Evaluation of Caffeine Gels on Physicochemical Characteristics and In Vivo Efficacy in Reducing Puffy Eyes
Abstract
The eyelids are the thinnest skin in the body, leading to be easy for the blood vessels to show through the skin caused a swollen and dark appearance called puffy eyes. Placing refrigerated damp tea bags on the eyelids has been believed for a long time that it can reduce the puffy eyes due to the vasoconstriction of caffeine. This study aimed to characterize physicochemical properties and to determine in vivo efficacy in reducing puffy eyes of the prepared caffeine gels. The formulation composed of 3% caffeine, 2% ethanol, 0.3% Uniphen ® P-23, 7.5% propylene glycol, 0.5% Carbopol ® Ultrez-21 and water to 100% was selected for eye irritation test and efficacy evaluation since it possessed good characteristics and provided sustained skin permeation. The 34 volunteers (18 women, 16 men) who easily developed puffy eyes after going to bed without sleep and with no irritation to caffeine gel as well as its gel base were treated with the gels in a randomized, double-blind, placebo-controlled trial. The skin permeation profiles showed that all caffeine gels allowed caffeine to permeate through the newborn pig skin. However, the overall efficacy of the selected caffeine gel in reducing puffy eyes was not significantly different from that of its gel base. It could be concluded that the cooling effect of the hydrophilic gels was the main parameter in reduction of eye puffiness rather than the vasoconstriction of caffeine.
Supplementary resource (1)
... Caffeine (1,3,7-trimethylxanthine) is a xanthine alkaloid that has gained so much attention in the cosmetic industry due to its active role in improving our skin condition by exerting anti-cellulitic, anti-photoaging and antioxidant activities as well as stimulating hair growth [5]. More importantly, caffeine, when topically applied, has been proven to effectively address dark circles under the eyes by reducing vascular leakage through its vasoconstrictive effects and improving wrinkles [2,6,7]. However, caffeine may not be perceived as an ideal candidate for skin permeation because of its hydrophilic properties (log P = − 0.07), unusual solubility behavior in non-aqueous solvents and potential to form aggregates in aqueous solutions [8,9]. ...
... However, caffeine may not be perceived as an ideal candidate for skin permeation because of its hydrophilic properties (log P = − 0.07), unusual solubility behavior in non-aqueous solvents and potential to form aggregates in aqueous solutions [8,9]. Thus, various strategies have been developed to improve the skin permeation of caffeine including a passive approach by incorporating it into gels, ointments, micro-and nano-emulsions and nanoparticles as well as physical methods with the use of ultrasound, iontophoresis and microneedles [7,[9][10][11][12][13][14][15]. ...
... One study tested three herbs including witch hazel for their antioxidant properties as they were reported to possess high polyphenolic content as well as anti-aging abilities via inhibition of collagenase and elastase. [5] These are enzymes that breakdown the structures of collagen and elastin respectively, gives the looks of sagging skin which can be seen in eye bags caused due to age. ...
... This study also revealed that for the witch hazel distillate, which was used for testing, the practical antiinflammatory effects are still considerable and validate the purpose for which they are advertised. [5] Cucumber: 47.8% (11 participants) According to one research paper, cucumber slices can subdue puffiness under the eyes because of its anti-inflammatory properties. [6] This is a very common and effective method that is also reflected in our study and echoed by another study which states that placing the two slice of cucumber on the eyes for ten minutes can reduce the puffiness noticeably. ...
Background: Periorbital edema is a major cosmetic concern for women across all the ages. Many lifestyle changes contribute to the worsening of puffy eyes in all age groups, while aging, chronic medical conditions are also a factor. The purpose of this study is to identify the various remedies women use to treat periorbital edema with a focus on studying homemade remedies, their mechanism of action and their effectivity. Study around this topic is important as there is a distinct lack of literature on a topic that is a cosmetic concern for women. Method: An online survey of 14 questions was conducted asking questions regarding periorbital edema and the quick effective homemade remedy used by them. Results: 50.8% (n=61) participants deal with puffy eyes while 49.2% (n=59) did not. From the 61 participants who dealt with eye puffiness, only 37.7% (n=23) took active measures to counteract it. From 23 respondents, it was found that most found using cold compression (n=17), getting enough sleep (n=11), and cucumbers (n=11) the most effective in dealing with eye puffiness, while vitamin E, K, caffeine treatments and witch hazel were less popular. Majority found these methods effective 'sometimes', and only one person didn't find them effective. Conclusion: Women find cold compression, cucumber, and getting enough sleep most effective. Although more than half the participants of the survey dealt with eye puffiness, majority chose not to treat them.
... Coffee silver skin extract demonstrated no irritancy in an in vitro test on human epidermis and in an in vivo test on subjects' skin when patched for 48 h [54]. Amnuaikit et al. reported that the gel base formula containing 3% caffeine caused no signs of discomfort after being applied on subjects' arms for 24 h [55]. Both coffee extract and the major compounds in coffee have also been reported for their nonirritating properties. ...
Encapsulation of bioactive compounds in the liposome system provides several advantages, such as enhancing the stability and lowering the toxicity of active compounds. Coffee berry extract (CBE) has previously been established to have in vitro anti-aging properties and to retard the aging of human skin. The purposes of this study were to encapsulate CBE in nanoliposomes and to assess its stability and in vitro anti-aging potential in human dermal fibroblasts (HDF), as well as in healthy human skin. In the HDF model, anti-aging potential was determined by nitric oxide (NO) and collagenase inhibition assays and a superoxide dismutase (SOD) activity assay, whereas in healthy human skin (in vivo), the skin elasticity and brightness were examined. First, liposomal CBE (L-CBE) was created with a particle size of 117.33 ± 2.91 nm, a polydispersity index (PDI) of 0.36 ± 0.03, and a zeta potential of -56.13 ± 1.87 mV. The percentages of encapsulation efficacy (%EE) and loading efficacy (%LE) were 71.26 ± 3.12% and 2.18 ± 0.18%, respectively. After undergoing a 12-week stability test, the L-CBE retained more phenolic content than the free CBE when stored at 4 °C, room temperature, and 45 °C. Compared to free CBE, the L-CBE demonstrated a more consistent, elevated, and prolonged release of phenolics from the lipid system. In human dermal fibroblasts, L-CBE showed lower toxicity, and at its maximum nontoxic concentration (10 mg/mL), it exhibited slightly higher anti-aging effects than CBE, including NO inhibition, enhanced SOD activity, and anti-collagenase activities. In clinical trials (30 volunteer subjects), none of the participants' skin was irritated when the L-CBE, the CBE, or base creams were applied. After 2 weeks of application, the L-CBE and CBE creams both demonstrated an improvement in skin elasticity and a reduction in melanin levels, and after 4 weeks, L-CBE cream showed a significantly greater improvement in skin elasticity and lightening. The results demonstrate that the encapsulation of the CBE in liposomal systems could increase its stability and skin penetration, reduce its toxicity, and maintain its anti-aging effect, which is powerful enough to be exploited in anti-aging and whitening agents for application in cosmetics and cosmeceuticals.
... The canthal, forehead, cheeks, and nasolabial region were all treated. Medical outcomes for fine wrinkles and skin texture were good in 37.5% of cases, sufficient in 37.5%, and insufficient in 25% of cases 25 . ...
... The maximal absorption of caffeine is reached at 100 min after local application in vivo (18). Amnuaikit e t al. (19) performed experiment on the 34 volunteers divided into four groups, and the studies were taken for four successive days (about 8-9 volunteers/ group/d). They were assigned to lie on the bed but did not sleep for one night. ...
Plants are a rich source of a wide variety of bioactive compounds that can be used for the preparation of cosmetics. Natural cosmetics with plant components such as vitamins, polyphenols, and alkaloids have become more and more popular. Alkaloids are important secondary metabolites in plants. They are known to possess therapeutic properties. Alkaloids can be used in the production of tonics, creams, lotions, face and hair masks, compresses for skin problems with numerous inflammations, and discoloration and antiaging products, as well as for reducing the formation of cellulitis. Alkaloids are also used in the production of ampoules for cosmetologists and aesthetic medicine doctors. However, at higher doses, they may exhibit toxic properties. Several studies have been carried out in evaluation of the activity of alkaloids from various plants for their use in cosmetics. This review describes alkaloids (caffeine, capsaicin, berberine, piperine, spilanthol, and anatabine) derived from various plants that are used in cosmetics, as well as their reported activities.
... 79 One of the most important cosmetic uses of caffeine is its use to reduce swelling around the eyes (puffy eyes). 80 Anti-dandruff agents. Dandruff is a very common condition of the scalp characterized by flaking and itching. ...
Skin appearance is essential for self‐esteem and quality of life, consequently, skin care products represent a huge market. In particular, cosmeceuticals constitute a hybrid category of skin care formulations, at the interphase of cosmetics and pharmaceuticals, rationally designed to target (patho)physiological mechanisms aiming to enhance skin health and appearance. Cosmeceuticals are marketed as anti‐aging, anti‐wrinkle, hair regrowth, skin whitening and wound healing agents with special emphasis on scar‐free healing. An overview on recent cutting‐edge advances concerning the discovery and development of enhanced performance cosmeceuticals by drug repositioning approaches is presented here. In this context, we propose “target repositioning”, a new term, to highlight that druggable protein targets implicated in multiple diseases (hubs in the diseasome) can be exploited to accelerate the discovery of molecularly targeted cosmeceuticals that can promote skin health as an added benefit, which is a novel concept not described before. In this direction, emphasis is placed on the role of mouse models, for often untreatable skin diseases, as well as recent breakthroughs on monogenic rare skin syndromes, in promoting compound repositioning to innovative cosmeceuticals.
... In a randomized, double-blind study, caffeine-based gel was found to reduce lower orbital edema and also reduce periorbital pigmentation. 14 ...
Background:
The periorbital region is among the first areas to be affected by the process of aging, which is influenced by genetic and constitutional factors. As the region plays an important role in overall facial appearance, rejuvenation of the area has immense cosmetic benefit and various treatment modalities have been used to achieve the same.
Aims:
This article reviews commonly used non-surgical and minimally invasive modalities for periorbital rejuvenation.
Methods:
The literature research considered published journal articles (clinical trials or scientific reviews). Studies were identified by searching electronic databases (MEDLINE and PubMed) and reference lists of respective articles. Only articles available in English were considered for this review.
Results:
Autologous platelet rich plasma (PRP) is increasingly used in dermatology for skin and hair conditions. The use of PRP is rapidly growing in popularity as a modality to achieve skin rejuvenation. The mechanism by which PRP leads to skin rejuvenation is by increasing the dermal fibroblast proliferation, expression of matrix metalloproteinase and collagen synthesis.
Conclusion:
The evidence discussed in this article indicates the increasing importance of minimally invasive modalities in periorbital rejuvenation and a promising role for PRP as solo therapy or in multimodality regimens.
Background:
The development of effective cosmetic products for the reduction of the signs of skin aging is a complex process which requires an optimized combination of ingredients and specialized systems to deliver the actives to the skin layers.
Aim:
To evaluate the tolerance and antiaging clinical efficacy of a cosmetic formulation containing a blend of nanoencapsulated antioxidants: ascorbyl palmitate, resveratrol, tocopherol, caffeine, carnosine, and niacinamide.
Methods:
Clinical efficacy was determined by subjective and instrumental analyses of collagen synthesis by fluorescence spectroscopy, by three-dimensional imaging analysis of suborbital edema, and by analysis of skin hydration and sebum content by biophysical techniques-Corneometer® and Sebumeter®.
Results:
The studied formulation was safe and effective for the improvement of skin appearance by increasing collagen synthesis and skin moisturizing and by reducing facial blemishes, swelling, and oiliness. A preclinical exploratory approach using an experimental model of human cell and skin cultures agreed with the observed antiaging effects, identifying mechanisms related to the containment of oxidative stress, reduction of melanin production, increased synthesis of type I procollagen, and regulation of the epidermal cohesion protein filaggrin.
Conclusions:
The skin benefits obtained resulted from the combination of the ingredients in the formulation and the nanoencapsulation-based delivery system, which favors the solubility, safety, efficacy, and bioavailability of the preparation to the skin.
Infraorbital dark circles are a significant esthetic concern with few publications however offering evidence-based recommendations for their classification and consequent management. A literature review has been undertaken to classify dark circles based on etiology: shadowing, vascular, idiopathic hyperpigmentation, post-inflammatory hyperpigmentation, constitutional and offer an analysis of current treatment modalities and their effectiveness in managing specific types of infraorbital circles. This review aims to provide a detailed account of dark circle etiology, assessment and management.
Ethical considerations and the limitation in availability of human skin for percutaneous absorption studies of drugs are the main reasons for the use of animal skin. Pig skin has been reported to have permeability properties resembling that of human skin. The aim of the current study was to investigate the suitability of newborn pig skin as a model in percutaneous absorption studies. The anatomical features of skin from newborn pigs have been investigated using light and electron microscopy. The use of pigs that have died of natural causes shortly after birth allows the experiments to be carried out under tissue retrieval rather than animal ethics regulations. The thickness of the stratum corneum and epidermis was found to be similar to that of human skin and considerably thinner than adult pig skin, although the hair follicle density was much greater than that in either adult pigs or humans. Assessment of integrity of full-thickness newborn pig skin was performed using water permeability and electrical resistance measurements. A resistance greater than 20 kΩcm2 was proposed as a stringent and conservative indicator of an intact barrier function. The in vitro permeation characteristics of some model compounds (tritiated water, [14C] mannitol, and propranolol hydrochloride) have also been investigated. With the exception of mannitol, newborn pig skin was found to have a similar permeation properties to human skin (factor of difference values between 1-1.5). In addition, a comparison has been made on the enhancing effect of two terpenes, carvacrol and menthol, on the permeation of propranolol hydrochloride. Permeability through newborn pig skin was approximately double that of human skin but the rank order of enhancement remained the same. The factor difference values suggest that as a human skin substitute, newborn pig skin may be a suitable model for percutaneous absorption screening studies.
Transdermal drug delivery has many advantages over the oral administration of drugs. This is the reason why many researchers have extensively investigated the transdermal absorption of drugs. However, a much smaller number of drugs are marketed using this route of delivery, compared to oral dosage forms, because drug absorption across the skin is very low due to the stratum corneum (the main barrier for drug absorption across the skin). Overcoming the penetration barrier would significantly improve the development of an efficient transdermal drug delivery system. Several techniques have been developed, or are under development, to bypass the stratum corneum. Approaches that have been made to overcome the stratum corneum fit into five different categories: (i) device and formulation; (ii) modification of stratum corneum by chemical enhancers; (iii) ablation; (iv) bypassing the stratum corneum via appendages; and (v) electrically assisted methods such as iontophoresis and electroporation. Furthermore, possible combinatorial uses of several approaches have been studied. Although the safety issues of these synergistic approaches still require clarification, several combinations could be promising. Finally, there is a necessity to regulate the intradermal disposition of drugs to develop a more efficient transdermal drug delivery system after overcoming the skin barrier.
The ability of Azone (1-dodecylazacycloheptan-2-one), a novel penetration enhancer, to increase the percutaneous delivery of metronidazole has been investigated, across full thickness human skin in vitro. A finite dose technique was used employing several vehicles. Azone at a concentration of 1% was found to be as effective as 5% and 10% concentrations in achieving enhanced transport of metronidazole. The presence of propylene glycol was found to be necessary for maximal enhancement, and the penetration of this compound was also found to be markedly enhanced by Azone. The delivery of metronidazole within the first 20 h of the experiments was increased about 25 times in the presence of 1% Azone. Repeated doses of the drug after a single dose of Azone indicated that the effect of Azone on the skin remains after several days.
The transport of ibuprofen from propylene glycol vehicles through rat skin has been monitored in vitro. Skin stored for up to 4 months showed no significant change in its permeability to the drug but when the same tissue was used for consecutive experiments dramatic increases in flux were observed. Significant effects on drug permeation caused by vehicle composition and pH were found and solubilities and vehicle-skin partition coefficients were measured for all vehicles. As the concentration of propylene glycol increased permeation was related to the increase in solubility and reduction in partition coefficient. The pH effect was related to the degree of ionisation of the drug and to the effective concentration or degree of saturation when solutions were used. With suspensions of ibuprofen penetration rates were effectively independent of pH until high values were used when the vehicle interfered with the barrier properties of the skin.
A double-blind, randomized, placebo-controlled study was conducted with 46 healthy female volunteers in order to test an anti-cellulite product containing retinol, caffeine and ruscogenine. An evaluation of different parameters related to cellulite appearance, i.e., the skin macrorelief, the dermal and hypodermal structures, the skin mechanical characteristics, and the cutaneous flowmetry was assessed using several non-invasive methods. This combination of different evaluation methods resulted in the demonstration of significant activity of the anti-cellulite product versus baseline and showed its superiority versus the placebo in skin macrorelief (decrease of the "orange peel" effect) and an increase in cutaneous microcirculation. By using a combination of methods, it was possible to detail the activity of an anti-cellulite product and to show superiority of the product in comparison with the placebo.
The use of human skin models for performing cutaneous bioavailability studies has been little investigated. For instance, only few studies have been reported on human skin models dealing with vehicle effects on percutaneous penetration. The present study aimed at evaluating the influence on caffeine's and alpha-tocopherol's cutaneous bioavailability of cosmetic vehicles such as a water-in-oil emulsion, an oil-in-water emulsion, a liposome dispersion and a hydrogel applied at finite dose using the reconstructed human skin models EpiDerm and Episkin. The results were compared with those obtained in human skin ex vivo using similar experimental conditions. It was demonstrated that the rank order of solute permeability could be correctly predicted when the preparation was applied at a finite dose in human skin models, at least when solutes with far different physicochemical properties such as caffeine and alpha-tocopherol were used. If only slight effects of cosmetic vehicle on skin bioavailability were observed in human skin ex vivo, they were less predictable using skin models. Especially, alcohol-containing vehicles seemed to behave differently in EpiDerm as well as in Episkin than on human skin ex vivo. Stratum corneum intercellular lipid composition and organization of human skin models differ to some extent from that of human stratum corneum ex vivo, which contributes to less pronounced barrier properties, together with the increased hydration of the outermost stratum corneum layers of the models. These features, as well as still unknown factors, may explain the differences observed in vehicle effects in human skin ex vivo versus human skin models.