Current Pharmaceutical Biotechnology - Volume 16, Issue 12, 2015

Skincare products with multiple beneficial functions are currently of great interest to most cosmeceutical consumers in the world, which provides a strong driving force for the search of new bio-active ingredients. Along with the development of cosmeceuticals, seeking the efficient delivery systems to convey these active substances to the human skin has also gained increasing attention in the field of research and development. In order to elevate the delivery efficacy of cosmetics/drugs, colloidal carriers such as vesicles, nano/micro-emulsions, and nano/micro-particles have been widely developed. This review focuses on the recent investigations of lipid- and surfactant-based vesicles for cosmeceutical applications. Categories, preparation methods, physicochemical characteristics, and safety and efficacy evaluations of lipid- and surfactant-based vesicles capable of delivering cosmeceuticals are discussed in this review.

Human hair serves a biological purpose of protecting the scalp, as well as physical attractiveness to the perception of beauty. Hair loss, graying of hair, dandruff and other conditions affecting hair conditions can be distressing to patients, as hair condition is often considered important in people’s own assessment of physical beauty. Different hair types can benefit from different treatment methods to promote hair health and growth. External factors like exposure to the sun and smoking, dietary factors including malnutrition of essential fatty acids and vitamins, and chemicals applied to the hair and scalp in shampoos and other treatments can all cause damage to existing hair and impair hair growth. Specific chemicals found in many shampoos, including antimicrobial agents, surfactants and preservatives, can all impair different aspects of hair health. In this review, we aim to discuss the main hair issues, such as hair loss, followed by the safety assessments of selected ingredients in shampoo, and possible nourishment for scalp improvement. This review highlights areas of disagreement in the existing literature, and points to new directions for future studies. Key conclusions include the carcinogenic chemicals to avoid, alternatives of such ingredients, and scalp nourishing treatments with micronutrients.

Elastic fibers are major constituents of the extracellular matrix (ECM) in dynamic tissues in the human body, and regulation of elastin and fibrillin-1 expression mediates the formation of these fibers. Traditional assays for the measurement of elastin and fibrillin-1, such as western blotting, Luna staining and immunostaining, are relatively complex and time-consuming. Thus, a relatively simple assay system that also provides rational results is urgently needed. In the study, we aimed to develop a human cell-based assay system that can be used to analyze functional compounds using the promoters of elastin (ELN) and fibrillin-1 (FBN1) genes integrated with a secreted alkaline phosphatase (SEAP) reporter in normal human fibroblast cells. We used this system to assess anti-aging compounds. We used several regulators of elastinogenesis, including retinol, coenzyme Q10, deoxyArbutin and ElestanTM (Manilkara multinervis leaf extract), to verify the efficacy of this assay system. Our results demonstrate that this assay system can be used as a fast and realistic method for identifying anti-aging components for future use in foods, cosmetics and drugs.

Background: Anti-aging skin care is a growing popular topic in cosmetic and aesthetic fields, and skin care rather then makeup tips draw more attention nowadays. The phenomenon of skin aging includes thinning of skin losses of elasticity and moisture, pigmented spot formation, and wrinkle development. Along with growth in age, the decreased rates of epithelium renewal and cellular recovery as well as the reduced contents of elastin, collagen, and glycosaminoglycans all contribute to creases or folds of skin. Available strategies for wrinkle treatments include topical use of skin care products with anti-aging contents, dermabrasion, laser, Botox injection, fillers injection, and facelift. Though all of these above options can provide different degrees of improvement in facial wrinkles, the cost-effect, pain of intervention therapy, and necessity of repetitive treatment may impact on choices made. Topical use of anti-aging skin products is the most convenient and cheap way to achieve skin anti-aging effect. LycogenTM is an antioxidant, which can prevent the downregulation of pro-collagen I, intracellular accumulation of malondialdehyde (MDA) and achieve the aim of skin rejuvenation. Methods: Twenty-six female patients were included in our study with ages between 30 and 45. They were randomly assigned to two groups: the vehicle control group and the experimental group. Patients in the control group applied a skin care product without LycogenTMto the face via sonophoresis after facial cleanser use in the morning and at night. The experimental group applied a LycogenTM -containing skin care product via sonophoresis in the same time schedule. We evaluated results, including pigmented spots, wrinkles, texture, pores, and red area by VISIA on weeks 0, 1, 2, 4, 6, 8, and 10 respectively. Results: In the aspect of pigmented spots, the experimental group showed significant difference in comparison with the vehicle control group on weeks 2, 6, 8, and 10. For wrinkles, the experimental group had better results on weeks 1, 2, 4, 8, and 10. Measured by texture, the experimental group had better results on weeks 1, 2, 4, 6, 8, and 10. Determined by pores, the experimental group had better results on weeks 2, 4, 6, 8, and 10. Concerning red areas, the experimental group had better results on weeks 6, 8, and 10. (p < 0.05). Conclusion: In our study, we applied a LycogenTM- containing product by sonophoresis as the experimental group in comparison with a skin care product without LycogenTM. VISIA (Canfield Imaging Systems, Fairfield, NJ) was used to evaluate facial skin in aspects of pigmented spots, wrinkles, texture, pores, and red area. Overall, LycogenTM had proven effectiveness on anti-oxidation as patients who used the Lycogen TM -containing product had better outcomes.

A new organoclay, bio-inorganic hybrid material, was successfully prepared following the "green chemistry" principles, exploiting microwave irradiation (as an alternative energetic source) in both the solvent-free synthesis of the organic filler (UVB filter) and in its hydrothermal intercalation in a sodium Bentonite clay (renewable natural inorganic source at low temperature). The organic filler is a benzylidene camphor derivative with the same cationic moiety as the well- known UV filter camphor benzalkonium methosulfate. The aim of the research was the ecosustainable development of a new UV protection model, suitable for use in cosmetic and pharmaceutical products, with potential advantages of stability, efficiency and safety compared to the commercially available UVB sunscreens. The organically modified clay was thoroughly investigated using X-ray diffraction (XRD), infrared spectroscopy (IR), thermo gravimetric analysis and differential thermal analysis (DTA). Results confirmed the complete intercalation of the organic filler in the interlayer region of the smectite clay, leading to a new bio-inorganic hybrid material with potential for cosmetic and pharmaceutical applications in the UV protection field, as confirmed by preliminary photochemical studies. This work represents the first example in the use of Na-Bentonite cationic clay (usually employed as rheological additive) as hosting agent of the synthesized quaternary UVB filter, as well as in the complete MW-assisted preparation of the organoclay, starting from the synthesis of the organic UV sunscreen to its hydrothermal intercalation.

Data obtained through high-throughput technologies have gradually revealed that a unique stratified epithelial architecture of human skin along with the antioxidant-response pathways provided vital defensive mechanisms against UV radiation. However, it is noteworthy that skin is a major target for toxic insult by UV radiations that can alter its structure and function. Substantial fraction of information has been added into the existing pool of knowledge related to natural products mediated biological effects in UV exposed skin cells. Accumulating evidence has started to shed light on the potential of these bioactive ingredients as protective natural products in cosmetics against UV photodamage by exerting biological effects mainly through wide ranging intracellular signalling cascades of oxidative stress and modulation of miRNAs. In this review, we have summarized recently emerging scientific evidences addressing underlying mechanisms of UV induced oxidative stress and deregulation of signalling cascades and how natural products can be used tactfully to protect against UV induced harmful effects.

The inhibition of melanogenesis by yeast extracts from cultivations of recombinant Pichia pastoris catalyzing ortho-hydroxylation of flavonoids was investigated. The recombinant yeast harbored a fusion gene composed of the CYP57B3 gene from Aspergillus oryzae and a cytochrome reductase gene from Saccharomyces cerevisiae. Ten flavonoids belonging to flavones, flavonols, flavanones, flavanols, and isoflavones were evaluated for biotransformation by the recombinant strain. The results showed that five flavonoids, including the flavone apigenin, the flavanones naringenin and liquiritigenin, and the isoflavones daidzein and genistein, could be biotransformed. The yeast extracts from the five biotransformation fermentations were then evaluated for inhibitory activity on melanogenesis in cultured mouse B16 melanoma cells. Three yeast extracts from biotransformation fermentation feeding with daidzein, genistein, or apigenin showed inhibitory activity on melanogenesis in the B16 cells, while the extract from genistein biotransformation exhibited the highest activity. The yeast extract from genistein biotransformation also showed inhibitory activity on cellular tyrosinase activity in the B16 cells. The present study shows a CYP with multiple flavonoid substrates for the first time and highlights the usage of yeast extracts from cultivations of the recombinant yeast catalyzing flavonoids’ biotransformation in the development of skin-whitening agents.

The control of gene expression is critical for metabolic engineering. The multi-copy plasmids has been widely used for high-level expression of genes. However, plasmid-based expression systems are liable to genetic instability and require a selective pressure to assure plasmid stability. In this study, we first constructed a lycopene producer Escherichia coli through promoter engineering. Saccharomyces cerevisiae mevalonate (MEV) pathway was also optimized to balance expression of the top and bottom MEV pathway by using the different strength promoters. The chromosomal heterologous expression of the optimized S. cerevisiae MEV pathway can further improved lycopene production. The final engineered strain, E. coli LYCOP 20, produced lycopene of 529.45 mg/L and 20.25 mg per gram of dry cell weight in the fed-batch culture. The engineered strain does not have a plasmid or antibiotic marker. This strategy used in this study can be applied in pathway engineering of E. coli and other bacteria.

A novel steroidal oxime (SO) was synthesized using an economic method and then characterized by Fourier transform infrared (FTIR) and 1H nuclear magnetic resonance (NMR). When dispersed in pure water, SO can self-assemble into a nano-scale circular structure which was verified by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The formation of SO nano aggregates may result from its ambiphilic characteristic which has the hydrophobic cholesterolbased backbone and the hydrophilic oxime head group. The prepared SO aggregates were then examined for its in vitro biocompatibility using the human keratinocytes cell line (HaCaT) as a representative skin exposure model. The biocompatibility was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and cell morphology observation. The results showed that the nano-scale SO aggregates did not cause serious damage to HaCaT cells at the designed concentrations and suggested that SO could be a potential material for preparing cosmeceutical carrier.

Skin color is primarily produced by melanin, which is a crucial pigment that protects the skin from UV-induced damage and prevents carcinogenesis. However, accumulated melanin in the skin may cause hyperpigmentation and related disorders. Melanin synthesis comprises consecutive oxidative reactions, and tyrosinase is the enzyme that catalyzes the rate-limiting process of melanogenesis. In this study, tyrosinase-related protein 1 (TRP-1) and TRP-2 contributed to melanin formation. N-(4-bromophenethyl) caffeamide ((E)-N-(4-bromophenethyl)-3-(3,4-dihydroxyphenyl)acrylamide; K36H), a caffeic acid phenyl amide derivative, inhibited α-melanocyte-stimulating hormone (α-MSH)-induced melanogenesis and tyrosinase activity in B16F0 cells. In addition, K36H reduced the protein expression of the phospho-cAMP response element binding protein (p-CREB), microphthalmia-associated transcription factor (MITF), tyrosinase, and TRP-1. Moreover, K36H promoted AKT and glycogen synthase kinase 3 beta (GSK3β) phosphorylation, thereby inhibiting MITF transcription activity. Thus, K36H attenuated α-MSH-induced cAMP pathways, contributing to hypopigmentation. The results of a safety assay revealed that K36H did not exhibit cytotoxicity or irritate the skin or eyes. According to these results, K36H may have the potential to be used as a whitening agent in the cosmetic and pharmaceutical industries.

Melanin uncontrollable accumulation is a serious social problem to not only women, but also men, and causes pigment over-expression disorders such as freckles, melasma or pigmented acne scars. The synergism is used widely in medication, and the effectiveness makes the drug applications more valuable. Within this experiment, three well-known compounds were chosen: kojic acid, 1-phenyl-2-thiourea (PTU) and arbutin, and they were combined individually with our substance linderanolide B, which is purified from Cinnamomum subavenium. Hence, deciphering the synergistic action of possible whitening agents was the goal of this study. The tyrosinase activity, melanin content, and the combination index (CI) values were observed in B16F10 cells, in addition, the consequences were detected by isobologram analysis. We discovered that certain melanin inhibitors showed synergistic properties when they were combined together to suppress tyrosinase activities. As a result, linderanolide B has a potential synergy on tyrosinase inhibition, and it can be used widely in cosmetic and medication industries.