Β-hydroxy Acid Research Articles

Pharmacokinetics and Bioequivalence of Fixed-Dose Combination of Simvastatin and Ezetimibe Tablets: A Randomized, Crossover, Open-Label Study in Healthy Volunteers.

The current study aimed to evaluate the bioequivalence of a new generic combination of simvastatin and ezetimibe with the reference formulation. An open-label, randomized, 3-period, 3-sequence, crossover study, including 60 healthy volunteers, was implemented. Participants received the test and reference formulation, each containing 20mg of simvastatin and 10mg of ezetimibe as a single-dose tablet, separated by a minimum of 2-week washout periods. Blood samples were collected for 20 time points from predose to 72 hours after the dose. The total ezetimibe assay was carried out using a validated liquid chromatography-tandem mass spectrometry, while unconjugated ezetimibe, simvastatin, and simvastatin β-hydroxy acid determination was done via a validated ultra-performance liquid chromatography-tandem mass spectrometry. Each assay was preceded by a liquid-liquid extraction step. The pharmacokinetic parameters were derived using noncompartmental analysis and then compared between the reference and test formulations via a multivariate analysis of variance. No statistical difference was found in under the concentration-time curve from time 0 to the last quantifiable concentration and maximum concentration of unconjugated ezetimibe, total ezetimibe, and simvastatin between the reference and test formulations. The 90% confidence intervals of unconjugated ezetimibe, total ezetimibe, and simvastatin natural log-transformed under the concentration-time curve from time 0 to the last quantifiable concentration, and maximum concentration were in the range of 80%-125% as per the bioequivalence acceptance criteria. Therefore, the test formulation was bioequivalent to the reference formulation.

Incorporation of Multiple β2-Hydroxy Acids into a Protein In Vivo Using an Orthogonal Aminoacyl-tRNA Synthetase.

The programmed synthesis of sequence-defined biomaterials whose monomer backbones diverge from those of canonical α-amino acids represents the next frontier in protein and biomaterial evolution. Such next-generation molecules provide otherwise nonexistent opportunities to develop improved biologic therapies, bioremediation tools, and biodegradable plastic-like materials. One monomer family of particular interest for biomaterials includes β-hydroxy acids. Many natural products contain isolated β-hydroxy acid monomers, and polymers of β-hydroxy acids (β-esters) are found in polyhydroxyalkanoate (PHA) polyesters under development as bioplastics and drug encapsulation/delivery systems. Here we report that β2-hydroxy acids possessing both (R) and (S) absolute configuration are substrates for pyrrolysyl-tRNA synthetase (PylRS) enzymes in vitro and that (S)-β2-hydroxy acids are substrates in cellulo. Using the orthogonal MaPylRS/MatRNAPyl synthetase/tRNA pair, in conjunction with wild-type E. coli ribosomes and EF-Tu, we report the cellular synthesis of model proteins containing two (S)-β2-hydroxy acid residues at internal positions. Metadynamics simulations provide a rationale for the observed preference for the (S)-β2-hydroxy acid and provide mechanistic insights that inform future engineering efforts. As far as we know, this finding represents the first example of an orthogonal synthetase that acylates tRNA with a β2-hydroxy acid substrate and the first example of a protein hetero-oligomer containing multiple expanded-backbone monomers produced in cellulo.

Versatile capillary electrophoresis method for the direct chiral separation of aliphatic and aromatic α-hydroxy acids, β-hydroxy acids and polyhydroxy acids using vancomycin as chiral selector

Hydroxy acids (HAs) are ubiquitous in nature and play significant roles in various industrial and biological processes. Most HAs harbor at least one chiral center, therefore the development of efficient chiral analysis techniques for HA stereoisomers is of crucial importance across a wide range of fields. A capillary electrophoresis (CE) method was developed for the chiral analysis and quantification of aliphatic and aromatic α-hydroxy acid (AHA) enantiomers, aliphatic β-hydroxy acid (BHA) enantiomers and aliphatic polyhydroxy acid (PHA) stereoisomers. Using a modified partial filling-counter current method with indirect UV detection, high resolution (Rs) was achieved with vancomycin as a chiral selector added to the background electrolyte composed of 10 mM of benzoic acid/L-histidine at pH 5 using a polyacrylamide-coated capillary. This method could be readily applied to the determination of the enantiomers of 12 aliphatic AHAs, 4 aromatic AHAs, 3 aliphatic BHAs, as well as to the determination of the stereoisomers of tartaric acid, 2,3-dihydroxybutanoic acid, 2,3,4,5-tetrahydroxypentanoic acid, and 2,3,4,5,6-pentahydroxyhexanoic acid without the need for sample derivatization. Finally, our study provides a robust and versatile strategy for the chiral and stereoselective analysis of a broad range of hydroxy acid compounds.

A general photocatalytic strategy for the synthesis of β-hydroxy acid derivatives from alkenes

A general and concise strategy to realize the photo-induced difunctionalization of alkenes to access β-hydroxy acid derivatives is developed.

A pilot study examining a double-conjugated, retinoid-based skincare regimen for darker, blemish-prone skin.

Retinoids and alpha- and beta hydroxy acids are common components utilized in regimens for blemish-prone skin. However, balancing efficacy and tolerability is often challenging. This pilot study evaluated a double-conjugated retinoid serum specifically formulated for blemish-prone skin (AHARet-SA) in combination with exfoliating peel pads (double-conjugated retinoid, glycolic, lactic, and salicylic acids), a cleanser, mineral-based sunscreen, and a lightweight moisturizer in female participants with mild-to-moderate blemish-prone skin. Fifty-five percent of participants were Fitzpatrick Skin Type (FST) IV and 27% were FST V. Participants used the exfoliating peel pads (3x/week for 8 weeks; 2x/week for 4 weeks) followed by nightly AHARet-SA and a moisturizer (as needed). Improvements in skin were assessed using the 5-point Investigator Global Assessment Scale, and participant satisfaction and tolerability were assessed over 12 weeks. Significant mean improvement from baseline in skin clarity occurred after 4 weeks (14%; p = 0.04) with progressive improvements through week 12 (52%; p = 0.004). Eighty-eight percent of participants reported improvements in the appearance and texture of their skin and fewer blemishes/breakouts. Mild, transient adverse events were reported. A regimen comprised of a double-conjugated serum and exfoliating peel pads formulated for blemish-prone skin led to significant improvements from baseline in skin clarity after 12 weeks in participants with predominately darker skin tones and mild-to-moderate blemish-prone skin.

Dermal-Epidermal Junction Proteins: A Useful Target for Addressing Age-Related Changes in Facial Skin

Skin aging is a natural physiological process that occurs due to intrinsic and extrinsic factors. Intrinsic aging of the skin is a well-balanced genetic process affected due to degeneration of skin tissues, hormonal changes, and a natural inability to repair skin damage [1]. Extrinsic factors involve modifiable lifestyle and environmental factors such as smoking, pollution, poor nutrition, and prolonged sun exposure. These factors result in dry and thin skin, flattening skin, wrinkles, rough texture, and facial sagging [1]. The human desire to look young daily makes addressing these skin issues necessary. Conventional skin-care products based on retinol, hyaluronic acid, and alpha and beta hydroxy acids have been used for facial wrinkles and sagging. Increased pollution, exposure to toxins, and ultraviolet irradiations cause skin damage [2]. Previously, skin formulations were based on ascorbic acid, tocopherol, niacinamide, retinyl palmitate, anti-aging peptides, and proteins as topical solutions that reduce Reactive Oxygen Species (ROS) [3]. Currently, green cosmetic awareness has led to plant-based skin care products that include anti-aging properties and pharmacological actions such as anti-allergy, pro-collagen, anti-inflammatory and anti-carcinogenic, UV-protective [4]. The Dermal-Epidermal Junction (DEJ) is a distinct interconnective network complex between the dermis and epidermis that has multiple roles in skin homeostasis and function [5]. Hence, the commentary highlights the significance of dermal-epidermal junction proteins, specifically collagen IV, a target of a newly developed complex DL-linefade. It enhances the performance of niacinamide-based skin formulations by acting synergistically and inducing collagen IV biosynthesis.

Bilateral Symmetrical Oval Hyperpigmentation on the Face: A Case of Seborrheic Melanosis

Introduction: Seborrheic melanosis is one of the causes of facial hyperpigmentation presenting in the sebaceous areas of the face. It is most commonly seen in Fitzpatrick skin types 4 - 6. Seborrheic melanosis can cause cosmetic concerns for the patients, leading them to seek bleaching methods that could also be hazardous for them. Case Presentation: A 19-year-old male patient presented with dark brown spots on both sides of his nasolabial folds. According to the skin examination, there were nummular oval macules with hyperpigmentation and mild desquamation at the junction of the nasolabial fold and the supralabial area bilaterally. The patient applied an over-the-counter cream that contained hydroquinone to the hyperpigmented areas for bleaching for one month before he consulted our dermatology department. The pigmentation was homogeneous, brown-black, and showed no contrast under Wood’s light examination. Additionally, there were hyperpigmented macules on a seborrheic basement at the alar-supralabial junction bilaterally. The anamnesis and clinical findings supported the diagnosis of seborrheic melanosis. Tacrolimus ointment 0.1% once per night and isoconazole nitrate cream once per day were prescribed as treatments for one month. A water-based moisturizer and sunscreen were also added to the treatment. Further, he used a facial peeling combination of alpha-hydroxy acid 10% and beta-hydroxy acid 2% two times per week. Hyperpigmentation was barely discernible on his face five months after the beginning of the therapy. Conclusions: Seborrheic melanosis must be distinguished from other types of facial melanoses in order to start appropriate treatment. To ensure the most effective treatment, a comprehensive evaluation of the patient’s medical history and a thorough physical examination are essential for an accurate diagnosis of seborrheic melanosis.

Total synthesis, structure elucidation and expanded bioactivity of icosalide A: effect of lipophilicity and ester to amide substitution on its bioactivity.

The first total synthesis of icosalide A, an antibacterial depsipeptide that is unique in that it contains two lipophilic beta-hydroxy acids, has been achieved by following Fmoc solid-phase peptide synthesis in combination with solution-phase synthesis. The ambiguity in the absolute stereochemistry of icosalide A has been resolved by synthesizing the reported structures and other relevant diastereomers of icosalides and comparing their NMR data. NMR-based structure elucidation of icosalide A revealed a well-folded structure with cross-strand hydrogen bonds similar to the anti-parallel beta-sheet conformation in peptides and displayed a synergistic juxtaposition of the aliphatic sidechains. 12 analogues of icosalide A were synthesized by varying the constituent lipophilic beta-hydroxy acid residues, and their biological activities against Bacillus thuringiensis and Paenibacillus dendritiformis were explored. Most of these icosalide analogues showed an MIC of 12.5 μg mL-1 against both bacteria. Swarming inhibition by icosalides was least in B. thuringiensis (8.3%) compared to that in P. dendritiformis (33%). Furthermore, this is the first report of icosalides showing assured inhibitory action (MIC between 2 and 10 μg mL-1) against the active stage of Mycobacterium tuberculosis and cancer cell lines such as HeLa and ThP1. This study could help optimize icosalides for anti-TB, antibacterial, and anti-cancer activities.

Analysis of Salicylic Acid in Face Creams Circulating in the Big Market Malang City

Salicylic acid is a skin remedy that is used to treat various skin problems such as acne. Salicylic acid is safe to use and contains Beta Hydroxy Acid (BHA), which is an ingredient used to reduce wrinkles and acne. Although it has benefits for removing acne, salicylic acid is a dangerous chemical if used in excess of the prescribed limits. To determine the levels of salicylic acid in anti acne creams circulating in Pasar Besar Malang City, qualitatively with color test using FeCl3 and quantitatively using UV-Vis spectrophotometry to analyze levels of salicylic acid in anti-acne cream. Qualitative research using FeCl3 showed that from four samples, one sample was declared negative, while three positive samples contained salicylic acid, while testing using UV-Vis spectrophotometry found all samples containing salicylic acid. The levels of salicylic acid in all samples were within the safe limits set by BPOM with the highest level contained in skin surface products, including substances harmful to the skin, should not be more than 2%.

In-Vitro Efficacy Investigation and an Open-Label, Single-Arm Clinical Study of a Gentle Micropeeling Cream for Sensitive and Non-Sensitive Skin

Skin exfoliators, specifically alpha and beta hydroxy acids, have been shown to improve overall skin health and the clinical signs of aging. A micropeeling cream was developed with hydroxy acids and a brown algae extract and the efficacy and tolerability were evaluated in two parts. In the first part of the pre-clinical investigation, the micropeeling cream and the placebo control were evaluated by ELISA, immunostaining, qPCR and an activity assay using ex vivo and in vitro models. In the second part of the clinical efficacy study, 36 female subjects were enrolled for bioinstrumental measurements, visual imaging and clinical evaluation for 28 days. Fifty percent of subjects had sensitive skin. The ex-vivo study showed an increase in loricrin, superoxide dismutase 2, and extracellular matrix expression, without stimulating inflammatory biomarkers. The dermatologist observed a significant enhancement in all the parameters evaluated at day 28, and radiance, homogeneity, and roughness were significantly better after the first cream application. The homogeneity, desquamation and pore diameter showed significant improvement at day 7. The cream improved markers associated with skin aging and protection ex vivo. It was well tolerated, even on sensitive skin, and provided a significant improvement of fine lines, skin texture, and overall skin characteristics.

Feasibility of Reflectance Confocal Microscopy Monitoring in Oily, Acne-Prone Facial Skin Treated with a Topical Combination of Alpha and Beta-Hydroxy Acids, Anti-Inflammatory Molecules, and Herculane Thermal Water: A Blinded, One-Month Study.

Oily, acne-prone skin is a common skin type which may be monitored in vivo using reflectance confocal microscopy (RCM). The aim of the study was to assess the feasibility of RCM in evaluating the effectiveness of a topical combination of alpha- and beta-hydroxy acids, anti-inflammatory and antibacterial molecules, and Herculane thermal water on acne-prone skin. Thirty-five subjects with oily, acne-prone skin were prescribed topical combination products and were evaluated by clinical, Wood's lamp, and RCM imaging at baseline and after 28 days. At 28 days, the RCM-evaluated number of dilated infundibula, infundibula filled with keratotic material, and infundibula with thickened bright borders, as well as the density of the inflammatory infiltrate, were significantly decreased. Wood's light images at 28 days showed a significantly reduced number of C. acnes-colonized infundibula, and both the median area and the intensity of the red-orange fluorescence were decreased. The reduction in the clinical score was concurrent with the improvement in the RCM parameters, suggesting that this non-invasive imaging technique is appropriate for efficiency evaluations of topical acne treatments.

Synthesis of Pseudoboehmite Nanoparticles and Use in Simvastatin Drug Delivery

Pseudoboehmite is an aluminium compound with a structure similar to that of boehmite. The unit cell of the pseudoboehmite is slightly larger than that of the boehmite because of the greater incorporation of water in the same structure [1]. It has particles of nanometric dimensions and can be synthesized with extremely high purity. Several papers published in the literature show the potential of using this material in the controlled release of drugs, including cancer treatment [2,3]. Using drugs in complexes incorporated into polymer matrices and ceramic gels can lead to adequate control of gastrointestinal absorption when administered orally. Consequently, there is the possibility of promoting a gradual action through the progressive release of the drug, thus increasing its efficiency and reducing dose and toxicity. Previous studies have shown that pseudoboehmite is non-toxic and can be used for drug delivery. During the tests to determine the toxicity of this material, it was observed that the blood glucose content was reduced in mice that took pseudoboehmite by gavage. Since pseudoboehmite is obtained via low-cost inorganic synthesis, different physicochemical characteristics can be incorporated into this high purity medium. The formed structure was evaluated as a drug delivery system to establish a profile of the influence of the physicochemical properties of a molecule in the process of interaction with pseudoboehmite, a drug with recognized pharmacological activity, simvastatin (IUPAC name (1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl 2,2-dimethylbutanoate) was choose. It also emphasizes the importance of pseudoboehmite as a drug carrier, serving as a precursor to new therapeutic systems. The synthesis of pseudoboehmite from ammonium hydroxide and aluminium nitrate was optimized to release simvastatin in vitro. After absorption and hydrolysis in the liver to form the active β-hydroxy acid metabolite, simvastatin acts as a potent reversible, competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, an early and rate-limiting enzyme in the biosynthesis of cholesterol.

32245 Efficacy of superficial versus medium-depth peels: Quantitative and qualitative analysis

Chemical peeling is a common mode of facial restructuring that promotes the growth of new skin with increased collagen deposition, reduced scarring, and improved overall tone. Contemporary peels incorporate actives such as alpha or beta hydroxy acids, phenol, and trichloroacetic acid (TCA). TCA in particular has gained wide acceptance as a peeling agent; low levels of TCA present in “superficial peels’’ primarily target the stratum corneum and viable epidermis while higher levels present in “medium depth peels” demonstrate efficacy in the deeper dermis.

Electrocarboxylation of Aryl Epoxides with CO2 for the Facile and Selective Synthesis of β-Hydroxy Acids.

Herein, an efficient and facile approach to valuable β-hydroxy acid derivatives from readily available aryl epoxides and CO2 with high chemo- and regioselectivity under mild and sustainable electrochemical conditions is described. This approach showed broad substrate scope and good functional-group compatibility. In addition to aryl epoxides, four- to six-membered aryl cyclic ethers could all be tolerated in the reaction to provide synthetically useful hydroxy acids with high efficiency. Further late-stage carboxylation of complex molecules and drug derivatives demonstrated its potential application in the pharmaceutical industry. Mechanistic studies disclosed possible reaction pathways.

Severe Allergic, Inflammatory and Traumatic Reactions of the Vestibule Associated with Acquired Neuroproliferative Vestibulodynia

ABSTRACT Introduction The endodermal vestibule epithelial surface is very thin (∼ 50 um) and unlike the ectodermal vulva has no protective keratinized stratified squamous epithelium, therefore the vestibule is particularly susceptible to injury as a reaction to allergy, inflammation, or trauma. In some women these injuries result in excess mast cell and nerve accumulation in the vestibular epithelium and stroma, leading to neuroproliferative vestibulodynia (NPV). Acquired NPV is diagnosed by first obtaining a detailed history. Penetration must have initially been pain-free, followed by persistent entrance dyspareunia after exposure of the endodermal vestibule to: a topical agent causing a severe allergic reaction such as an antifungal vaginal cream; recurrent inflammatory conditions including vaginal candidiasis; or repeated blunt trauma, as with horseback riding. Acquired NPV is often observed in women with very sensitive genital skin. There are limited data regarding the various agents and conditions associated with acquired NPV. Objective The objective of this study was to examine the various agents and conditions that potentially caused NPV among our patients. Identification of iatrogenic or other topical triggers of NPV could inform both providers and the public of agents to potentially avoid applying these to the vestibule. Methods A retrospective chart review of women who underwent complete vestibulectomy for suspected NPV between June 2019 – November 2021 was performed. Inclusion criteria for this study: i) a history consistent with acquired NPV, ii) undergone vulvoscopy to rule out other forms of vestibulodynia, iii) a positive vestibular anesthesia test, iv) treatment by complete vestibulectomy with vaginal advancement flap, and v) a diagnosis of neuroproliferative vestibulodynia confirmed by immunohistochemical staining of excised vestibular tissue by CD117 and PGP9.5. Results A total of 47 charts were reviewed: 43% (n = 20, mean age 34 ± 15 years) had acquired NPV and met inclusion criteria; 57% (n = 27, mean age 28 ± 10 years) had congenital NPV. A history of entrance dyspareunia following a severe allergic reaction to a topical agent occurred in 12 women, the most common substance being topical miconazole (n=7, 58%). Other topical agents included a hotel shampoo (n=1), hair dye (n=1), lubricant (n=1), scented soap (n=1), and spermicide (n=1). Four (20%) reported recurrent inflammatory conditions including vaginal candidiasis treated with oral medication; four (20%) reported symptoms after blunt perineal trauma including a 30 fall from a waterfall (n=1), horseback riding (n=1), bicycle riding (n=1), and straddle injury (n=1). Eight patients (40%) reported having sensitive genital skin. Conclusions In our patient population, the most common agent triggering NPV was topical miconazole which contains inactive ingredients that may be associated with allergic reactions including: benzoic acid, beta hydroxy acid, peglicol 5 oleate, and pegoxol 7 stearate. Since the endodermal vestibule epithelium is thin without keratin, making it vulnerable to injury, topical agents to the vestibule, especially when it is inflamed, should be avoided and oral agents for inflammatory conditions be considered when appropriate. Women often purchase over the counter topical miconazole without knowledge of the potential side effects. Disclosure No

Effectiveness and safety of red yeast rice predominated by monacolin K β-hydroxy acid form for hyperlipidemia treatment and management.

To assess the lipid-lowering activity and safety of a dietary supplement containing monacolin K β-hydroxy acid form (MKA), Heye (), and Cangzhu (), compared to lifestyle modifications. Totally 117 subjects with moderate to severe dyslipidemia (according to Chinese guidelines) and low CV risk were randomly assigned into three treatment groups: lifestyle modification (LM), LM plus a low dosage of MKA, LM plus a high dosage of MKA, and treated for 60 d. The primary endpoint was the reduction of low density lipoprotein cholesterol (LDL-C) and total cholesterol (TC). Safeties along with Traditional Chinese Medicine Syndromes were assessed through the study. A low dosage of MKA along with lifestyle modifications caused a significant decrease in LDL-C by 15.6% on average (95% , 9.6% to 21%) with, a decrease in TC by 15.3% on average (95% CI, 9.26% to 21.4%), and a decrease in non-HDL-C by 35.4% (95% CI, 25.76% to 41.34%). Weak evidence of a reduction of triglycerides but an increment of HDL-C was observed in patients with severe hyperlipidemia. No severe adverse events occurred during the study. Our results confirm the LDL-C and TC lowering properties of MKA is clinically meaningful. It also produces a significant reduction of non-HDL-C, and slightly effects on TG and HDL-C as well.

Acne Information on Instagram: Quality of Content and the Role of Dermatologists on Social Media.

While it is evident that many patients turn to social media for information about skin care, the quality and content of available information are not well characterized. In this study, we investigated acne-related information available on Instagram, one of the most popular social media platforms. We searched for the “top” Instagram posts using the hashtag #acne and characterized them based on their source and content. Posts were excluded if they were unrelated, not in English, or duplicates. 900 posts were assessed, and 439 were included. A majority of the content (258 posts) was generated by influencers, followed by retailers (97) and non-dermatologist providers (67). Dermatologists were responsible for 17 posts, accounting for <4% of the included content. 124 separate ingredients were mentioned as potential acne treatments. The ingredients with the most mention were beta-hydroxy acids (eg, salicylic acid), alpha-hydroxy acids (eg, glycolic acid), vitamin C, niacinamide, and sunscreen. 254 posts recommended at least one specific intervention, and among these posts only 11% referenced a treatment with grade A evidence based on American Academy of Dermatology guidelines. A vast amount of content is readily available to patients on this platform. This content is heterogeneous in message and quality, and dermatologists are responsible for only a small portion of it. J Drugs Dermatol. 2022;21(3): doi:10.36849/JDD.6411.

Differential Oligomerization of Alpha versus Beta Amino Acids and Hydroxy Acids in Abiotic Proto-Peptide Synthesis Reactions.

The origin of biopolymers is a central question in origins of life research. In extant life, proteins are coded linear polymers made of a fixed set of twenty alpha-L-amino acids. It is likely that the prebiotic forerunners of proteins, or protopeptides, were more heterogenous polymers with a greater diversity of building blocks and linkage stereochemistry. To investigate a possible chemical selection for alpha versus beta amino acids in abiotic polymerization reactions, we subjected mixtures of alpha and beta hydroxy and amino acids to single-step dry-down or wet-dry cycling conditions. The resulting model protopeptide mixtures were analyzed by a variety of analytical techniques, including mass spectrometry and NMR spectroscopy. We observed that amino acids typically exhibited a higher extent of polymerization in reactions that also contained alpha hydroxy acids over beta hydroxy acids, whereas the extent of polymerization by beta amino acids was higher compared to their alpha amino acid analogs. Our results suggest that a variety of heterogenous protopeptide backbones existed during the prebiotic epoch, and that selection towards alpha backbones occurred later as a result of polymer evolution.

Eurotium cristatum produced β-hydroxy acid metabolite of monacolin K and improved bioactive compound contents as well as functional properties in fermented wheat bran

For the first time, wheat bran was fermented with Eurotium cristatum (E. cristatum), and alterations in the structural and functional characteristics were explored. The results showed that the soluble dietary fibre (SDF) content significantly increased in fermented bran, and the water and oil holding capacities improved. The total polyphenols, anthocyanin, and main flavour substance phenylethyl alcohol were significantly increased by E. cristatum fermentation. The ferulic acid content was approximately 12.06 times higher in fermented bran than in unfermented bran. These changes may be due to the release of hydrolytic enzymes during E. cristatum fermentation. E. cristatum fermentation enhanced the antioxidant and anti-obesity activities of bran. Furthermore, this study showing that E. cristatum fermentation produced β-hydroxy acid metabolites of monacolin K (MKA) in wheat bran. Thus, this research suggests that E. cristatum can be a starter culture to produce functional foods.

25154 Enhanced topical delivery of salicylic acid from an encapsulated system

Salicylic acid is a beta hydroxy acid that is clinically proven in the prevention and treatment of acne by encouraging skin exfoliation and unclogging of pores. Despite its bioactivity, the low water solubility of salicylic acid makes it challenging to formulate, and also limits its permeation into skin when applied topically. Various carrier-based delivery systems have been developed in recent years targeting either enhanced penetration for better efficacy, or controlled release for less side effect and long-lasting benefit. Among them, the multilamellar vesicle (MLV) delivery system encapsulates active ingredients in its onion-like structure; the individual “layers” peel off over time to provide deep and sustained active release. In this study, we compared the skin penetration of 2% salicylic acid from a topical gel with and without a specific MLV delivery system. Human skin explants were treated with the gel formulations for 24 hours in triplicates on a Franz diffusion cell setup. ATR-FTIR imaging was conducted on skin cross sections after the treatment. Unique spectrospopic signals (eg, 850 cm-1) were identified to monitor salicylic acid. The hyperspectral images revealed that a deeper and overall greater level (2-fold) of salicylic acid was delivered into skin through MLV encapsulation as compared with the control formula, which contains an equal amount of salicylic acid in free form. This proves that the MLV is an effective vehicle for topical delivery of salicylic acid.