranate peel extract to reduce hair color changing. METHODS: Pomegranate peel extract-loaded liposomes were prepared with lipidic film hydration method. The characterizations of formulations (F1 and F2) were defined by several parameters. The pH, particle size, polydispersity index, zeta potential, microscopical image, loading capacity (LC), and encapsulation efficiency (EE) of formulations were determined. The antioxidant capacity of formulations and actives were tested. The effect of formulations on hair color change was shown with ex-vivo studies. RESULTS: The results showed that cholesterol influenced particle size, zeta potential, and antioxidant capacity. The particle sizes of formulations were 217.71 ± 6.74 nm and 577.5 ± 1.41 nm for F1 and F2, respectively. F2 formulation had better results for zeta potential (33.8 mV) while F1 was neutral. Morphologic images confirmed vesicular structure or liposomes. The EE was found higher for F2 than F1 (F1: 57.14 and F2: 78.69). Antioxidant studies confirmed that active substance and the vesicular system had a synergistic effect on protection from oxidation. Selected formulation reduced hair color change as shown in ex-vivo tests. CONCLUSION: Pomegranate peel extract-loaded liposomes were designed for hair color protection. It was shown with this study that prepared formulations have a good color protection on hair fibers due to antioxidant properties of pomegranate peel extract and film forming effect of liposomal formulations. According to results, prepared liposomal formulations may serve as a good alternative for reducing dyeing frequency and protecting hair fibers.

Comparative Evaluation of Clinical Efficacy and Safety of Collagen Laminin-Based Dermal Matrix Combined With Resveratrol Microparticles (Dermalix) and Standard Wound Care for Diabetic Foot Ulcers.

This is an open, prospective, comparative parallel-arm medical device clinical study of Dermalix (Dx) in diabetic foot wounds. Dx is a 3-dimensional collagen-laminin porous-structured dermal matrix prepared and additionally impregnated with resveratrol-loaded hyaluronic acid and dipalmitoylphosphatidylcholine-based microparticles. The aim was to evaluate the efficacy and safety of Dx, an investigational medical device, in Wagner 1 and 2 wounds in comparison to a standard wound care (SWC) that consists of irrigation and cleaning with sterile saline solution. Forty-eight patients were randomized to receive either SWC or SWC + Dx. A 4-week treatment period was followed by a 2-month follow-up without treatment. The wound area measurement, total collagen, vascular epidermal growth factor, tumor necrosis factor, interleukin 1, caspase 3, glutathione, reduced/oxidized glutathione, and lipid peroxidation levels were evaluated. At the end of 4 weeks, the percentage closures of wounds were determined as 57.82% for Dx, and 26.63% for SWC groups. Dx had a significant effect on tumor necrosis factor, caspase 3, and reduced/oxidized glutathione levels. Dx provided 2 times faster wound healing and decreased oxidative stress. Application of Dx in the first phase of wound would help the wound area heal faster with a safe profile.

An examination of carbopol hydrogel/organogel bigels of thymoquinone prepared by microwave irradiation method.

Nigella sativa L. is shown wide spread over the world and contains many useful phytochemicals. Much of the biological activity of the seeds has been shown due to the presence of thymoquinone (TQ). Its poor aqueous solubility of TQ hinders its delivery to target site. The aim of this work was to prepare TQ bigels composed of Carbopol 974 P NF (C974) in PEG 400 (organogel) or C974 in water (hydrogel) with microwave heating method. A novel technique, high speed homogenization followed by microwave heating, was used to prepare organogels. The pH, electrical conductivity, differential scanning calorimetry, rheological properties, and morphological structure of the formulations have been evaluated, and the effect of microwave on drug content and TQ antioxidant activity has been investigated. The bigels of TQ were successfully produced via high-speed homogenization followed by microwave-assisted heating for the first time in this study. Highly lipophilic TQ was successfully dissolved in organogel, and it was not affected from the microwaves. It can be stated that microwave heating is a promising method to obtain C974 organogels and thus bigels with appropriate above indicated investigated physicochemical characteristics. The time and energy consumption could be decreased with microwave-assisted heating, especially for gel preparation in the field of pharmaceuticals.

Propolis loaded liposomes: evaluation of antimicrobial and antioxidant activities.

Propolis, a natural bee product, has both antimicrobial/antifungal and antioxidant characteristics. Active substances having antimicrobial and antifungal effects are used to avoid infections, which develop during long treatment process of chronic wounds. Antioxidant substances protect wound areas against the effect of free radicals and accelerate the healing process. For this purpose, propolis was used to develop topical liposome formulations for wound treatment. Characterization studies (particle size distribution, polydispersity index, Zeta Potential, morphology pH, loading capacity, encapsulation efficiency, in-vitro release behaviour) as well as stability studies were performed. Then in-vitro antioxidant (free radical scavenging capacity and trolox equivalent antioxidant capacity) and antimicrobial/antifungal activities of formulations have been evaluated. The particle size of formulations was found within the range of 300-750 nm depending on the concentration of lipid and water phase in the formulation. The Zeta Potential and pH values of optimum formulation were -23.0 ± 0.666 and 6.34, respectively. Loading capacity and encapsulation efficiency were 66.535 ± 2.705% and 57.321 ± 2.448%. At the end of 8 h, 48.16% of propolis was released and the formulations were found stable during 3 months at +4 °C. Drug loaded liposome formulations significantly scavenged the ABTS+ radical in a dose-dependent manner of propolis when compared with unloaded liposome formulations (p < 0.05). The minimum inhibitory concentration (MIC) values of liposomes ranged from 512 to 128 µg/mL for bacteria and 256 to 128 µg/mL for fungi. Overall results showed that effective and innovative alternative was developed for topical application in wound treatment with propolis loaded liposomal formulations having antioxidant and antimicrobial effects.

Antioxidant properties evaluation of topical astaxanthin formulations as anti-aging products.

BACKGROUND: The reactive oxygen species lead to skin aging via oxidative damage that are induced by UV radiation. Therefore, topical formulations which have antioxidant effect could reduce aging level. Astaxanthin is an antioxidant substance. AIMS: The aim of this study was to investigate antioxidant activity and cytotoxicity potential of the astaxanthin-loaded gel formulations. METHODS: Astaxanthin-loaded oleoresin and algae extract were used as natural active materials. The lipogel and hydrogel of these natural materials were prepared as anti-aging formulations. The formulations were characterized via parameters such as, pH, rheological analysis, mechanical properties, and stability. And also in vitro release experiments of the formulations were carried out. The antioxidant activity and cytotoxicity test were performed. RESULTS: The results of characterization studies confirmed the formulations suitable for topical application. After 24 hours, 99 µg, 88.3 µg, 403 µg, and 234.8 µg of astaxanthin released through oleoresin lipogel, oleoresin hydrogel, algae extract lipogel, and algae extract hydrogel, respectively. It was found by the cytotoxicity tests that astaxanthin is more proliferative in lipogel formulations compared to hydrogel formulations. And finally, the highest antioxidant activity was found in the algae extract hydrogel and algae extract lipogel formulation, respectively (P < .05). CONCLUSIONS: Topical formulations of astaxanthin-loaded oleoresin and algae extract were prepared successfully. At the same time, according to antioxidant activity and release studies, algae extract loaded could be suggested as topical anti-aging formulations.

Preparation and Characterization of Caffeine Loaded Liposome and Ethosome Formulations for Transungual Application.

OBJECTIVES: Nail plates have a structure that prevents transungual delivery of active agents. This situation makes it difficult to treat nail diseases. MATERIALS AND METHODS: In this study, CF-loaded liposome and ethosome formulations were prepared for ungual application. Formulations were characterized by size, microscopic observation, pH, and entrapment efficiency measurements. The effects of formulations and experimental conditions on nails were tested with characterization of nails before and after ex vivo permeation experiments. RESULTS: Microscopic observation confirmed the presence of spherical-structured vesicles. The particle sizes of vesicles were found as 545.3±0.121 nm, 610.2±0.943 nm, 349.5±0.145 nm and 337.9±0.088 nm for liposomes (FI-FII) and ethosomes (FIII- FIV), respectively. The polydispersity index of particles was found under 0.5, and the pH of formulations was around 7. The encapsulation efficiency was found low due to the hydrophilic character of CF. Nail characterization studies showed that the experimental conditions had an effect on the nail plate. CONCLUSION: The cumulative amount of drug after ex vivo permeation studies was found higher for ethosomes than for liposomes. The results confirm that liposomal systems could be promising systems for ungual drug delivery.

Preparation and in vitro evaluation of melatonin-loaded HA/PVA gel formulations.

Melatonin-loaded hyaluronic acid (HA) and poly(vinyl alcohol) (PVA) gels were prepared by using freeze-thaw technique and an emulsion method followed by freeze-thaw technique to produce a new synergistic system for topical application. Freeze-thaw hydrogels and emulgels were characterized by means of Fourier transform infrared spectroscopy, rheology and swelling tests. The porous structure of the hydrogels was shown by scanning electron microscopy observations and thermal properties were tested by differential scanning calorimetry measurements. Bioadhesion and in vitro release characterization of formulations were performed by texture profile analysis and dialysis bag method, respectively. The pore size of both formulations was ranging from 900 nm to 30 µm. Melatonin showed a good compatibility with the polymeric matrices as the pores were smaller for the drug-loaded systems. In vitro release studies showed that the release was improved by emulgel formulations. After 24 h, the release percentage was found to be 13.240% ± 1.094 and 15.192% ± 2.270 for hydrogel and emulgel, respectively. Emulgels had better bioadhesion properties than simple freeze-thaw samples. As a conclusion, regarding the in vitro characterization studies HA and PVA hydrogel and emulgel formulations and their lyophilized forms could be promising systems for topical application of melatonin.

Dual-Prevention for UV-Induced Skin Damage: Incorporation of Melatonin-Loaded Elastic Niosomes into Octyl Methoxycinnamate Pickering Emulsions.

Incorporation of antioxidants into sunscreens is a logical approach, yet co-delivery of them with UV filters is a challenge. Here, we purposed a combination therapy, in which the chemical UV filter, octyl methoxycinnamate, was accumulated on upper skin while the antioxidant, melatonin, can penetrate deeper layers to show its effects. Melatonin-loaded elastic niosomes and octyl methoxycinnamate Pickering emulsion were prepared separately. Lyophilized elastic niosomes were dispersed into the Pickering emulsion to prepare the proposed combination formulation. The characterization studies of the formulations revealed that elastic niosomes can be prepared with tunable nanometer sizes, whereas Pickering emulsions can encapsulate the UV filter in micrometer-sized droplets. Melatonin-loaded elastic niosomes prepared with Tween80/Span80 mixture were 146 nm with a PI of 0.438, and 58.42% entrapment efficiency was achieved. The mean diameter size of the combination formulation was 27.8 µm. Ex vivo permeation studies revealed that 7.40% of octyl methoxycinnamate and 58% of melatonin were permeated through the rat skin while 27.6% octyl methoxycinnamate and 37% of melatonin accumulated in the skin after 24 h. Cell culture studies with real-time cell analyzer showed that the proposed formulation consist of melatonin-loaded elastic niosomes and octyl methoxycinnamate Pickering emulsion had no negative effect on the cell proliferation and viability. According to α,α-diphenyl-ß-picrylhydrazyl free radical scavenging method, the proposed formulation showed as high antioxidant activity as melatonin itself. It is concluded that the proposed formulation would be a promising dual therapy for UV-induced skin damage with co-delivery strategy.

Wound healing effects of collagen-laminin dermal matrix impregnated with resveratrol loaded hyaluronic acid-DPPC microparticles in diabetic rats.

An alternative formulation for the treatment of diabetic foot wounds that heal slowly is a requirement in pharmaceutical field. The aim of this study was to develop a dermal matrix consisting of skin proteins and lipids with an antioxidant that will enhance healing and balance the oxidative stress in the diabetic wound area due to the high levels of glucose. Thus a novel three dimensional collagen-laminin porous dermal matrix was developed by lyophilization. Resveratrol-loaded hyaluronic acid and dipalmitoylphosphatidylcholine microparticles were combined with this dermal matrix. Characterization, in vitro release, microbiological and in vivo studies were performed. Spherical microparticles were obtained with a high RSV encapsulation efficacy. The microparticles were well dispersed in the dermal matrix from the surface to deeper layers. Collagenase degraded dermal matrix, however the addition of RSV loaded microparticles delayed the degradation time. The release of RSV was sustained and reached 70% after 6h. Histological changes and antioxidant parameters in different treatment groups were investigated in full-thickness excision diabetic rat model. Collagen fibers were intense and improved by the presence of formulation without any signs of inflammation. The highest healing score was obtained with the dermal matrix impregnated with RSV-microparticles with an increased antioxidant activity. Collagen-laminin dermal matrix with RSV microparticles was synergistically effective due to presence of skin components in the formulation and controlled release achieved. This combination is a safe and promising option for the treatment of diabetic wounds requiring long recovery.

A comparative evaluation of coenzyme Q10-loaded liposomes and solid lipid nanoparticles as dermal antioxidant carriers.

BACKGROUND: The effective delivery of coenzyme Q10 (Q10) to the skin has several benefits in therapy for different skin pathologies. However, the delivery of Q10 to deeper layers of skin is challenging due to low aqueous solubility of Q10. Liposomes and solid lipid nanoparticles (SLN) have many advantages to accomplish the requirements in topical drug delivery. This study aims to evaluate the influence of these nanosystems on the effective delivery of Q10 into the skin. METHODS: Q10-loaded liposomes (LIPO-Q10) and SLNs (SLN-Q10) were prepared by thin film hydration and high shear homogenization methods, respectively. Particle size (PS), polydispersity index (PI), zeta potential (ZP), and drug entrapment efficiency were determined. Differential scanning calorimetry analysis and morphological transmission electron microscopy (TEM) examination were conducted. Biocompatibility/cytotoxicity studies of Q10-loaded nanosystems were performed by means of cell culture (human fibroblasts) under oxidative conditions. The protective effect of formulations against production of reactive oxygen species were comparatively evaluated by cytofluorometry studies. RESULTS: PS of uniform SLN-Q10 and LIPO-Q10 were determined as 152.4 ± 7.9 nm and 301.1 ± 8.2 nm, respectively. ZPs were -13.67 ± 1.32 mV and -36.6 ± 0.85 mV in the same order. The drug entrapment efficiency was 15% higher in SLN systems. TEM studies confirmed the colloidal size. SLN-Q10 and LIPO-Q10 showed biocompatibility towards fibroblasts up to 50 µM of Q10, which was determined as suitable for cell proliferation. The mean fluorescence intensity % depending on ROS production determined in cytofluorometric studies could be listed as Q10 ≥ SLN-Q10 > LIPO-Q10. CONCLUSION: The LIPO-Q10 system was able to enhance cell proliferation. On the contrary, SLN-Q10 did not show protective effects against ROS accumulation. As a conclusion, liposomes seem to have advantages over SLN in terms of effective delivery of Q10 to skin for antioxidant purposes.