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Purpose: A rise in market demand for anti-aging skin care products has resulted in a proliferation of cosmeceuticals, including products that contain vitamin C. Many topicals containing vitamin C claim to reduce the appearance of wrinkles. However, these claims have not been systematically evaluated., Methods: A systematic review of literature published between January 2015 and September 2022 was performed per PRISMA guidelines. Scopus, Web of Science, and PubMed were queried for records relevant using the following Medical Subject Heading (MeSH) terms: “Topical Vitamin C OR Ascorbic acid”, “Vitamin C efficacy”, “dermatology”, “cosmetology”, and “skin anti-aging”. Variables of interest included: study type, study location, study duration, sample size, patient description, type and ingredients of the topical formulation, outcome measurement, results, and adverse events., Results: After deduplication, consideration of inclusion and exclusion criteria, and title/abstract screening, 5,428 initial records were reduced to 7 articles, including 4 meeting Level IB criteria, one meeting Level IIA criteria, and 2 meeting Level IIB criteria. Methods for assessing clinical improvements included global photodamage score, skin topography assessment, reflectance confocal microscopy (RCM) skin analysis, Dynamical Atlas, and participant self-assessment.  Conclusions: While 4 of the 7 studies met Level IB evidence, further high-quality, prospective, and comparative studies are indicated to better elucidate the role of topical vitamin C in wrinkle reduction. All the studies used vitamin C in combination with other ingredients or therapeutic mechanisms, thereby complicating any specific conclusions regarding the efficacy of vitamin C. Citation: Sanabria B, Berger LE, Mohd H, et al. Clinical efficacy of topical vitamin C on the appearance of wrinkles: a systematic literature review. J Drugs Dermatol. 2023;22(9):898-904. doi:10.36849/JDD.7332.

Owing to their complicated pathophysiology, the treatment of skin diseases necessitates a complex approach. Conventional treatment using topical corticosteroids often results in low effectiveness and the incidence of local or even systemic side effects. Nanoformulation of potent anti-inflammatory drugs has been selected as an optimal strategy for enhanced topical delivery of corticosteroids. In order to assess the efficiency of various nanoformulations, we formulated hydrocortisone (HC) and hydrocortisone-17-butyrate (HCB) into three different systems: lipid nanocapsules (LNC), polymeric nanoparticles (PNP), and ethosomes (ETZ). The systems were characterized using dynamic light scattering for their particle size and uniformity and the morphology of nanoparticles was observed by transmission electron microscopy. The nanosystems were tested using ex vivo full thickness porcine and human skin for the delivery of HC and HCB. The skin penetration was observed by confocal microscopy of fluorescently labelled nanosystems. ETZ were proposed as the most effective delivery system for both transdermal and dermal drug targeting but were also found to have a profound effect on the skin barrier with limited restoration. LNC and PNP were found to have significant effects in the dermal delivery of the actives with only minimal transdermal penetration, especially in case of HCB administration.

There are only a limited number of molecules in a cosmetic formulation, which can passively cross the stratum corneum and be absorbed into the skin layers. However, some actives should never cross the skin in large concentrations due to their potential for side effects, for example, sunscreens. Artificial intelligence is gaining an increasing role as a predictive tool, and in this regard, we selected the Formulating for Efficacy ® Software to forecast the changes in bioavailability of selected topical cosmetic compounds. Using the Franz diffusion cell methodology, various oils were selected as those with low release capability, and these were compared to those suggested by the software in Benzophenone-3-containing formulations. The software was able to predict the lipophilic phases, which, if utilized in the emulsion, were stable and sometimes even more pleasant in appearance and consistency than the reference emulsions prepared by the formulator. To date, however, Formulating for Efficacy ® Software still has limitations as far as predicting the hydrophilic phase, as well as not being able to choose the emulsifier or the preservative system.

Managing pediatric tuberculosis (TB) remains a public health problem requiring urgent and long-lasting solutions as TB is one of the top ten causes of ill health and death in children as well as adolescents universally. Minors are particularly susceptible to this severe illness that can be fatal post-infection or even serve as reservoirs for future disease outbreaks. However, pediatric TB is the least prioritized in most health programs and optimal infection/disease control has been quite neglected for this specialized patient category, as most scientific and clinical research efforts focus on developing novel management strategies for adults. Moreover, the ongoing coronavirus pandemic has meaningfully hindered the gains and progress achieved with TB prophylaxis, therapy, diagnosis, and global eradication goals for all affected persons of varying age bands. Thus, the opening of novel research activities and opportunities that can provide more insight and create new knowledge specifically geared towards managing TB disease in this specialized group will significantly improve their well-being and longevity.

Tetrahydrocurcumin (THC) has been well known for its superior antioxidant properties. Therefore, it is speculated that it might be effective to relieve oxidative stress-induced diseases, such as skin hyperpigmentation. In this work, an in vitro B16F10 melanoma cell model was used to study the impact of THC on the melanogenic process under stressed conditions. It was demonstrated that THC could effectively inhibit the α-MSH (melanocyte-stimulating hormone) induced melanin production in B16F10 melanoma cells and the expressions of three key enzymes involved with the biosynthetic process of melanin, tyrosinase (TYR), tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2), were all significantly reduced. In addition, an in vitro human keratinocyte cell model was used to investigate the potential protective role of THC on H 2 O 2 -induced cytotoxicity. It was found that THC could prevent H 2 O 2 -induced oxidative stress based on the results of both the cell viability study and the intracellular ROS (reactive oxygen species) study assessed by the flow cytometry. Last, THC was formulated into a lecithin based nanoemulsion, and an in vitro Franz diffusion cell study using Strat-M ® membrane concluded that the nanoemulsion could significantly enhance the membrane permeation compared to the unformatted THC suspension. This research demonstrated the anti-melanogenic benefits of THC on the melanoma and keratinocyte cell models and the topical delivery efficacy could be significantly enhanced using a lecithin based nanoemulsion.

Excessive sweating and body odors in many cultures can cause negative perceptions of an individual and in many cases is related to poor hygiene. Personal hygiene products have been developed with the intention of preventing these undesirable issues. The aim of this paper is to review the main active ingredients used in marketed deodorant and antiperspirant formulations as well as to identify new strategies and future methods to optimize such products and prevent malodor. PubMed and ScienceDirect databases were used to search for studies reporting the use of deodorants and antiperspirants, the compounds used in the formulations, their mechanisms of action and associated controversies, as well as new trends and approaches in the area. Even today, we are still using well-known and established actives such as triclosan and aluminum salts, and these are still the most used compounds in deodorants with bactericidal and antiperspirant properties. These substances have been on the market for more than 40 years, and still there are many questions concerning the safety of both actives. There is a general increased interest globally for lifestyles that focus on sustainability and more natural products such as plant sources and the use of, for example, essential oils. The research that focuses in the area of antiperspirants and deodorants is now more focused on studies of the armpit biochemistry and function and control of the microbiota present in this area. Other possible areas of interest are biotechnological solutions and finding new compounds that will interfere with the biochemistry of the process of sweat decomposition. Further approaches include formulations with probiotics which would maintain the balance of axillary microbiota., (© 2021 the International Society of Dermatology.)

The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and -29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDerm TM three-dimensional human skin irritation test and hen's egg test chorioallantoic membrane assay (HET-CAM).

In this study we aimed to develop a semi-solid formulation of polymeric nanoparticles loaded with adapalene to enhance the efficacy and improve the skin tolerability in acne therapy. An amphiphilic and biocompatible copolymer that self-assembles to nanospheres (known as TyroSpheres) was used to encapsulate adapalene and increase its solubility. A water-soluble viscous agent was applied to prepare a gel formulation of adapalene-loaded TyroSpheres (aapalene-TyroSphere). Particle size, morphology, homogeneity, and rheological characteristics of the adapalene-TyroSphere gel formulations were studied. The formulation with the preferred physical and structural properties was further investigated for in vitro skin irritation and in vivo comedolytic activity in a rhino mouse model. Based on the in vitro skin irritation study encapsulation of adapalene in TyroSphere significantly decreased secretion of pro-inflammatory cytokines (IL-1α and IL-8), confirming that the TyroSphere formulation of adapalene is less irritant than the commercial gel (Differin). TyroSphere gel formulation of adapalene improved the comedolytic properties of the formulation by significantly reducing the size of open utricles in rhino mice compared to Differin treatment. Using TyroSpheres, we were able to develop an alternative topical formulation of adapalene, which is potentially less irritant and more potent than the commercial product.

Drug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol-polyethylene glycol based orodispersible strip containing isoniazid, a first-line anti-tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and characterization of the orodispersible strip. The optimized strip was physically amalgamated with a monolayer, uniformly distributed surface geometry. It was 159.2 ± 3.0 µm thick, weighed 36.9 ± 0.3 mg, had an isoniazid load of 99.5 ± 0.8%w/w, disintegration and dissolution times of 17.6 ± 0.9 s and 5.5 ± 0.1 min respectively. In vitro crystallinity, thermal measurements and in silico thermodynamic predictions confirmed the strip's intrinsic miscibility, thermodynamic stability and amorphous nature. A Korsmeyer-Peppas (r = 0.99; n > 1 = 1.07) fitted kinetics typified by an initial burst release of 49.4 ± 1.9% at 4 min and a total of 99.8 ± 3.3% at 30 min was noted. Ex vivo isoniazid permeation through porcine buccal mucosa was bi-phasic and characterized by a 50.4 ± 3.8% surge and 95.6 ± 2.9% at 5 and 120 min respectively. The strip was physicomechanically robust, environmentally stable and non-cytotoxic., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Dermal delivery of hydrophobic drugs by microemulsion (ME) formulations and effect from ME microstructures were studied. Anti-fungal drug, clotrimazole (CLOT), was used as the model compound. ME formulations possessing different microstructures were prepared using a ME system that contains isopropyl myristate as oil, Labrasol and Cremophor EL as surfactant and co-surfactant, and water. Permeation experiments on human cadaver skin were conducted for ME and the control formulations of different CLOT concentrations. Dermal delivery of CLOT assessed by the dermal tissue drug concentration was found to be significantly higher for MEs when compared with the control formulation, evidenced by dermal retention Enhancement Ratio (ER D ) of 5.1, 2.8, and 3.0 for tested O/W, bi-continuous, and W/O MEs, respectively. The highest concentration was observed with O/W ME, suggesting the ME microstructure is an important formulation variable for enhancing dermal delivery efficiency. ME gel formulations prepared by incorporating 1.0%(w/w) of Carbopol980 showed comparable dermal CLOT concentration to MEs, but up to 2.4 fold higher than the commercial CLOT cream product, Lotrimin ® . Furthermore, Fluorescein Isothiocynate (FITC), used as a model compound for highly hydrophobic drugs, was also studied for dermal delivery by MEs, and results show consistent ME microstructure effect, suggested by significantly higher FITC concentrations in all skin layers, SC, viable epidermis, and dermis, from O/W ME over bi-continuous and W/O MEs., (Copyright © 2017 Elsevier B.V. All rights reserved.)

This study investigates the potential application of polymeric nanospheres (known as TyroSpheres) as a formulation carrier for topical delivery of cholecalciferol (i.e., Vitamin D3, VD3) with the goal to improve the skin delivery and stability of VD3. High drug loading and binding efficiencies were obtained for VD3 when loaded in TyroSpheres. VD3 was released from TyroSpheres in a sustained manner and was delivered across the stratum corneum, which occurred independent of the initial drug loading. An ex vivo skin distribution study showed that TyroSphere formulations delivered 3-10μg of active into the epidermis which was significantly higher than that delivered from Transcutol ® (the control vehicle). In addition, an in vitro cytotoxicity assay using keratinocytes confirmed that VD3 encapsulation in the nanoparticles did not alter the drug activity. Photodegradation of VD3 followed zero-order kinetics. TyroSpheres were able to protect the active against hydrolysis and photodegradation, significantly enhancing the stability of VD3 in the topical formulation., (Copyright © 2016 Elsevier B.V. All rights reserved.)

The purpose of this study is to develop a new formulation of adapalene for the topical treatment of acne. We investigated applicability of polymeric nanocarriers based on tyrosine-derived nanospheres (TyroSpheres) for adapalene delivery. TyroSpheres effectively encapsulated adapalene and substantially enhanced its aqueous solubility, while decreasing the crystallinity of the drug in the formulation. Skin distribution of adapalene via TyroSphere formulation was evaluated ex vivo using human cadaver and porcine ear skin, and this was compared with the commercial adapalene formulation, Differin®. Sustained drug release across stratum corneum in 51 h was observed from TyroSpheres. Additionally, in vitro skin irritation studies demonstrated that encapsulation of adapalene in TyroSpheres significantly reduced the irritancy of the drug to monolayer HaCaTs and reconstituted human epidermis (EpiDerm™, MatTek Corp.). The results suggest that TyroSpheres provide a promising carrier system to deliver hydrophobic drugs to hair follicles and upper epidermis while minimizing skin irritation of the encapsulated drug., (Copyright © 2016 Elsevier Inc. All rights reserved.)

To date, effective treatment, prophylaxis, and control of tuberculosis (TB) infection is mainly dependent on the use of drugs. However, patient noncompliance with prescribed anti-TB treatment schemes remains a major problem confronting successful pharmacotherapeutic outcomes. Thus, the development of alternative delivery systems that can improve adherence for the existing anti-TB bioactives has been intensified in recent times. The aim of this investigation was to engineer an optimal, thermodynamically stable oral film (OF) formulation containing a key anti-TB agent, pyrazinamide (PYZ), employing molecular modeling and experimental tools. Four PYZ-loaded film variants (OF 1, OF 2, OF 3, OF 4) were constructed in silico and then prepared in vitro using the Accelrys Materials Studio software and solvent casting method, respectively. Screening and selection of the optimal OF was based on the computation of the total interaction energy (ET), kinetic energy (EK), solubility parameter (S), and cohesive energy density (CED) as well as determining mass, thickness, dissolution and disintegration times, dissolution pH, drug loading capacity, and surface morphology in vitro. OF 2 was selected as the optimal formulation as it displayed the lowest ET (-8006.28 kcal/mol), dissolution time (9.96 min), disintegration time (56.49 s), and weight (39.33 mg); moderate EK (1052.98 kcal/mol); highest S (44.55 (J/cm(3))(0.5)) and CED (1.99 × 10(9) J/m(3)), slim dimension (166 μm), good and unvarying drug loading capacity (98.04%), acceptable dissolution pH (6.70), and well-layered surface topography. The drug release behavior of the optimal OF 2 was best elucidated with the zero order (R(2) = 0.97) and Korsmeyer-Peppas (R(2) = 0.99) models. X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) analyses showed that OF 2 was made of physically mixed multiple component polymeric and nonpolymeric compounds. OF 2 was semicrystalline in nature and displayed a dual phased ex vivo mucosal permeation pattern. In silico and in vitro physicomechanical quantities revealed OF 2's flexibility, robustness, and compressibility. OF 2 was most stable under controlled environmental humidity, pressure, and temperature conditions in silico and in vitro. OF 2 was potentially non-cytotoxic and biocompatible. Succinctly, this work demonstrated the applicability of a combination of atomistic molecular mechanics and dynamics calculations as well as experimental analyses to the fabrication, screening, optimization, and characterization of drug formulations. Lastly, the fabricated OF 2 formulation can function as a potential alternative for the effective loading and delivery of PYZ.

The irritancy of topical products has to be investigated to ensure the safety and compliance. Although several reconstructed human epidermal models have been adopted by the Organization for Economic Cooperation and Development (OECD) to replace in vivo animal irritation testing, these models are based on a single cell type and lack dermal components, which may be insufficient to reflect all of the components of irritation. In our study, we investigated the use of acellular porcine peritoneum extracellular matrix as a substrate to construct full-thickness human skin equivalents (HSEs) for use as irritation screening tool. The acellular peritoneum matrix (APM) exhibited excellent skin cell attachment (>80%) and proliferation for human dermal fibroblasts (HDF) and immortalized human keratinocytes (HaCaT). APM-HSEs based on coculture of HDF and HaCaT were prepared. Increased HDF seeding density up to 5 × 10(4)/cm(2) resulted in APM-HSEs with a thicker and more organized epidermis. The epidermis of APM-HSEs expressed keratin 15, a keratinocyte proliferation marker, and involucrin, a differentiation marker, respectively. To assess the use of APM-HSEs for irritation testing, six proficiency chemicals, including three nonirritants (phosphate-buffered saline, polyethylene glycol 400, and isopropanol) and three irritants (1-bromohexane, heptanol, and sodium dodecyl sulfate) were applied. The APM-HSEs were able to discriminate nonirritants from irritants based on the viability. Levels of cytokines (interleukin [IL]-1α, IL-1ra, IL-6, IL-8, and granulocyte macrophage colony-stimulating factor [GM-CSF]) in these treatment groups further assisted the irritancy ranking. In conclusion, we have developed partially differentiated full-thickness APM-HSEs based on acellular porcine peritoneum matrix, and these APM-HSEs demonstrated utility as an in vitro irritation screening tool.