Topical Treatment Of Acne Vulgaris Research Articles

Preparation, characterization, and in vitro evaluation of microemulsion based cream formulations for the topical treatment of acne vulgaris

AbstractBy lowering the significant adverse effects of traditional medications, this study intends to create cream formulations based on microemulsions that contain extract from Allium sativum L. for the treatment of acne vulgaris. Characterization experiments were carried out on the developed cream formulations based on microemulsions. Textural profile analysis and spreadability tests were conducted. Furthermore, cell culture studies and toxicity analysis were performed. As a result, the pH and viscosity values of the developed formulations were found between 6.43 ± 0.00 and 6.66 ± 0.01, and between 13.90 ± 0.080 and 137.20 ± 8.02 P, respectively. The highest‐performing empty and loaded cream formulations in terms of spreadability and textural profile analysis were those with the highest beeswax content. The highest‐performing empty and loaded cream formulations in terms of spreadability and textural profile analysis were those with the highest beeswax content. According to the visual physical evaluation of the formulations, it was observed that the developed formulations were neat, smooth, and homogeneous. The optimum formulation developed was non‐cytotoxic, which maintained cell viability by over 90%. Additionally, the skin irritation experiment was also non‐irritant with a relative cell viability of 92.6%. In conclusion, the developed A. sativum extract‐loaded microemulsion‐based cream formulations appear to be promising formulations for the acne vulgaris treatment, without malodors.

Exploring the efficacy of AHA–BHA infused nanofiber skin masks as a topical treatment for acne vulgaris

AbstractThis study investigates the efficacy of AHA–BHA infused nanofiber skin masks as a topical treatment for acne vulgaris. The skin is a vital organ that functions as a barrier to protect the body from external substances. In recent years, there has been a growing emphasis on skin treatment research. Hyaluronic acids (HAs) are commonly used in cosmetic and drug formulations to regulate excessive skin cornification, making them promising candidates for acne treatment. The introduction of HAs in dermatology has revolutionized the field of skin care, and they are used to treat various skin disorders, such as acne, ichthyosis, keratoses, warts, psoriasis, and photoaged skin. The antiaging benefits of HA have gained considerable attention in cosmetic dermatology, resulting in a surge in cosmetic products and skin care systems that contain HA. The study found that AHA–BHA‐infused nanofiber skin masks are effective in treating acne vulgaris. The nanofiber masks were found to reduce inflammation, sebum production, and acne lesions. The study suggests that AHA–BHA‐infused nanofiber skin masks could be a promising topical treatment for acne vulgaris.

Acne vulgaris and treatment with topical retinoids - adapalene and tretinoin

Introduction and purpose: Acne vulgaris is a disease that mainly affects young people and is associated with overactive sebaceous glands. The disease mainly affects the face but can also occur on the back. Depending on the clinical picture, we can distinguish different types of acne and make our treatment dependent on it. The aim of the study will be to compare the effects of topical retinoids on acne vulgaris. State of knowledge: Topical retinoids have a direct anti-inflammatory effect and prevent the formation of blackheads and microcomedones. Five retinoids are currently available for topical treatment of acne vulgaris. We distinguish three generations. The mechanism of action is not fully understood, but it is known that they react with the RAR and RXR receptors. In the review paper, we will compare the effects of adapalene with tretinoin. Conclusion: According to the indicated study results, there is no significant difference in the effect of treatment with adapalene or tretinoin. Adapalene showed less irritation during treatment than tretinoin. The most important thing during acne treatment is choosing the right concentration and formulation by the dermatologist so that the patient does not stop treatment.

Topical treatment of acne vulgaris: Endolift® direct optical energy combined with LIGHTSCAN™ fractional laser

This study evaluated the efficiency of a novel minimally invasive outpatient laser procedure, Endolift®, which destroys sebaceous glands with the combination of LASEmaR® 1500 and LIGHTSCAN™ - a fractional, non-ablative laser treatment. Thirty patients with acne vulgaris moderate to severe of both sex were treated, ranging from 18 to 35 years old; 70% had moderate and severe acne, and 30% had moderate acne. Only one session was performed of 200 microns of laser fibre inserted under the skin without anaesthesia. Eufoton® LASEmaR® 1500 works at a wavelength of 1470 nm. Three patients reported acne eruptions between 7 to 10 days after the treatment, which resolved in a few days; 70% of patients reported improvements after 3 to 4 weeks, and over time it has been going on to improve; the number of acne was significantly reduced, and the inflammation was superficial. Thirty% of patients reported improvements after 45 days. The final result is seen after 9 months; until then, we can expect gradual improvement. For 65% of the patients, one session was enough, with recommended measures to keep acne under control; for the 35%, we used 2 to 3 treatments based on LIGHTSCAN™ to keep acne under control. Patients reported a reduction in skin pores and an improvement in skin quality. There was no downtime and any side effects. In this study, patients with moderate to severe acne undergo 1 to 3 treatments based on direct optical energy reporting reduction of acne and skin inflammation.

Tretinoin 0.1% and Benzoyl Peroxide 3% Cream for the Treatment of Facial Acne Vulgaris.

To assess the efficacy, safety, and clinical application of tretinoin 0.1%-benzoyl peroxide 3% cream for the topical treatment of acne vulgaris. A systematic review of the literature was performed using the terms Twyneo OR tretinoin and benzoyl peroxide OR S6G5T-3 in MEDLINE (PubMed) and EMBASE. ClinicalTrials.gov was searched to obtain completed clinical trial results not published elsewhere. All human studies published in English prior to November 2022 related to pharmacology, clinical trials, safety, and efficacy were evaluated for inclusion. In two 12-week, phase 3, randomized, vehicle-controlled clinical trials, tretinoin 0.1%-benzoyl peroxide 3% cream significantly reduced inflammatory and noninflammatory facial acne lesions and significantly improved Investigator Global Assessment (IGA) rating to clear or almost clear. The cream has a suitable safety profile, with application site pain and dryness as the most common adverse events. Tretinoin-BPO had similar IGA success compared to other topical retinoid and retinoid-BPO treatments for acne vulgaris. Compared to individual tretinoin and benzoyl peroxide therapy, the combination product streamlines application, which will improve medication adherence; however, the cost of tretinoin-BPO cream may be prohibitive. Tretinoin 0.1%-benzoyl peroxide 3% cream is safe and effective for the treatment of moderate-to-severe acne. Long-term trial data on efficacy and tolerability are not yet available.

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

Tretinoin (TRE) is, for its anti-comedogenic and comedolytic activity, widely used in the topical treatment of acne vulgaris. The effect lies in the regulation of sebum production and collagen synthesis. The study is devoted to the formulation of dermal gels containing TRE using microemulsion as the drug solubilizer. The aim was to evaluate the effect of the reference microemulsion (ME) and lecithin-containing microemulsion (MEL) on the release of TRE through the synthetic membrane (in vitro) and the pig's ear skin (ex vivo) through the Franz cell diffusion method. Subsequently, after an ex vivo study, the amount of the drug in the skin influenced by the applied formulation was determined. In addition, the impact of ME on the microscopic structure, texture, and rheological properties of gels was evaluated. On the basis of the analysis of texture, rheological properties, and drug release studies, Carbopol formulations appear to be more appropriate and stable. Considering the synthetic membrane as a stratum corneum, the Carbopol gel penetrated about 2.5-higher amounts of TRE compared to the Xanthan gel. In turn, ex vivo studies suggest that MEL slows the drug transfer to the dissolution medium, simulating absorption into the blood, which is a desirable effect in local treatment. The drug retention study proved the highest amounts of TRE in the skin to which microemulsion-Carbopol formulations were applied. The results confirm the benefit of TRE solubilization in ME due to its bioavailability from the tested dermal formulations.

Development and characterization of the electrospun melittin-loaded chitosan nanofibers for treatment of acne vulgaris in animal model

Acne is an inflammatory disease of the sebaceous glands. Melittin (Mel) is one of the principal toxic components of bee venom that can cause antibacterial and anti-inflammatory effects. Chitosan is a biodegradable polysaccharide has anti-inflammatory, antimicrobial, and regenerative properties. In this study, chitosan (Ch)/Mel 0.001 and 0.003% nanofibers were fabricated for topical treatment of acne vulgaris. Physicochemical properties of Ch/Mel were evaluated using FTIR and FESEM. Furthermore, encapsulation efficiency, tensile strength, water absorption capacity, enzymatic activity, drug release, antimicrobial, and cell cytotoxicity were assayed. Animal models were exerted to study the impact of Ch/Mel nanofibers on the treatment of Propionibacterium acnes. The FESEM results showed that nanofibers were successfully prepared in nano-scale fiber diameter. The FTIR confirmed the presence of Mel in structures. The addition of melittin to the polymer solution reduced electrical conductivity, induced viscosity and tensile strength of the fibers, and decreased the percentage of the swelling. The Mel loading into Ch/Mel 0.003% was reported at 86.74±1%. This Mel releasing process (89.65%) of Ch/Mel 0.003% was slowly completed during 72 h. The Mel retained its hemolytic activity after being loaded into the polymer structure. The drug toxicity study displayed the lack of any significant toxicity from Ch/Mel nanofibers on normal Human Dermal Fibroblasts (HDF). The Ch/Mel 0.003% achieved the highest growth inhibition in P. acnes in vitro and animal studies, this group showed the greatest reduction in inflammation and redness. The Ch/Mel 0.003% structure is proposed as a suitable topical drug delivery system for treating acne vulgaris.

A review article on Winlevi

<p class="abstract">Acne is a most common multiform skin condition. Androgen plays a major role in acne pathogenesis in both males and females. The appliance of anti-androgen is potentially effective. However, anti-androgens for topical application are not available in market. Clascoterone (cortexolone 17α propionate), an ester derivative of cortexolone is an androgen receptor inhibitor developed as a topical cream and solution for the treatment of androgen dependent skin disorders, including acne vulgaris. Although the mechanism of action of clascoterone (Winlevi) for topical treatment of acne vulgaris is not known. In 2020 clascoterone 1% has been first approved by United States of America (USA) for the topical therapy of acne vulgaris people aged 12 years or above. Assessment of acne is done based on overall severity of acne based on grades- grade 0, grade 1, grade 2, grade 3, and grade 4 (clear- severe). Both inflammatory on non-inflammatory lesions were counted. Treatment success is achieved when the grade or score is clear or almost clear. Clascoterone cream is well tolerated with no significant clinical safety issues. Clascoterone 1% twice daily treatment have the most effective favourable results with low adverse events. Currently first line treatment targeting aspects of acne includes benzyl peroxide topical or oral antibiotics, topical retinoid. Females with acne is treated with combined oral contraceptives (e. g. norgestimate and norethindrone are approved by FDA for treatment of acne in females) or spironolactone which affects androgens. Androgen receptors are present throughout the skin and found in sebaceous glands, dermal cells, and sebocytes. Androgen inhibiton is an effective way for treatment of acne in females.</p>

Mechanistic support of traditional Persian medicine for the treatment of acne vulgaris: A scoping review.

Acne vulgaris is one of the most prevalent skin diseases, which also contributes to many psychological problems. Despite the recent progress in the treatment of acne vulgaris, the necessity for discovering more effective solutions has motivated many lines of research on natural and medicinal plants. The Traditional Persian Medicine (TPM) introduced some plants and remedies for acne treatment. Given the universal welcome for herbal medicine, this review was performed to formally assess the evidence for herbal medicines for acne vulgaris in TPM. The medicinal plants used in this study for treating acne vulgaris were selected based on common references to the plants in five famous textbooks of TPM from different time periods. Then, the anti-inflammatory and anti-microbial effects of these medicinal plants were investigated according to the recent literature available in five electronic databases including Scopus, Web of Sciences, PubMed, Google Scholar, and Science Direct. Twenty-one herbs were commonly references in traditional TPM texts as helpful for topical treatment of acne vulgaris. The data collected from the electronic databases demonstrated most of these plants (eg, Astragalus sarcocolla, Ficus carica, and Hordeum vulgare) have both anti-inflammatory and anti-microbial mechanisms, which may assist to treat acne vulgaris. This scoping review demonstrated many medicinal plants recommended by TPM books have therapeutic potential for acne vulgaris via multiple mechanisms.

Clascoterone: a new topical anti-androgen for acne management.

Clascoterone is an androgen receptor inhibitor which has been approved by the United States Food and Drug Administration for the topical treatment of acne vulgaris in patients 12 years of age and older. It competes with androgens, especially dihydrotestosterone, for androgen-receptor binding and limits their binding, thus inhibiting downstream signaling of pathways involved in the pathogenesis of acne. It inhibits androgen receptor-regulated gene transcription, and antagonizes lipid and inflammatory cytokine production in a dose-dependent manner in human primary sebocytes. Clascoterone is commercially available as 1% (10 mg/g) cream. Adverse effects of topical clascoterone are mild and infrequent, and are mostly limited to local skin reactions. Long-term safety studies have shown an absence of systemic antiandrogenic effects like reduced libido or feminization in male participants. Clascoterone seems a promising topical drug with a novel mechanism of action that could be added to the armamentarium of therapies for acne.

Oral isotretinoin treatment in patients with acne vulgaris during the COVID-19 pandemic: A retrospective cohort study in a tertiary care hospital.

BackgroundPatients with acne vulgaris continue to present increasingly in dermatology outpatient clinics and seek treatment during the COVID‐19 pandemic. As far as we know, the effect of isotretinoin on COVID‐19 has not been studied before.AimWe aimed to evaluate whether patients receiving oral isotretinoin are at increased risk of COVID‐19 infection by comparing them with patients on topical treatment for acne vulgaris.MethodsThe data were collected retrospectively from a cohort of 267 acne vulgaris patients, who were under follow‐up for acne vulgaris treatment during the pandemic period.ResultsTotal of 227 patients (141 receiving isotretinoin treatment and 86 receiving topical treatment) were included of whom 29 patients had COVID‐19 infection during acne vulgaris treatment. Fifteen (10.6%) patients were receiving oral isotretinoin and 14 (16.3%) were receiving topical acne treatment at the time of COVID‐19 infection. The mean cumulative dose was 2340 ± 1988 mg at the time of COVID‐19 infection. The mean elapsed time between the onset of isotretinoin treatment and positive PCR result for COVID‐19 was 13.3 ± 10.3 weeks. Nine patients (64.3%) receiving isotretinoin treatment and 9 patients (60%) under topical treatment had loss of taste and smell during COVID‐19 infection. Isotretinoin treatment was not found to be associated with a significant increased risk of getting COVID‐19 (odds ratio, 0.671; 95% confidence interval, 0.247–1.823; P = 0.434).ConclusionAs a conclusion, the results of this study encourage dermatologists and acne vulgaris patients to initiate oral isotretinoin treatment safely during the pandemic period.

Clascoterone 1% cream in acne vulgaris: a profile of its use

Clascoterone 1% cream (WINLEVI®) is an androgen receptor inhibitor approved for the topical treatment of acne vulgaris in patients aged ≥ 12 years in the USA. It is believed to compete with androgens (specifically Dihydrotestosterone) in binding to androgen receptors, thereby inhibiting downstream signaling of acnegenic pathways. In clinical trials, application of clascoterone 1% cream twice daily for 12 weeks was effective and generally well tolerated in acne vulgaris patients, with a tolerability profile similar to that of the vehicle.

Subclinical effects of adapalene-benzoyl peroxide: a prospective in vivo imaging study on acne micromorphology and transfollicular delivery.

Adapalene-benzoyl peroxide (A-BPO) is a first-line topical treatment for acne vulgaris. In vivo reflectance confocal microscopy (RCM) and optical coherence tomography (OCT) detect micromorphological changes over time and visualize transfollicular delivery. To visualize temporal, subclinical effects of A-BPO on acne micromorphology using RCM and OCT, and evaluate their impact on transfollicular delivery of microparticulate carrier systems. Fifteen patients with mild to moderate acne received a 6-week course of A-BPO. Micromorphological changes were evaluated at time 0, 3 and 6weeks with RCM (n=1190 images) and OCT (n=210 scans). Transfollicular delivery of microparticles was assessed at baseline and week 6. In vivo imaging visualized steady normalization of skin micromorphology in response to A-BPO over 6weeks, including decreased hyperkeratinization of follicular borders (RCM median decrease -71.2%, P<0.05), reduced intrafollicular keratinous content (RCM median decrease -47.7%, P<0.05) and increased epidermal thickness (OCT median increase of 25.25%, P<0.05). Imaging visualized microparticles in the follicular unit. Despite a visible reduction in keratin and sebum, transfollicular microparticle delivery appeared unaffected. Reflectance confocal microscopy and OCT detect A-BPO-induced changes in micromorphology and visualize transfollicular microparticle delivery. Keratolysis and sebolysis did not have a measurable effect on transfollicular delivery of microparticles.

Fabrication and Characterization of Multiple Herbal Extracts-loaded Nanofibrous Patches for Topical Treatment of Acne Vulgaris

Herbal extracts have recently received considerable interest in acne therapy owing to their enhanced skin compatibility compared with antibiotics and synthetic agents. In this study, electrospun poly (vinyl alcohol)/chitosan (PVA/CS) fibrous patch incorporating a combination of herbal extracts with complementary mechanisms of action was developed as an alternative acne therapy for patients with resistance to the conventional treatments. The herbal extracts-loaded electrospun fibers displayed uniform and smooth-surfaced nanofibers (dia. 100–300 nm), high drug loading efficiency (89.5–97.7 %) and good water absorbing properties. Results of the in vitro release and antibacterial studies suggest the patches are capable of sustained release of polyphenol-rich extracts, which may, together with the chitosan present in the fiber, endow the patch with potent bacterial inhibition of Propionibacterium acnes. The herbal extracts-loaded patches exhibited pronounced clinical therapeutic efficacy in treating mild-to-moderate facial acne by rapidly reducing inflamed lesions and restoring epidermal barrier. Also, the herbal patches demonstrated improved biocompatibility or tolerability in comparison with the synthetic drug benzoyl peroxide. Overall, the present study has provided a facile approach to develop biocompatible polymers based electrospun fibrous patch for the efficient delivery of herbal extracts for topical skin therapy, opening new perspectives for a new generation of cosmetotextiles.

Targeted clindamycin delivery to pilosebaceous units by chitosan or hyaluronic acid nanoparticles for improved topical treatment of acne vulgaris

We developed chitosan or hyaluronic acid nanoparticles to entrap clindamycin and evaluated for the first time the impact of these two polymeric nanosystems on the targeted drug delivery to the pilosebaceous units, considering the sebaceous characteristics of skin affected by acne. Chitosan and hyaluronic acid nanoparticles respectively presented diameters of 362 ± 19 nm and 417 ± 9 nm (PDI < 0.47), entrapped 42 % and 48 % of the clindamycin content (drug loading of 8.8 % and 0.5 %) and had opposite surface charges (+27.7 ± 0.9 mV and -30.2 ± 2.7 mV). Although only the hyaluronic acid nanoparticles showed increased deposition of the drug into the pilosebaceous structures, both nanoparticles revealed enhanced targeted delivery of clindamycin to these structures as compared to commercial formulation (53 ± 20 % and 77 ± 9% of the total drug that penetrated the skin was found on the pilosebaceous units from, respectively, chitosan and hyaluronic acid nanoparticles). Remarkably, the “targeting potential” of the nanoparticles was more pronounced when the skin was pretreated to simulate a sebaceous condition. In conclusion, both polymeric nanocarriers targeted drug delivery to the pilosebaceous structures at different extensions and, in the case of oily skin conditions, such targeting was increased.

Clascoterone: First Approval.

Clascoterone (Winlevi®) is an androgen receptor inhibitor being developed as a topical cream and solution by Cassiopea (a spin-out company of Cosmo Pharmaceuticals) for the treatment of androgen-dependent skin disorders, including androgenetic alopecia and acne vulgaris. Although the exact mechanism of action of clascoterone for the topical treatment of acne vulgaris is unknown, the drug is believed to compete with the androgen dihydrotestosterone for binding to androgen receptors in the sebaceous gland and hair follicles to attenuate signalling necessary for acne pathogenesis. In August 2020, clascoterone cream 1% received its first approval in the USA for the topical treatment of acne vulgaris in patients 12years of age or older. Clinical studies of a different formulation of clascoterone (a solution containing a higher concentration of the drug) for the treatment of androgenetic alopecia are underway in Germany and the USA. This article summarizes the milestones in the development of clascoterone leading to this first approval for the topical treatment of acne vulgaris.

A retrospective assessment and comparison of the effectiveness of benzoyl peroxide; the combination of topical niacinamide, gallic acid, and lauric acid; and the combination of benzoyl peroxide and erythromycin in acne vulgaris.

Acne vulgaris is a chronic inflammatory skin disease that mostly develops during adolescence and continues throughout adulthood. It affects the face, the main location of cosmetic appearance. Despite many developments in acne treatment, various combination therapies are needed to create the best option. Ninety patients were included in this study. We used the global acne grading system (GAGS) and the lesion counting and photographic standards that were used by Hayashi et al., to assess acne severity. The patients were randomly divided into three groups as group 1 (using only 5% BPO, twice a day), group 2 (using only the combination of 5% BPO + 3% erythromycin, twice a day), and group 3 (using only the combination of 4% niacinamide + 1% gallic acid + 1% lauric acid, twice a day). Thirty patients were included in each group. The scores were evaluated at weeks 0, 2, 4 and 8, and compared with each other. As a result of the study, all three treatment types were found to be effective. The combination of 4% niacinamide + 1% gallic acid + 1% lauric acid can be used as an alternative topical treatment for acne vulgaris to prevent resistance against topical antibiotics and the side effects of some other treatments.

Trifarotene: First Approval.

Topical trifarotene (Aklief®) is a first-in-class, fourth-generation retinoid [selective retinoic acid receptor (RAR)-γ agonist] being developed by Galderma Research and Development LLC for the treatment of acne vulgaris. In October 2019 trifarotene received its first global approval in the USA for the topical treatment of acne vulgaris in patients 9years of age and older. This article summarizes the milestones in the development of trifarotene leading to its first global approval for acne vulgaris.

Development and Evaluation of Particulate Microcarriers of Adapalene as a Topical Delivery System

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.

Topical treatment of acne vulgaris: efficiency, side effects, and adherence rate.

ObjectiveAdherence is a problem in the topical treatment of acne. This study was designed to evaluate the efficiency of current topical treatment and adherence in patients.MethodsPatients with acne vulgaris who had recently been prescribed a topical therapy were selected. A dermatologist-directed questionnaire was completed. Demographic data, acne severity, treatment and the manner of use, side effects, and reason for discontinuation were recorded.ResultsA total 250 patients were included, 178 female (71.2%) and 72 male (28.8%) participants, mean age was 18.6 ± 2.8 years. Of 250 patients, 114 (45.6%) had given up therapy for two reasons: unresponsiveness in 71 (62.3%) and side effects in 43 (37.7%) patients. For antibacterial treatments, the rate of unresponsiveness was higher but the rate of side effects was lower. Discontinuation owing to unresponsiveness was higher in patients with severe acne. Side effects were higher in patients with comedonal-type acne. The lowest rates of side effects and discontinuation were among every-other-night users.ConclusionIn this study, patients with acne gave up treatment owing to side effects and unresponsiveness, which reduced the treatment efficiency.