Topical Treatment Of Acne Research Articles

Development and Evaluation of Dapsone Loaded Topical Liposomes

Topical liposomal drug delivery is becoming promising system with several advantages like skin deposition, controlled release, targeted action and reduced drug quantity etc. Topical treatments are used for various diseases and disorders. Acne vulgaris is a worldwide skin disease. For acne treatments oral, injectable routes are used but topical route is the better route for site delivery. Dapsone, as antibacterial and anti-inflammatory drug has been recommended in topical acne treatment. Multilamellar vesicles (MLV) of dapsone were prepared using conventional thin film hydration method. Optimization techniques were used to determine, formulation with high drug entrapment efficiency and optimum vesicle size. Soya lecithin and cholesterol were used as independent variables. The prepared liposomes were characterized for size, shape, entrapment efficiency, zeta potential, in-vitro drug release (by Franz diffusion cell) and skin deposition. Maximum entrapment was found to be 33.44%. In skin permeation study, liposomal gels resulted in significantly slower drug release than equivalent plain gels. Liposomal gels were found to have 2-3 fold increase in the skin deposition than plain gel, indicating liposome forms depots in skin layers and thus providing a better option to deal with skin-cited acne vulgaris. Amongst different storage conditions (kept for 2 months), the liposomes stored at 2 to 8 °C were found to be most stable, as compare to room temperature and 45 °C.

Formulation of tretinoin-loaded topical proniosomes for treatment of acne: in-vitro characterization, skin irritation test and comparative clinical study

Tretinoin (TRT) is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Therefore, the aim of this study was the development of TRT-loaded proniosomes to improve the drug efficacy and to increase user acceptability and compliance by reducing its side effects. Nine formulae were prepared according to 32 factorial design and were evaluated for their morphology, vesicle size, entrapment efficiency (EE %), and% of drug released after 5 h. Hydrogel of the candidate formula, N8G (proniosomes prepared with 0.025% TRT, and Span60: cholesterol molar ratio of 3:1 and incorporated in 1% carbopol gel) was developed and evaluated for skin irritation test and clinical study in acne patients compared to marketed product. Candidate formula showed higher efficacy and very low irritation potential when compared to marketed product in human volunteers.

Treatment failure of patients using topical acne treatments: An observational retrospective cohort study

Treatment failure of patients using topical acne treatments: An observational retrospective cohort study

Systematic review on the rapidity of the onset of action of topical treatments in the therapy of mild-to-moderate acne vulgaris

The time until a patient achieves a relevant improvement during the treatment of a skin disease is important for selecting a therapy, but has been largely neglected in reviews and guidelines. The aim of this systematic review was to determine the time until the onset of action (TOA) of topical acne treatments. The primary outcome was the TOA defined as the time until a 25% reduction in the mean number of inflammatory lesions had been achieved. A systematic literature search in Medline and Embase was carried out. Clinical trials that evaluated head-to-head comparisons of treatments in patients suffering from mild-to-moderate papulopustular acne were included. Abstract and full-text screening and data extraction were done independently by two investigators. With respect to inflammatory lesions, different concentrations of benzoyl peroxide (BPO) or adapalene did not seem to influence the TOA. BPO seemed to act more quickly than isotretinoin and tretinoin. Adapalene showed a shorter TOA than isotretinoin. Conflicting results were seen when comparing adapalene with tretinoin, with a tendency for adapalene to be faster. Clindamycin/BPO seemed to act more quickly than adapalene. Inconsistent results were seen for the comparison of clindamycin/BPO and BPO alone with a slight indication of a shorter TOA for clindamycin/BPO. Adapalene/BPO and clindamycin/BPO showed comparable TOA. When interpreting the data, the different study designs and the limited study quality need to be taken into account. Further research is needed to identify treatments that offer an early onset of action and possibly help to optimize patients' adherence. TOA should be considered as an additional outcome in acne trials.

Carrier-based drug delivery system for treatment of acne.

Approximately 95% of the population suffers at some point in their lifetime from acne vulgaris. Acne is a multifactorial disease of the pilosebaceous unit. This inflammatory skin disorder is most common in adolescents but also affects neonates, prepubescent children, and adults. Topical conventional systems are associated with various side effects. Novel drug delivery systems have been used to reduce the side effect of drugs commonly used in the topical treatment of acne. Topical treatment of acne with active pharmaceutical ingredients (API) makes direct contact with the target site before entering the systemic circulation which reduces the systemic side effect of the parenteral or oral administration of drug. The objective of the present review is to discuss the conventional delivery systems available for acne, their drawbacks, and limitations. The advantages, disadvantages, and outcome of using various carrier-based delivery systems like liposomes, niosomes, solid lipid nanoparticles, and so forth, are explained. This paper emphasizes approaches to overcome the drawbacks and limitations associated with the conventional system and the advances and application that are poised to further enhance the efficacy of topical acne formulations, offering the possibility of simplified dosing regimen that may improve treatment outcomes using novel delivery system.

Nano-lipoidal carriers of tretinoin with enhanced percutaneous absorption, photostability, biocompatibility and anti-psoriatic activity

Tretinoin (TRE) is a widely used retinoid for the topical treatment of acne, psoriasis, skin cancer and photoaging. Despite unmatchable efficacy, it is associated with several vexatious side effects like marked skin erythema, peeling and irritation, eventually leading to poor patient compliance. Its photo-instability and high lipophilicity also pose challenges in the development of a suitable topical product. The present study, therefore, aims to develop biocompatible lipid-based nanocarriers of TRE to improve its skin delivery, photostability, biocompatibility and pharmacodynamic efficacy. The TRE-loaded liposomes, ethosomes, solid lipid nanoparticles (SLNs) and nanostructured lipidic carriers (NLCs) were prepared and characterized for micromeritics, surface charge, percent drug efficiency and morphology. Bioadhesive hydrogels of the developed systems were also evaluated for rheological characterization, photostability, ex vivo skin permeation and retention employing porcine skin, and anti-psoriatic activity in mouse tail model. Nanoparticulate carriers (SLNs, NLCs) offered enhanced photostability, skin transport and anti-psoriatic activity vis-à-vis the vesicular carriers (liposomes, ethosomes) and the marketed product. However, all the developed nanocarriers were found to be more biocompatible and effective than the marketed product. These encouraging findings can guide in proper selection of topical carriers among diversity of such available carriers systems.

Evaluation of a New Topical Treatment for Acne with Azelaic Acid-Loaded Nanoparticles

Azelaic acid, a saturated dicarboxylic acid, is used in the treatment of acne. However, some side effects and low patient compliance have been associated with several topical formulations of azelaic acid. Thus, nanotechnology presents an innovative strategy that can overcome these problems. Polymeric nanoparticles are generally applied to control drug release and to reduce local drug toxicity. In this study, we used the polymer PLGA (acid poly (DL-lactic-co-glycolic)) which is a biocompatible and biodegradable polymer that provides a slow and controlled drug release. The aim of this study was to evaluate a new topical treatment for acne with azelaic acid-loaded PLGA nanoparticles in terms of size, surface charge, encapsulation efficiency, morphology, drug-polymer interactions, efficacy, toxicity and safety of excipients.Nanoparticles were produced by a modified spontaneous emulsification/solvent diffusion method and included into a gel of carbopol 940. Size and zeta potential were determined by photon spectroscopy and electrophoretic mobility, respectively. Efficiency encapsulation was accessed by HPLC analysis using an adaptation of a previously described method. Loaded and blank nanoparticles morphology was observed by SEM. Drug-polymer interactions and thermal characteristics were evaluated by DSC. Staphylococcus epidermidis and Propionibacterium acnes susceptibility to the azelaic acid-loaded nanoparticles were tested by the broth microdilution method (efficacy test) and the minimum inhibitory concentration (MIC) values were determined using vancomycin as a positive control. The cytotoxicity of the nanoparticles was investigated on a Saccharomyces cerevisiae model. Excipients safety was accessed by occluded patch tests in humans (blank nanoparticles). The tests were performed in 12 healthy, female volunteers with skin type II whose ages were in between 22-38 years. All the tests were carried out according to the Declaration of Helsinki and received the approval of local Ethical Committee.Nanoparticles formed a soft white powder (Figure 1A). The loaded nanoparticles mean size was 378.63±60.86 nm (0.09±0.03, P.I.) (Figure 1B) and zeta potential was -7.82 ± 9.01 mV. The encapsulation efficiency was 76±3.81%. Entrapped nanoparticles were visible in the empty nanoparticles sample (Figure 1C). Monodispersed and spherical loaded nanoparticles were observed by SEM (Figure. 1D). System efficacy test suggested similar results of azelaic acid-loaded nanoparticles and azelaic acid in the free form against S. epidermidis and P. acnes (Table 1). DSC analysis suggested an interaction between the polymer (PLGA) and the drug. Cytotoxicity of azelaic acid-loaded nanoparticles on S. cerevisiae was concentration-dependent although not pronounced. Occluded patch test seemed indicate that the formulation excipients were safe.Small and anionic PLGA nanoparticles demonstrated to be efficient in the encapsulation of azelaic acid.Nanoparticles proved to be efficient against the most common bacteria associated with acne. Further studies will include additional bacteria susceptibility tests.

Development and Evaluation of a Novel Topical Treatment for Acne with Azelaic Acid-Loaded Nanoparticles

Azelaic acid (AzA) is used in the treatment of acne. However, side effects and low compliance have been associated with several topical treatments with AzA. Nanotechnology presents a strategy that can overcome these problems. Polymeric nanoparticles can control drug release and targeting and reduce local drug toxicity. The aim of this study was to produce and evaluate an innovative topical treatment for acne with AzA-loaded poly-DL-lactide/glycolide copolymer nanoparticles. A soft white powder of nanoparticles was prepared. The mean size of loaded nanoparticles was < 400 nm and zeta potential was negative. Spherical nanoparticles were observed by scanning electron microscopy. Encapsulation efficiency was around 80% and a strong interaction between the polymer and the drug was confirmed by differential scanning calorimetric analysis. In vitro drug release studies suggested a controlled and pulsatile release profile. System efficacy tests suggested similar results between the loaded nanoparticles and the nonencapsulated drug against the most common bacteria associated with acne. Cytotoxicity of AzA-loaded nanoparticles was concentration dependent, although not pronounced. The occluded patch test seemed to indicate that the formulation excipients were safe and thus AzA-loaded nanoparticles appear to be an efficient and safe treatment for acne.

A Honey Trap for the Treatment of Acne: Manipulating the Follicular Microenvironment to ControlPropionibacterium acnes

Today, as 40 years ago, we still rely on a limited number of antibiotics and benzoyl peroxide to treat inflammatory acne. An alternative way of suppressing the growth of Propionibacterium acnes is to target the environment in which it thrives. We conjecture that P. acnes colonises a relatively “extreme” habitat especially in relation to the availability of water and possibly related factors such as ionic strength and osmolarity. We hypothesise that the limiting “nutrient” within pilosebaceous follicles is water since native sebum as secreted by the sebaceous gland contains none. An aqueous component must be available within colonised follicles, and water may be a major factor determining which follicles can sustain microbial populations. One way of preventing microbial growth is to reduce the water activity (a w) of this component with a biocompatible solute of very high water solubility. For the method to work effectively, the solute must be small, easily diffusible, and minimally soluble in sebaceous lipids. Xylose and sucrose, which fulfil these criteria, are nonfermentable by P. acnes and have been used to reduce water activity and hence bacterial colonisation of wounds. A new follicularly targeted topical treatment for acne based on this approach should be well tolerated and highly effective.

Formulation and characterization of solid lipid nanoparticles loaded Neem oil for topical treatment of acne

ObjectiveTo investigate the treatment of acne and pimples as well as improves skin elasticity by solid lipid nanoparticles (SLNs) loaded Neem oil. MethodNeem oil as a natural agent was incorporated into SLNs prepared by double emulsification method using different concentration of lecithin and Tween 80. The characteristics of SLNs with different concentration of lipid were investigated. ResultsThe average particle size of Neem oil loaded SLNs decreased with increasing concentration of surfactant. SLNs of (221.6 ± 2.0) nm with a Polydispersity index of (0.948 ± 0.040) were obtained at higher concentration of lipid and surfactant. High entrapment efficiency of 82.10% revealed the ability of solid lipid nanoparticles to incorporate a high quantity of Neem oil. Furthermore the stability of SLNs indicated with negligible drug leakage after 3 weeks. ConclusionThe result concluded that Neem oil loaded solid lipid nanoparticles with more lecithin content in their colloid exhibit sustained effect which satisfactorily produced the antibacterial action on Acne microbes. Therefore Neem oil loaded SLN was used successfully for prolonged treatment of Acne.

Needlestick injuries, topical acne treatment and Mephisto sign correction

Needlestick injuries, topical acne treatment and Mephisto sign correction

Needlestick injuries, topical acne treatment and Mephisto sign correction

Needlestick injuries, topical acne treatment and Mephisto sign correction

Needlestick injuries, topical acne treatment and Mephisto sign correction

Needlestick injuries, topical acne treatment and Mephisto sign correction

A split-face clinical trial to compare the safety and efficacy of two topical acne treatments in subjects with mild to moderate acne vulgaris

A split-face clinical trial to compare the safety and efficacy of two topical acne treatments in subjects with mild to moderate acne vulgaris

Chitosan-solid lipid nanoparticles as carriers for topical delivery of tretinoin

Tretinoin (TRE) or all-trans retinoic acid is employed in the topical treatment of various skin diseases including acne and psoriasis. However, its use is strongly limited by side effects and high chemical instability. TRE encapsulation in nanostructured systems reduces these problems. Chitosan is a biopolymer that exhibits a number of interesting properties such as bioadhesion and antibacterial activity. The aim of this work was to prepare and characterize solid lipid nanoparticles (SLN) containing TRE, with and without addition of chitosan, to assess their in vitro cytotoxicity in keratinocytes and to evaluate their antibacterial activity against bacteria related to acne. SLN without (SLN-TRE) and with (SLN-chitosan-TRE) chitosan were prepared by hot high pressure homogenization. The hydrodynamic mean diameter and zeta potential were 162.7±1.4nm and −31.9±2.0mV for SLN-TRE, and 284.8±15.0nm and 55.9±3.1mV for SLN-chitosan-TRE. The SLN-chitosan-TRE exhibited high encapsulation efficiency, high physical stability in the tested period (one year), were not cytotoxic to keratinocytes and showed high antibacterial activity against P. acnes and S. aureus. Therefore chitosan-SLN can be good candidates to encapsulate TRE and to increase its therapeutic efficacy in the topical treatment of acne.

Therapeutic agents and herbs in topical application for acne treatment

Acne vulgaris suppresses an individual's self-confidence by causing distress with regard to physical appearance, which affects a significant number of individuals during puberty and is delineated by adolescence. Several treatments have been introduced to decrease the aesthetic and psychological problems caused by acne. The topical application of therapeutic agents has been found to be more feasible than hormonal treatment and laser therapy. The ingredients in topical acne treatments, particularly herbs and naturally derived compounds, have received considerable interest as they have fewer adverse effects than synthetic agents.

Comedolytic effect and reduced skin irritation of a new formulation of all-trans retinoic acid-loaded solid lipid nanoparticles for topical treatment of acne

Novel drug delivery systems, such as solid lipid nanoparticles (SLN), have been proposed to reduce retinoic acid (RA)-induced skin irritation. However, one question still remains: could it be accomplished without reducing efficacy? To evaluate this question the comedolytic effects and epidermal thickening of RA-loaded SLN were compared to the conventional RA formulations (gel or cream), as well as the potential of these formulations to induce skin irritation. The comedolytic effects and epidermal thickening of these formulations, both containing RA at 0.01 or 0.05%, were investigated in a rhino mouse model, while the studies of RA-induced skin irritation were evaluated through rabbit skin irritation tests and in the rhino mouse model. RA-loaded SLN, as compared to the placebo, produced a comedolytic effect with a significant reduction of the utricle diameter, which proved to be similar to that observed for marketed gels or creams regardless of the RA concentration. RA formulations (SLN or marketed cream) also induced an epidermal proliferation leading to a thickened epidermis in treated animals. In both animals studied (rhino mice and rabbits), the RA-loaded SLN, when compared to conventional formulations, promoted a significant reduction in RA-induced skin irritation (erythema and scaling). Then, RA-loaded SLN represents an interesting alternative to reduce RA-induced skin irritation without reducing efficacy, and constitutes an innovative approach for the topical treatment of acne with RA.

What's new in acne? New therapeutic approaches

Well-known topical and systemic treatments for acne have advanced little over the last 10 years. However, many therapeutic approaches are being evaluated both in terms of topical and systemic treatments. The purpose of this paper is to show the progress of innovative drug projects in treating acne. The topical use of new formulations using lipid nanoparticles and microspheres could help for new products based on anti-androgens or retinoids more concentrated and better tolerated. New active agents such as topical antimicrobial peptides, inhibitors of ectopeptidase, omiganan pentahydrochloride, antisense oligonucleotides, lauric acid are many original ways to explore for the treatment of acne. New treatment regimens for doxycycline and isotretinoin would increase tolerance. Dapsone has been evaluated for isotretinoin-resistant forms. Phototherapy narrowband light (blue or red) can find its place in the strategy for the management of acne. Finally, acne vaccines could be developed too.

Azelaic acid modulates the inflammatory response in normal human keratinocytes through PPARγ activation

Azelaic acid (AzA), a nine-carbon dicarboxylic acid, is an agent for the topical treatment of acne. It has also been shown to be effective in rosacea; however, the mechanism of action has not been clarified. Because inflammation is a common feature of both conditions, we investigated the effects of azelaic acid on the inflammatory response of normal human keratinocytes to ultraviolet B light, which is a photosensitizer agent in rosacea. AzA, at 20 mM, a concentration achievable following topical application of a 15% gel, suppresses ultraviolet B light-induced interleukins-1beta, -6 and tumor necrosis factor-alpha mRNA expression and protein secretion. Mechanistically, azelaic acid significantly reduced the ultraviolet B light-induced nuclear translocation of nuclear factor kB p65 subunit and the phosphorylation of the p38 mitogen and stress-activated protein kinase. Moreover, as peroxisome proliferators-activated receptor gamma, (PPARgamma) which has a crucial role in the control of inflammation, is activated by fatty acids and products of lipid peroxidation, we further investigated the effect of azelaic acid on the expression of this nuclear receptor. AzA induced peroxisome proliferators-activated receptor-gamma mRNA and its transcriptional activity. The PPARgamma antagonist GW9662 abrogated the inhibitory effects of AzA on the UVB-induced pro-inflammatory cytokines release and on the cell proliferation. Our study provides new insights into the molecular mechanisms of the activity of azelaic acid and lands additional evidences for its therapeutic effects on inflammatory skin diseases, such as rosacea.

Perspectives on Therapeutic Options for Acne: An Update

It is clear that acne vulgaris often has medical and psychosocial implications that can range from mild to severe. To minimize these risks, evaluation and appropriate treatment are necessary, even in the younger pediatric patient. This article provides an overview of the current information on the topical and systemic treatment of acne, including innovative delivery options and new formulations and combinations of existing medications.