Facial Treatment with 3-O-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment

Ascorbic acid (AA) is a water-soluble vitamin that is found at high concentrations in normal skin. The important and well-known benefits of using AA in skin health include the stimulation of collagen synthesis and the assistance of protection against photo-oxidative damages. To maintain stability and improve drug delivery to the active site, a variety of AA derivatives have been chemically synthesized. Among these compounds, we focus here on a lipophilic derivative, 3-O-cetyl ascorbic acid (3-CetylAA), which remains poorly characterized for cosmetic applications. Uptake analysis in three healthy human volunteers’ skin was conducted using a serial tape-stripping technique detecting 3-CetylAA (on average, 128 ± 27 pmol per µg) in the stratum corneum after a 5-h topical treatment when treated with 25 mM 3-CetylAA-containing cream for 13 days twice daily and continuously. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) imaging of vertical cryosections of pig skin revealed the presence of 3-CetylAA in the epidermal layer after topical treatment with 3-CetylAA-containing cream. In sun-exposed human skin, 3-CetylAA improved the texture after treatment with 25 mM 3-CetylAA-containing cream for 4 weeks or more when used twice daily or continuously. An in vitro transformation assay using BALB/c 3T3 A31-1-1 cells demonstrated that 10 µM 3-CetylAA, which is the same concentration exhibited in vitro biological activities in another lipophilic AA derivative, 2-O-octadecyl ascorbic acid, was non-carcinogenic and did not potentiate the UVC-induced transformation frequency when applied for 3 days after UVC irradiation. These results demonstrate that 3-CetylAA is a promising candidate as a lipophilic derivative of AA for cosmetic purposes.

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Development of cyclosporine-loaded nanoemulsion for topical treatment of psoriasis

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v10ispl1.1676 ◽

2019 ◽

Vol 10 (SPL1) ◽

Author(s):

Siti Hajar Musa ◽

Norazlinaliza Salim ◽

Norashikin Shamsudin ◽

Mahiran Basri ◽

Hamid Reza Fard Masoumi

Keyword(s):

Topical Treatment ◽

Oral Delivery ◽

Ostwald Ripening ◽

Normal Skin ◽

Severe Case ◽

Transepidermal Water Loss ◽

Water Soluble ◽

Colloidal System ◽

Thaw Cycle ◽

Ostwald Ripening Mechanism

Psoriasis is an autoimmune disease in which the symptoms are obviously appeared on the patient's body with thick, red/ salmon colour and dry patches. Clinically, topical treatment has been the first-line treatment for psoriasis, whether or not the systemic and phototherapy is required. Currently, cyclosporine is one of the standard oral medications used for moderate to a severe case of psoriasis. However, through oral delivery, it cannot be used for a long period and causes bad effects. Thus, a new delivery system of cyclosporine is in need to be developed to overcome its toxic effects by skipping the first pass body metabolism. A nanoemulsion colloidal system, as the main carrier for big, non-water-soluble cyclosporine, is believed could help in the delivery of activities through the stratum corneum of the skin layer. Nanoemulsion system, which mainly consists of oil phase (a mixture of virgin coconut oil, nutmeg oil, and cyclosporine), aqueous phase, and surfactant, was successfully being developed by using Mixture Experimental Design optimization tool with droplet size range between 110-160 nm. Stability studies were carried out with respect to; pH, storage at different temperatures, coalescence and Ostwald ripening mechanism, free-thaw cycle, and FTIR analysis. From the obtained results, this newly-developed nanoemulsion containing cyclosporine was proven to be stable and successfully maintained its physicochemical characteristics even after 3 months of storage at 4°C and 25°C temperature. Ostwald ripening mechanism contributed to the instability of the system at 45°C of storage. Introduction of standard cyclosporine, blank nanoemulsion, and nanoemulsion containing cyclosporine to the HaCaT cells in the treatment of MTT assay study has confirmed the safety of the nanoemulsion. Permeation study of the newly-developed nanoemulsion containing cyclosporine showed it was best fitted the Korsmeyer-Peppas kinetic model. In addition, the transepidermal water loss and hydration studies proved the efficacy of cyclosporine-loaded nanoemulsion in increasing the water storage of the volunteers’ normal skin after 3h of application.

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Anticataract activity of pioglitazone by using in-Vitro goat lens model

Indian Journal of Pharmacy and Pharmacology ◽

10.18231/j.ijpp.2021.036 ◽

2021 ◽

Vol 8 (3) ◽

pp. 208-211

Author(s):

Rinkal R. Aware ◽

Hemant J. Pagar ◽

Ganesh D. Barkade ◽

Shweta Dhawane

Keyword(s):

Ascorbic Acid ◽

Protein Content ◽

Room Temperature ◽

Water Soluble ◽

Time Interval ◽

Lens Model ◽

Sodium Potassium ◽

Water Soluble Protein ◽

Varied Concentration

In the present study we have selected antioxidants agents like Pioglitazone and Ascorbic acid were subjected for anti-cataract activity by in vitro glucose induced cataract model. In the procedure, goat lenses was incubated along with the aqueous humor solution containing 55mM glucose with Enalpril as a standard compound and Pioglitazone with varied concentration for the time interval of 72 hours at room temperature. There was a formation of blur layer on the goat eyeball occurs after 10-12 hours and this process complete after 72 hours. The cataract inducing lenses showing higher level of Na, MDA (P<0.001) along with the decreases in sodium-potassium ATPase activity and water-soluble protein content. The goat lenses treated with Ascorbic acid 40 µg/ml and Pioglitazone in concentrations of 15, 30, and 60 µg/ml showed increased protein content and prevent the formation of cataract.

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Assessment of Drug Delivery Kinetics to Epidermal Targets In Vivo

The AAPS Journal ◽

10.1208/s12248-021-00571-3 ◽

2021 ◽

Vol 23 (3) ◽

Author(s):

M. Hoppel ◽

M. A. M. Tabosa ◽

A. L. Bunge ◽

M. B. Delgado-Charro ◽

R. H. Guy

Keyword(s):

Experimental Approach ◽

Input Function ◽

Drug Uptake ◽

Tape Stripping ◽

Healthy Human ◽

Topical Product ◽

Human Volunteers ◽

Dermal Pharmacokinetics

AbstractIt has proven challenging to quantify ‘drug input’ from a formulation to the viable skin because the epidermal and dermal targets of topically applied drugs are difficult, if not impossible, to access in vivo. Defining the drug input function to the viable skin with a straightforward and practical experimental approach would enable a key component of dermal pharmacokinetics to be characterised. It has been hypothesised that measuring drug uptake into and clearance from the stratum corneum (SC) by tape-stripping allows estimation of a topical drug’s input function into the viable tissue. This study aimed to test this idea by determining the input of nicotine and lidocaine into the viable skin, following the application of commercialised transdermal patches to healthy human volunteers. The known input rates of these delivery systems were used to validate and assess the results from the tape-stripping protocol. The drug input rates from in vivo tape-stripping agreed well with the claimed delivery rates of the patches. The experimental approach was then used to determine the input of lidocaine from a marketed cream, a typical topical product for which the amount of drug absorbed has not been well-characterised. A significantly higher delivery of lidocaine from the cream than from the patch was found. The different input rates between drugs and formulations in vivo were confirmed qualitatively and quantitatively in vitro in conventional diffusion cells using dermatomed abdominal pig skin.

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In Vitro and In Vivo Prolonged Biological Activities of Novel Vitamin C Derivative, 2-O-.ALPHA.-D-Glucopyranosyl-L-Ascorbic Acid (AA-2G), in Cosmetic Fields.

Journal of Nutritional Science and Vitaminology ◽

10.3177/jnsv.44.345 ◽

1998 ◽

Vol 44 (3) ◽

pp. 345-359 ◽

Cited By ~ 56

Author(s):

Yoshimaru KUMANO ◽

Tetsuo SAKAMOTO ◽

Mariko EGAWA ◽

Ichiro IWAI ◽

Muneo TANAKA ◽

...

Keyword(s):

Ascorbic Acid ◽

Vitamin C ◽

Biological Activities

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Co-Loading of Ascorbic Acid and Tocopherol in Eudragit-Nutriosomes to Counteract Intestinal Oxidative Stress

Pharmaceutics ◽

10.3390/pharmaceutics11010013 ◽

2019 ◽

Vol 11 (1) ◽

pp. 13 ◽

Cited By ~ 5

Author(s):

Maryam Rezvani ◽

Maria Letizia Manca ◽

Carla Caddeo ◽

Elvira Escribano-Ferrer ◽

Claudia Carbone ◽

...

Keyword(s):

Oxidative Stress ◽

Ascorbic Acid ◽

Protective Effect ◽

Natural Antioxidants ◽

Water Soluble ◽

Proliferative Effect ◽

The Stability ◽

Stress Damage ◽

Negative Zeta Potential

The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit® L100), a water-soluble prebiotic fibre (Nutriose® FM06), a phospholipid mixture (Lipoid S75), and two natural antioxidants (ascorbic acid and tocopherol) were combined to fabricate eudragit-nutriosomes by a simple, solvent-free procedure. The vesicles were spherical and oligolamellar, with some multicompartment structures in Eudragit-nutriosomes, small in size (~100 nm), with highly negative zeta potential. The effect of Eudragit® and Nutriose® on the stability on storage and in simulated gastrointestinal fluids were confirmed by the Turbiscan® technology and in vitro studies, respectively. Eudragit-nutriosomes exhibited a protective effect against H2O2-induced oxidative stress, and a proliferative effect in Caco-2 cells, as they provided the closure of the scratched area after 96 h of incubation.

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Nutritional and Anti Oxidant Potential of Commonly Growing Plant Foods from Southern India

Defence Life Science Journal ◽

10.14429/dlsj.5.13959 ◽

2020 ◽

Vol 5 (1) ◽

pp. 31-37

Author(s):

C. Rajendran ◽

S. KirtanaKirtana ◽

Rashmi Venkatesh ◽

Pooja Yadav ◽

Anilakumar Kandankath Raghavan

Keyword(s):

Ascorbic Acid ◽

Nutritional Composition ◽

Water Soluble ◽

Food Supplementation ◽

Nutrient Deficiencies ◽

Fruit Pulp ◽

Mineral Contents ◽

Curry Leaves

Certain varieties of plants are abundantly available with rich in nutrients, but the complete sets of nutritional composition studies have not been carried out. Among them, the matured leaves of Murrya keonigii; seeds and leaves of Moringa oleifera, and fruit pulp of Aegle marmelos were chosen. The proximate analysed for above samples showed that the moisture varies from 2.4% -8.2%, crude proteins from 18.75%- 34.57 %, fat content from 5.6% -19.6%, ash content from 3.87%-15.6% and carbohydrate from 28.65% - 41.23%, respectively. Estimation of mineral contents revealed that the leaves and seeds of moringa had higher concentrations than others. Determination of total antioxidant (total flavonoid) was higher (63.550 μg (RU)/ml of samples) in matured curry leaves than others. Determination of in vitro antioxidant activity with FRAP revealed highest activity in curry leaves (174.5μg) to a least activity with seeds of moringa (45.725 μg), whereas the DPPH revealed highest activity for fruit pulp of bael (1680.6μg ascorbic acid) to the least in leaves of moringa (263.15 μg ascorbic acid equivalent/mg). The ABTS showed IC50 value of 210.52 ±0.5774 for curry leaf, 487.8 ±0.3347 and 205.36 moringa seeds and leaves and 513.24 IC50 μg for pulp of bael fruit. Quantitative analysis of water soluble vitamins such as thiamine (B1) varied from 2.172 -5.558 mg; riboflavin (B2) from 2.201 -11.354 mg; pyridoxine (B6) from 4.608 -194.001 mg; biotin (B7) from 36.864 -153.027 mg, respectively. Further, the vitamin C (ascorbic acid) varied from 6.733 -23.142 mg /100g of oven dried samples, respectively. Therefore, the above foods are well intended to be included in routine diet regime and may also be willing to utilise for food supplementation with other suitable diets to manage the conditions such as malnutrition and nutrient deficiencies.

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Extraction, Purification, Bioactivities and Application of Matrix Proteins From Pearl Powder and Nacre Powder: A Review

Frontiers in Bioengineering and Biotechnology ◽

10.3389/fbioe.2021.649665 ◽

2021 ◽

Vol 9 ◽

Author(s):

Jingying Pei ◽

Yan Wang ◽

Xianguo Zou ◽

Huajun Ruan ◽

Changming Tang ◽

...

Keyword(s):

Matrix Protein ◽

Biological Activities ◽

Water Soluble ◽

Isolation And Purification ◽

Outer Corner ◽

Extraction And Purification ◽

Prism Layer ◽

The Mind

Natural pearls are formed when sand or parasites (irritants) accidentally enter into the oyster body and form pearls under the cover of the nacre layer. Pearl powder is a powdery substance by grinding pearls into small grains, however, the nacre powder is the inner layer of outer corner layer and middle prism layer. Pearl medicine in China has a history of more than 2,000 years, pearl has the effects of calming the mind, clearing the eyes, detoxifying the muscle and so on. In this paper, the researches on the extraction of pearl powder and nacre powder, the isolation and purification of matrix protein and the various biological activities (osteogenic activity, antioxidant, anti-inflammatory, anti-apoptotic, promoting the migration of fibroblasts, and so on) are reviewed in detail. To provide readers with a faster understanding, the method of extraction and purification and the application of nacre powder and pearl powder are clearly presented in the form of figures and tables. In line with the concept of waste or by-product, there are more reports of nacre extract than pearl extract, due to the expensive and limited in origin of pearls. Mainly on the direct use of nacre powder and pearl powder or on the use of extracts (mainly water soluble proteins) through experiments in vivo or in vitro, and shows whether it is effective through the results of various indexes. There is no further study on substances other than extracts, and the structural analysis of extracts needs further exploration.

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Antioxidant and Antisteatotic Activities of a New Fucoidan Extracted from Ferula hermonis Roots Harvested on Lebanese Mountains

Molecules ◽

10.3390/molecules26041161 ◽

2021 ◽

Vol 26 (4) ◽

pp. 1161

Author(s):

Zeinab El Rashed ◽

Giulio Lupidi ◽

Hussein Kanaan ◽

Elena Grasselli ◽

Laura Canesi ◽

...

Keyword(s):

Therapeutic Potential ◽

Biological Activities ◽

Radical Scavenging ◽

Bioactive Compound ◽

13C Nmr Spectroscopy ◽

Antioxidant Property ◽

Structural Features ◽

Water Soluble ◽

Cellular Models

Fucoidan is a fucose-rich sulfated polysaccharide with attractive therapeutic potential due to a variety of biological activities, including antioxidant action. Fucoidan is typically found in the cell wall of marine brown algae, but extra-algal sources have also been discovered. In the present work, for the first time we extracted a water soluble fucoidan fraction from the roots of the terrestrial shrub Ferula hermonis. This fucoidan fraction was termed FUFe, and contained fucose, glucose, sulfate, smaller amounts of monosaccharides such as galactose and mannose, and a minor quantity of proteins. FUFe structural features were investigated by FTIR, 1H NMR and 13C NMR spectroscopy. The antioxidant property of FUFe was measured by DPPH, ABTS and FRAP assays, which revealed a high radical scavenging capacity that was confirmed in in vitro cellular models. In hepatic and endothelial cells, 50 μg/mL FUFe could reduce ROS production induced by intracellular lipid accumulation. Moreover, in hepatic cells FUFe exhibited a significant antisteatotic action, being able to reduce intracellular triglyceride content and to regulate the expression of key genes of hepatic lipid metabolism. Altogether, our results candidate FUFe as a possible bioactive compound against fatty liver disease and related vascular damage.

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Nanoemulsion and Nanoliposome Based Strategies for Improving Anthocyanin Stability and Bioavailability

Nutrients ◽

10.3390/nu11051052 ◽

2019 ◽

Vol 11 (5) ◽

pp. 1052 ◽

Cited By ~ 17

Author(s):

Bing-Huei Chen ◽

Baskaran Stephen Inbaraj

Keyword(s):

Biological Activities ◽

Water Soluble ◽

Protective Effects ◽

Physicochemical Stability ◽

Acai Berry ◽

In Vitro Bioaccessibility ◽

Anthocyanin Stability ◽

Purple Sweet Potato ◽

Processing And Storage

Background: Anthocyanins, a flavonoid class of water-soluble pigments, are reported to possess several biological activities, including antioxidant, anti-inflammatory, and anti-cancer. However, anthocyanins are highly susceptible to degradation in high pH, light, heat, and oxygen during processing and storage. Conventional microencapsulation techniques fail to provide stability to anthocyanins under physiological environments mainly because of their large particle size as well as low zeta potential and encapsulation efficiency. Methods: Nanotechnology provides novel strategies for preparing nanoformulations to enhance the physicochemical stability of anthocyanins. Nanoemulsion and nanoliposome are the two most commonly used nanosystems in pharmaceutical and food-related fields. In this review, an overview of various nanoemulsion and nanoliposome systems reported recently for enhancing stability, bioavailability, and bioactivity of anthocyanins is presented. Results: Anthocyanin nanoemulsions with different oil, water, surfactant, and cosurfactant ratios were prepared from extracts of mangosteen peel, purple sweet potato, cranberry, red cabbage, blueberry, jaboticaba peel, and acai berry and evaluated for their antioxidant activity, enhancement of physicochemical stability, topical skin application, and urinary tract infection. Likewise, unilamellar and multilamellar nanoliposomes were prepared using different types and levels of lecithin without or with cholesterol from anthocyanin standards and extracts of Hibiscus sabdariffa, mulberry, elderberry, black carrot, and pistachio green hull for the evaluation of physicochemical and oxidative stability, in vitro bioaccessibility, and melanogenic activity, as well as protective effects against diabetes mellitus and cataract. Conclusion: This review provides an insight into the current nanotechnology updates on enhancement of anthocyanin stability and biological activity.

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