Functionalized chitosan nanoparticles for cutaneous delivery of a skin whitening agent: an approach to clinically augment the therapeutic efficacy for melasma treatment.

The increase in the production of melanin level inside the skin prompts a patient-inconvenient skin color disorder namely; melasma. This arouses the need to develop efficacious treatment modalities, among which are topical nano-delivery systems. This study aimed to formulate functionalized chitosan nanoparticles (CSNPs) in gel form for enhanced topical delivery of alpha-arbutin as a skin whitening agent to treat melasma. Ionic gelation method was employed to prepare α-arbutin-CSNPs utilizing a 24 full factorial design followed by In vitro, Ex vivo and clinical evaluation of the nano-dispersions and their gel forms. Results revealed that the obtained CSNPs were in the nanometer range with positive zeta potential, high entrapment efficiency, good stability characteristics and exhibited sustained release of α-arbutin over 24 h. Ex vivo deposition of CSNPs proved their superiority in accumulating the drug in deep skin layers with no transdermal delivery. DSC and FTIR studies revealed the successful amorphization of α-arbutin into the nanoparticulate system with no interaction between the drug and the carrier system. The comparative split-face clinical study revealed that α-arbutin loaded CSNPs hydrogels showed better therapeutic efficacy compared to the free drug hydrogel in melasma patients, as displayed by the decrease in: modified melasma area and severity index (mMASI) scores, epidermal melanin particle size surface area (MPSA) and the number of epidermal monoclonal mouse anti-melanoma antigen recognized by T cells-1 (MART-1) positive cells which proved that the aforementioned system is a promising modality for melasma treatment.

Oleuropein as a novel topical antipsoriatic nutraceutical: formulation in microemulsion nanocarrier and exploratory clinical appraisal.

Introduction: Oleuropein is a promising nutraceutical found in abundance in olive leaf, with reported antioxidant and anti-inflammatory properties, and hence could be a valuable treatment for dermatological diseases such as psoriasis.Areas covered: In order to overcome the poor skin penetration of oleuropein, it was formulated in a microemulsion nanocarrier. The selected microemulsion formulation displayed a particle size of 30.25 ± 4.8 nm, zeta potential 0.15 ± 0.08 mV and polydispersity index 0.3 ± 0.08, with storage stability for 1 year in room temperature and total deposition in skin layers amounting to 95.67%. Upon clinical examination in psoriatic patients, the oleuropein microemulsion formulation was proven superior to the marketed Dermovate cream composed of clobetasol propionate, in terms of reduction of Psoriasis Area and Severity Index (PASI) scores, as well dermoscopic imaging and morphometric analysis of the psoriasis lesions, in which oleuropein microemulsion exhibited marked improvement in the clinical manifestations of psoriasis.Expert opinion: The findings of this study further prove the promising role of nutraceuticals, as well as nanoparticles in enhancing the therapeutic outcome of treatments, and open new era of applications in a variety of diseases.

Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy.

Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ±â€¯5.68 nm and -36.10 ±â€¯2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases.

Clinical cosmeceutical repurposing of melatonin in androgenic alopecia using nanostructured lipid carriers prepared with antioxidant oils.

BACKGROUND: The present work aims to formulate nanostructured lipid carriers (NLCs) exhibiting high skin deposition and high inherent antioxidant potential to repurpose the use of melatonin hormone and some antioxidant oils in the treatment of androgenic alopecia (AGA). RESEARCH DESIGN AND METHODS: NLCs were characterized for their size, charge, drug entrapment, anti-oxidant potential, physical stability, in vitro release, surface morphology, and ex-vivo skin deposition. Their merits were clinically tested on patients suffering from AGA by calculating the degree of improvement, conduction of hair pull test, histometric assessment, and dermoscopic evaluation. RESULTS: Results revealed that melatonin NLCs showed nanometer size, negatively charged surface, high entrapment efficiency, and high anti-oxidant potential, in addition to sustained release for 6 h. Furthermore, NLCs displayed good storage stability and they were able to increase the skin deposition of melatonin 4.5-folds in stratum corneum, 7-folds in epidermis, and 6.8-folds in the dermis compared to melatonin solution. Melatonin NLCs displayed more clinically desirable results compared to the melatonin solution in AGA patients, manifested by increased hair density and thickness and decreased hair loss. CONCLUSIONS: The aforementioned system was shown to be a very promising treatment modality for AGA, which is worthy of futuristic experimentation.

Melatonin vitamin C-based nanovesicles for treatment of androgenic alopecia: Design, characterization and clinical appraisal.

The present study aimed to develop vitamin C based nanovesicles (aspasomes) loaded with the antioxidant melatonin, as a novel cosmeceutical to be used for clinical treatment of androgenic alopecia (AGA). Aspasomes were assessed regarding their particle size, charge, drug entrapment, anti-oxidant potential, physical stability, in vitro release, surface morphology, and ex-vivo skin deposition. Clinically, melatonin aspasomes were tested on AGA patients, and assessed by evaluating the degree of improvement through conduction of hair pull test, histometric analysis and dermoscopic evaluation. Results revealed that melatonin aspasomes showed favorable pharmaceutical properties in addition to clinically promising results compared to melatonin solution, manifested by increased hair thickness, density and decreased hair loss, with photographic improvement in most patients. Therefore, melatonin vitamin C-based aspasomes were clinically auspicious in the treatment of AGA, hence, paving the way for their further exploration in other oxidative-dependent dermatological diseases.

Carboxytherapy Versus Skin Microneedling in Treatment of Atrophic Postacne Scars: A Comparative Clinical, Histopathological, and Histometrical Study.

BACKGROUND: Acne scarring has been a challenge to treat. Microneedling gained popularity in treatment of such scars. Meanwhile, carboxytherapy (CXT) is considered a novel treatment modality for acne scars. OBJECTIVE: To evaluate efficacy of CXT versus microneedling in treatment of acne scars. METHODS AND MATERIALS: Thirty-two patients with atrophic acne scars received 6 sessions of microneedling and CXT on right and left sides of face, respectively. Clinical evaluation with histopathological and computerized morphometric analysis was performed at 2 months after treatment. RESULTS: After either microneedling or CXT, there was significant decrease of total acne scars and its 3 types separately (icepicks, boxcar, and rolling) (p ≤ .001). Comparing both sides of face, there was no significant difference regarding grading response and reduction percentage of total scars and its types (p > .05). Histopathologically, there was an improvement of character and organization of collagen and elastic fibers in addition to significant increase in epidermal thickness on both sides of face, with no significant difference between them (p > .05). CONCLUSION: Both CXT and microneedling are equally effective, tolerable, safe, and noninvasive treatment modalities of atrophic acne scars. Similar histopathological changes were observed after both modalities, helping in better understanding their action.