- Long-Term Effectiveness and Safety of Up to 48 Weeks' Treatment with Topical Adapalene 0.3%/Benzoyl Peroxide 2.5% Gel in the Prevention and Reduction of Atrophic Acne Scars in Moderate and Severe Facial Acne. [Journal Article]
- AJAm J Clin Dermatol 2019 Jun 17
- CONCLUSIONS: Reductions in atrophic acne scars and acne lesions observed after 24 weeks of treatment with A0.3/BPO2.5 gel were maintained with treatment up to 48 weeks. The additional improvement in atrophic scar count with 48 weeks' A0.3/BPO2.5 treatment, compared to delayed application at 24 weeks, highlights the importance of early initiation of effective acne treatment to prevent and reduce the formation of acne scars.
- Carboxylation of Aryl Triflates with CO2 Merging Palladium and Visible-Light-Photoredox Catalysts. [Journal Article]
- OLOrg Lett 2019 Jun 12
- We report herein a visible-light-promoted, highly practical carboxylation of readily accessible aryl triflates at ambient temperature and a balloon pressure of CO2 by the combined use of palladium an…
We report herein a visible-light-promoted, highly practical carboxylation of readily accessible aryl triflates at ambient temperature and a balloon pressure of CO2 by the combined use of palladium and photoredox Ir(III) catalysts. Strikingly, the stoichiometric metallic reductant is replaced by a nonmetallic amine reductant providing an environmentally benign carboxylation process. In addition, one-pot synthesis of a carboxylic acid directly from phenol and modification of estrone and concise synthesis of pharmaceutical drugs adapalene and bexarotene have been accomplished via late-stage carboxylation reaction. Furthermore, a parallel decarboxylation-carboxylation reaction has been demonstrated in an H-type closed vessel that is an interesting concept for the strategic sector. Spectroscopic and spectroelectrochemical studies indicated electron transfer from the Ir(III)/DIPEA combination to generate aryl carboxylate and Pd(0) for catalytic turnover.
- Incorporation of benzoyl peroxide nanocrystals into adapalene-loaded solid lipid microparticles: Part I - Nanocrystalline benzoyl peroxide. [Journal Article]
- IJInt J Pharm 2019 Jun 10; 564:171-179
- Hair follicles are a promising target for the administration of drugs to treat diseases associated with the pilosebaceous unit, such as acne. For solid lipid microparticle dispersions a successful an…
Hair follicles are a promising target for the administration of drugs to treat diseases associated with the pilosebaceous unit, such as acne. For solid lipid microparticle dispersions a successful and selective delivery of adapalene via targeted erosion of the particles in sebum has been shown. By embedding nanoparticulate benzoyl peroxide in lipid microparticles, the therapeutic potency of adapalene can be further increased by improving follicular deposition of benzoyl peroxide and minimizing direct contact between benzoyl peroxide and stratum corneum, which is responsible for the irritating potential of this active agent. The aim of this study was to develop a novel nanoparticulate formulation for benzoyl peroxide suitable for the incorporation in solid lipid microparticles. In this contribution, a wet grinding process using liposomal dispersions of fully hydrated phosphatidylcholine was developed, upscaled and optimized for solid content and stabilizer concentration. The resulting novel nanosuspension was characterized by particle size and morphology and examined for chemical and physical stability as well as solubility and polymorphism. During the process development a dependency between the colloidal microstructure of the stabilizer dispersion and milling efficiency was found: while physical mixtures fail to deliver nanosuspensions, liposomal dispersions succeed with the same amount of stabilizer.
- The Role of Topical Retinoids in Prevention and Treatment of Atrophic Acne Scarring: Understanding the Importance of Early Effective Treatment [Journal Article]
- JDJ Drugs Dermatol 2019 Mar 01; 18(3):255-260
- Atrophic acne scarring is a frequent occurrence among acne patients. These facial marks are often very emotionally distressing for the patient and can result in adverse impact to quality of life. Whi…
Atrophic acne scarring is a frequent occurrence among acne patients. These facial marks are often very emotionally distressing for the patient and can result in adverse impact to quality of life. While most clinicians consider scarring as a sequela of moderate to severe acne, recent studies have found that scars are also associated with mild acne. Risk factors include time to effective treatment, severity of acne, family history, and excoriations. New data shows that early and effective acne treatment can reduce the development of new scars, confirming the widespread perception of this approach in prevention. It is also becoming clear that the inflammatory process drives both the development of acne lesions and atrophic scars. This implies that inhibiting activation of inflammatory pathways early is key to preventing scars. Data also suggests a useful role for adapalene for the treatment of well-established acne scars with scar remodeling accompanied by the production of new collagen and elastic tissue. Acne guidelines and recommendations continue to highlight the central role of retinoids, with fixed-dose combination retinoids being particularly important due to targeting of multiple inflammatory pathophysiologic factors and for patient convenience. Higher concentrations of retinoids such as adapalene 0.3%/benzoyl peroxide 2.5% (A0.3/BPO2.5) have shown increased efficacy, particularly among patients with moderately severe and severe acne – a population at high risk for scarring. Further, controlled study of A0.3/BPO2.5 in patients with moderate acne (mean, 40 acne lesions per half face) and mild-moderate scarring demonstrated A0.3/BPO2.5 was significantly superior to vehicle in reducing scar counts from baseline over 24 weeks. While scar counts lessened on the A0.3/BPO2.5 side, counts increased on the vehicle side during the study. This occurred in the setting of active acne, where the efficacy of A/BPO is well known, emphasizing the dual actions of A0.3/BPO2.5 in both treatment and prevention. J Drugs Dermatol. 2019;18(3):255-260.
- Adapalene-loaded poly(ε-caprolactone) microparticles: Physicochemical characterization and in vitro penetration by photoacoustic spectroscopy. [Journal Article]
- PlosPLoS One 2019; 14(3):e0213625
- Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, …
Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its commercial formula. In this sense, the microencapsulation of this drug using polyesters can circumvent its topical side effects and can lead to the enhancement of drug delivery into sebaceous glands. The goal of this work was to obtain ADAP-loaded poly(ε-caprolactone) (PCL) microparticles prepared by a simple emulsion/solvent evaporation method. Formulations containing 10 and 20% of ADAP were successfully obtained and characterized by morphological, spectroscopic, and thermal studies. Microparticles presented encapsulation efficiency of ADAP above 98% and showed a smooth surface and spherical shape. Fourier transform infrared spectroscopy (FTIR) results presented no drug-polymer chemical bond, and a differential scanning calorimetry (DSC) technique showed a partial amorphization of the drug. ADAP permeation in the Strat-M membrane for transdermal diffusion testing was evaluated by photoacoustic spectroscopy (PAS) in the spectral region between 225 and 400 nm after 15 min and 3 h from the application of ADAP-loaded PCL formulations. PAS was successfully used for investigating the penetration of polymeric microparticles. In addition, microencapsulation decreased the in vitro transmembrane diffusion of ADAP.
- Adapalene Gel 0.1% Versus Placebo as Prophylaxis for Anti-Epidermal Growth Factor Receptor-Induced Acne-Like Rash: A Randomized Left-Right Comparative Evaluation (APPEARANCE). [Journal Article]
- OOncologist 2019 Mar 19
- CONCLUSIONS: The results of the APPEARANCE trial indicate that adapalene does not prevent acne-like rash over placebo when added to topical moisturizer and oral minocycline but instead may have a detrimental effect. Therefore, adapalene is not recommended as prophylaxis against acne-like rash induced by anti-epidermal growth factor receptor therapies.Given that acne-like rash was completely controlled with placebo in approximately half of patients, predictive measures to identify patients needing intensive prophylaxis are required.Adapalene is not recommended as prophylaxis against acne-like rash induced by anti-EGFR therapies.
- Comparison of the efficacy and safety of 0.1% adapalene gel and 0.025% tretinoin cream in the treatment of childhood acanthosis nigricans. [Journal Article]
- PDPediatr Dermatol 2019; 36(3):330-334
- CONCLUSIONS: Lack of histopathological evaluations.We found no significant difference between topical 0.1% adapalene gel and 0.025% tretinoin in the treatment of AN.
- The efficacy of glycolic acid, salicylic acid, gluconolactone, and licochalcone A combined with 0.1% adapalene vs adapalene monotherapy in mild-to-moderate acne vulgaris: a double-blinded within-person comparative study. [Journal Article]
- CCClin Cosmet Investig Dermatol 2019; 12:151-161
- CONCLUSIONS: The results showed no hindrance of using a cosmeceutical combined with standard treatment. Nevertheless, this cosmeceutical product showed some benefits in reducing complications from acne.
- Adapalene suppressed the proliferation of melanoma cells by S-phase arrest and subsequent apoptosis via induction of DNA damage. [Journal Article]
- EJEur J Pharmacol 2019 May 15; 851:174-185
- Malignant melanoma was the leading cause of mortality among the skin-associated cancer owing to its highly metastatic feature, increasing incidence and drug resistance requirement. Retinoids played i…
Malignant melanoma was the leading cause of mortality among the skin-associated cancer owing to its highly metastatic feature, increasing incidence and drug resistance requirement. Retinoids played important roles in the treatment of cancer via the activation of retinoid acid receptor (RAR) or retinoid X receptor (RXR). Our present study showed that the third-generation retinoid adapalene exhibited strong inhibitory effects on the proliferation of melanoma cells than other retinoids, such as all-trans-retinoic acid (ATRA), isotretinoin, acitretin and bexarotene, and adapalene exerted significant inhibitory effects on the colony formation of melanoma cells. Further study confirmed that adapalene treatment triggered dramatic S phase arrest and apoptosis, and S phase arrest was the potential mechanism of apoptosis induction. In addition, adapalene treatment dramatically regulated the expression of S phase-related protein, and increased the protein level of DNA damage marker，which were consistent with the results of the induction of the tail moment in comet assays. Meanwhile, DNA damage response was activated and the DNA repair pathway was simultaneously inhibited by adapalene treatment, which might furtherly potentiate S phase arrest and subsequent apoptosis. Taken together, these results showed that adapalene exhibited strong anti-cancer activity, and might be a candidate agent for the clinical treatment of melanoma.
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- Topical Retinoids in Acne Vulgaris: A Systematic Review. [Review]
- AJAm J Clin Dermatol 2019; 20(3):345-365
- CONCLUSIONS: Topical retinoids are safe and efficacious for the treatment of acne vulgaris. They should be used in combination with benzoyl peroxide to optimize results in patients. The differences in efficacy of topical retinoids appears minor; therefore, the type of topical retinoid is not as important as choosing a particular strength of topical retinoid and combining it with an antimicrobial agent. Adapalene has a superior tolerability profile amongst topical retinoids.