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This study aimed to develop and evaluate a novel herbal gel formulation containing celecoxib and bioactive compounds of Salai Guggul for effective pain management. Celecoxib, a selective COX-2 inhibitor with anti-inflammatory and analgesic properties, was combined with menthol, safflower oil, and Salai Guggul extract to enhance therapeutic efficacy through synergistic effects. Three gel formulations (CHG I, CHG II, and CHG III) were prepared using varying concentrations of key excipients and evaluated for physicochemical properties, including pH, viscosity, extrudability, spreadability, and in vitro drug diffusion. All formulations exhibited favorable properties with pH values near skin compatibility, acceptable viscosity, and superior extrudability and spreadability. In vitro drug diffusion studies revealed that CHG I provided the highest drug release (97.27%) over 240 minutes. The study demonstrated the potential of this herbal gel formulation as a promising topical treatment for pain management, offering improved skin permeation and prolonged drug release. [ABSTRACT FROM AUTHOR]

This study presents the formulation development and characterization of a topical ethosomal gel incorporating Alpinia galanga and Aloe Vera extract, aimed at enhancing skin absorption and therapeutic efficacy. Preformulation studies assessed the physicochemical properties of the herbal extracts, utilizing Fourier Transform Infrared Spectroscopy (FTIR) for purity identification and various qualitative tests to confirm the presence of active phytoconstituents. The partition coefficient was determined to evaluate drug permeability and differential scanning calorimetry (DSC) was employed for melting point analysis. Ethanol-based ethosomal formulations were prepared via the classical cold method, followed by the formulation of gels using Carbopol 934. The characterization of ethosomes included assessment of entrapment efficiency and vesicle morphology via optical microscopy. Physical evaluation of the final gel formulations encompassed measurements of pH, spreadability, viscosity, consistency, and drug content, along with an in vitro release study using a Franz diffusion cell. Results indicated successful incorporation of the active compounds in a stable ethosomal gel formulation, with favorable characteristics for topical application. This innovative delivery system has the potential to improve the therapeutic outcomes of Alpinia galanga and Aloe vera in topical treatments. [ABSTRACT FROM AUTHOR]

The present work was performed with the objective of novel topical formulation development of poorly watersoluble drug Diclofenac diethylamine by loading the drug-containing nanosponge into the topical formulation. The nanosponges are polymeric nanoparticles that entrap the drug. The drug-loaded nanosponge has different absorption characteristics in comparison to the pure drug in the topical drug delivery system. The drug was first loaded in the ethylcellulose nanosponge using the emulsion solvent diffusion method. Then Diclofenac diethylamine nanosponge-loaded topical gel formulations were developed by using Carbopol 940 as a gel-forming polymer. The Diclofenac diethylamine-loaded nanosponges were evaluated for various evaluation parameters such as particle size distribution, surface morphology, drug entrapment efficiency, polydispersity index, etc. The topical gel formulations were evaluated for pH, in vitro drug release, viscosity, in vivo performance and compared with the marketed formulation. The average size of prepared nanosponge formulations was found in the range of 102.8 nm to 475.5 nm. Scanning electron microscopy photographs of developed formulations reveal the spongy and porous nature of particles along with spherical shape. The polydispersity index (PI) was found in the range of 0.756 to 0.954. It was found that formulation F3 with a drug-to-polymer ratio of 1:3 has the highest drug loading. Further nanosponges were characterized for different parameters and results revealed acceptable characteristics of B3 formulation. These prepared nanosponges were loaded in topical Carbopol gel (Formulation AB3) and evaluated for in vitro and in vivo performance. The data were fitted to different kinetic models which reveal typical zero order in vitro drug diffusion with prolonged drug release. The developed formulation generated better analgesic and anti-inflammatory responses compared to the standard marketed formulation. [ABSTRACT FROM AUTHOR]

A lot of people use emulsion gels because they are easier to use than creams and ointments and because they release drugs faster and more thoroughly. The study's goals were to develop and clarify an antifungal emulgel that can be put on the skin. In the Miconazole Emulgel method, the gelling agent, carbopol 934 is used with great accuracy. For the water phase, Tween 20 is an emulsifier. Propylene glycol is a co-surfactant. Methyl and propyl paraben are preservatives. And liquid paraffin is the oil in the oil phase mixture. Triethanolamine is used to bring the pH of the emulgel to between 6 and 6.4. Miconazole, which is like cholesterol for fungi, stops fungi from growing by decreasing ergosterol production, which makes membranes more mobile. There were no signs of phase separation in the improved F6 formulation. The improved mix had better drug content, spreadability, extrudability and viscosity. A 14-17 mm zone of blockage showed that the antifungal worked against Candida albicans and the drug released in vitro was 97.45%. All of the items had a pH level between 6 and 6.4, which means they were safe for the skin. The results show that the topical Miconazole Emulgel with Carbopol 934 is very smooth, easy to apply and calming. [ABSTRACT FROM AUTHOR]

Abstract Background Trifarotene is effective for treating acne and other skin issues. To ensure its quality and meet regulatory standards, a reverse phase liquid chromatography (RP-LC) stability-indicating method was developed and validated for its quantification in pure and topical dosage forms. An isocratic elution chromatographic method was employed, using an octadecylsilyl silica gel-packed column (150 mm × 4.6 mm, 3 µm particle size). The mobile phase was a mixture of phosphate buffer and acetonitrile (40:60 v/v). Chromatographic conditions included a flow rate of 0.5 mL/min, column temperature of 40 °C, detection at 265 nm, and injection volume of 20 µL. Results The developed analytical method reports the retention time of trifarotene 11.2 min, higher theoretical plate count, asymmetric peak, and good resolution between the peaks of trifarotene, phenoxyethanol, and environmentally generated impurities. Conclusion The analytical method has been found to be linear, accurate, robust, specific, and selective for impurities produced during forced degradation studies. The proposed analytical method can be utilized for routine pharmaceutical analysis of trifarotene to judge its quality and safety.

Background: Trifarotene is effective for treating acne and other skin issues. To ensure its quality and meet regulatory standards, a reverse phase liquid chromatography (RP-LC) stability-indicating method was developed and validated for its quantification in pure and topical dosage forms. An isocratic elution chromatographic method was employed, using an octadecylsilyl silica gel-packed column (150 mm × 4.6 mm, 3 µm particle size). The mobile phase was a mixture of phosphate buffer and acetonitrile (40:60 v/v). Chromatographic conditions included a flow rate of 0.5 mL/min, column temperature of 40 °C, detection at 265 nm, and injection volume of 20 µL. Results: The developed analytical method reports the retention time of trifarotene 11.2 min, higher theoretical plate count, asymmetric peak, and good resolution between the peaks of trifarotene, phenoxyethanol, and environmentally generated impurities. Conclusion: The analytical method has been found to be linear, accurate, robust, specific, and selective for impurities produced during forced degradation studies. The proposed analytical method can be utilized for routine pharmaceutical analysis of trifarotene to judge its quality and safety. [ABSTRACT FROM AUTHOR]

Background and Aims: This study developed a new, simple, and rapid spectrophotometric method for determining ichthammol as a local antiseptic in topical formulations. The developed spectrophotometric method for determining ichthammol was applied to topical formulations. Methods: The linearity range of the ichthammol was 5.0-50.0 μg/mL at a wavelength of 235 nm. Ethanol:water (50:50; v/v) was used as the solvent. The method was validated using the limit of quantification, limit of detection, linearity, selectivity, robustness, recovery, precision, stability, and accuracy of the method using the International Conference on Harmonisation guidelines for validation of analytical procedures: text and methodology Q2 (R1). Results: The limits of detection and quantification were calculated to be 0.044 μg/mL and 0.148 μg/mL, respectively. Intra-day and inter-day relative standard deviation values were calculated to be less than 1.024 %. The assay recovery and precision of ichthammol from topical formulations at 5.0, 20.0, and 50.0 μg/mL were evaluated. The mean recoveries for ichthammol in the topical formulation were calculated at 97.944-99.860%. It was determined that the ichthammol sample solution was stable for 24 h at 4.0°C. The validated method was applied to the cream formulation, and the amount of ichthammol in the cream was determined to be 97.442%. Conclusion: The validated method was successfully applied to determine ichthammol in topical formulations. The proposed method is reproducible and reliable and can be safely used for routine analysis. [ABSTRACT FROM AUTHOR]

Staphylococcus aureus , particularly multi-drug resistant strains, presents significant challenges in dairy farming due to its role in causing bovine mastitis, which leads to substantial economic losses and limited treatment options. Seeking alternative therapies, we investigated the potential of a topical formulation derived from the medicinal herb Salvia officinalis to combat S. aureus growth and biofilms associated with bovine mastitis. Through systematic extraction in different solvents and fractionation by column chromatography, we isolated and identified three key multicyclic terpenoids—ferruginol, sugiol, and sclareol—exhibiting significant antimicrobial activity. The formulation effectively inhibited biofilm formation, with minimum inhibitory concentration (MIC) values ranging from 0.09 to 0.74 mg ml−1 against clinical S. aureus strains, comparable to or lower than those of the pure compounds. Moreover, it displayed robust anti-adhesive properties, reducing biofilm formation by 20%–79% at subinhibitory concentrations. Furthermore, the formulation successfully disrupted pre-existing biofilms, achieving reductions ranging from 30% to 82%. Cytotoxicity assays confirmed the safety of the formulation on mammary epithelial cells, with cell viability maintained at 100% at MIC. Our findings underscore the therapeutic potential of Sa. officinalis -derived compounds in managing bovine mastitis caused by S. aureus , emphasizing their antimicrobial efficacy and safety profile. [ABSTRACT FROM AUTHOR]

The assessment of the mucoadhesive properties peak mucoadhesive force (F max) and work of mucoadhesion (W muc) with texture analyzers is a common in vitro method for analyzing formulation capabilities. Challenges arise in selecting and standardizing experimental conditions due to various variables influencing mucoadhesion. This complexity hampers direct product performance comparisons. In our study, we explored factors (contact force and time, probe speed and mucin in artificial saliva) impacting a model formulation's mucoadhesive capacity. Using Omcilon-A®Orabase on porcine buccal mucosa, we systematically varied experimental conditions, employing a statistical approach (Central Composite Design - CCD). Three variables (contact force, contact time, probe speed) and their interactions were assessed for their impact on F max and W muc. Results showed that contact time and force positively affected F max , while only contact time influenced W muc. In the mucin artificial saliva test, a force of 0.5 N, time of 600 s, and speed of 1 mm/s yielded optimal F max (0.587 N) and W muc (0.468 N.s). These conditions serve as a reference for comparing mucoadhesive properties of formulations for topical oral use. [Display omitted] [ABSTRACT FROM AUTHOR]

Enhancement of orthodontic tooth movement (OTM) through local administration of biofunctional molecules has become increasingly significant, particularly for adult patients seeking esthetic and functional improvements. This comprehensive systematic review analyzes the efficacy of various biofunctional molecules in modulating OTM, focusing on the method of administration and its feasibility, especially considering the potential for topical application. A search across multiple databases yielded 36 original articles of experimental human and animal OTM models, which examined biofunctional molecules capable of interfering with the biochemical reactions that cause tooth movement during orthodontic therapy, accelerating the OTM rate through their influence on bone metabolism (Calcitriol, Prostaglandins, Recombinant human Relaxin, RANKL and RANKL expression plasmid, growth factors, PTH, osteocalcin, vitamin C and E, biocompatible reduced graphene oxide, exogenous thyroxine, sclerostin protein, a specific EP4 agonist (ONO-AE1-329), carrageenan, and herbal extracts). The results indicated a variable efficacy in accelerating OTM, with Calcitriol, Prostaglandins (PGE1 and PGE2), RANKL, growth factors, and PTH, among others, showing promising outcomes. PGE1, PGE2, and Calcitriol experiments had statistically significant outcomes in both human and animal studies and, while other molecules underwent only animal testing, they could be validated in the future for human use. Notably, only one of the animal studies explored topical administration, which also suggests a future research direction. This review concluded that while certain biofunctional molecules demonstrated potential for OTM enhancement, the evidence is not definitive. The development of suitable topical formulations for human use could offer a patient-friendly alternative to injections, emphasizing comfort and cost-effectiveness. Future research should focus on overcoming current methodological limitations and advancing translational research to confirm these biomolecules' efficacy and safety in clinical orthodontic practice. [ABSTRACT FROM AUTHOR]

Acne affects most of the world's population, causing an impact on the self-esteem of adolescents and young adults. One of the causes is the presence of the bacteria Cutibacterium acnes which are part of the natural microbiota of the skin. Topical treatments consist of anti-inflammatory and antibiotics, which could select resistant strains. Alternatives to the antibiotic are biocomposites that have antimicrobial activity like biosurfactants which are produced by bacteria. An innovative way of applying these compounds is bioadhesive polymeric films that adhere to the skin and release the active principle topically. Rhamnolipids have great potential to be used in the treatment of acne because they present antimicrobial activity against C. acnes in low and safe concentrations (MIC of 15.62 µg/mL, CBM of 31.25 µg/mL and CC50 of 181.93 µg/mL). Four films with different rhamnolipids concentrations (0.0; 0.1; 0.2; and 0.3%, w/w) were obtained as to visual appearance, mass variation, thickness, density, solubility, pH, water vapor transmission, mechanical properties (folding endurance, bioadhesion strength, tensile strength, elongation at break and Young's modulus), scanning electron microscopy and infrared. The results show that these formulations had a homogeneous appearance; elastic mechanical properties; pH similar to human skin and bioadhesive. The polymeric films containing rhamnolipids were effective against C. acnes, in the in vitro test, at the three concentrations tested, the film with the highest concentration (0.3%, w/w) being the most promising for presenting the highest antimicrobial activity. Thus, the polymeric film containing rhamnolipids has the potential to be used in the treatment of acne. [ABSTRACT FROM AUTHOR]

Skin penetration of an active pharmaceutical ingredient is key to developing topical drugs. This penetration can be adjusted for greater efficacy and/or safety through the selection of dosage form. Two emerging dosage forms, cream–gel and gel-in-oil emulsion, were tested for their ability to deliver diclofenac into the skin, with the target of maximising skin retention while limiting systemic exposure. Prototypes with varying amounts of solvents and emollients were formulated and evaluated by in vitro penetration testing on human skin. Cream–gel formulas showed better skin penetration than the emulgel benchmark drug even without added solvent, while gel-in-oil emulsions resulted in reduced diffusion of the active into the receptor fluid. Adding propylene glycol and diethylene glycol monoethyl ether as penetration enhancers resulted in different diclofenac penetration profiles depending on the dosage form and whether they were added to the disperse or continuous phase. Rheological characterisation of the prototypes revealed similar profiles of cream–gel and emulgel benchmark, whereas gel-in-oil emulsion demonstrated flow characteristics suitable for massaging product into the skin. This study underlined the potential of cream–gel and gel-in-oil emulsions for adjusting active penetration into the skin, broadening the range of choices available to topical formulation scientists. [ABSTRACT FROM AUTHOR]

A classical emulsion formulation based on petrolatum and mineral oil as the internal phase with emulsifier wax as a typical topical emulsion cream was investigated for the effect of process parameters on drug product quality and performance attributes. The Initial Design of Experiment (DoE) suggested that an oil phase above 15%, coupled with less than 10% emulsifying wax, resulted in less stable emulsions. Different processing parameters such as homogenization speed, duration, cooling rate, and final temperature showed minimal influence on properties and failed to improve stability. The final DoE suggested that the optimal emulsion stability was achieved by introducing a holding period midway through the cooling stage after solvent addition. Within the studied holding temperature range (25–35 °C), a higher holding temperature correlated with increased emulsion stability. However, the application of shear during the holding period, using a paddle mixer, adversely affected stability by disrupting the emulsion microstructure. IVRT studies revealed that the release of lidocaine was higher in the most stable emulsion produced at a holding temperature of 35 °C compared to the least stable emulsion produced at a holding temperature of 25 °C. This suggests that a holding temperature of 35 °C improves both the stability and active release performance. It appears that a slightly higher holding temperature, 35 °C, allows a more flexible and stable emulsifying agent film around the droplets facilitating stabilization of the emulsion. This study offers valuable insights into the relationship between process parameters at various stages of manufacture, microstructure, and various quality attributes of emulsion cream systems. The knowledge gained will facilitate improved design and optimization of robust manufacturing processes, ensuring the production of the formulations with the desired critical quality attributes. [ABSTRACT FROM AUTHOR]

Purpose: N-methyl-D-aspartate (NMDA) receptors that are expressed by T-cells modulate T-cell proliferation, cytotoxicity and cell migration toward chemokines. Several studies have shown an anti-inflammatory effect of NMDA receptor antagonists. This study compares the effect of the noncompetitive low-affinity NMDA receptor antagonist N-(2-adamantyl)-hexamethyleneimine hydrochloride (hemantane) in a topical formulation (gel) with the cyclooxygenase (COX) inhibitor diclofenac in a topical formulation (gel) in rats with arthritis induced by Freund’s Complete Adjuvant (FCA). Methods: On day 14 after an FCA injection into the left hind paw, rats with contralateral hind paw edema were selected for further investigation (29/65). They were treated with 5% hemantane gel or 1% diclofenac gel applied locally to hind paws daily for 2 weeks starting 14 days after the FCA injection. Rats with arthritis were examined hind paw edema, hyperalgesia, and motor deficits; their body weight and hematological parameters were recorded. The rats were euthanized on day 28, followed by histological examination of the ankle joint (HE stain). Results: Rats with arthritis exhibited hind paw inflammation and hyperalgesia, motor deficits, changes of hematological parameters, reduced weight gain and spleen hypertrophy. Histological examination of the ankle joint revealed degenerative-dystrophic lesions of the cartilaginous tissue, proliferative inflammation of the synovium, edema and lymphocytic/macrophage infiltration of periarticular tissues. Hemantane gel reduced hind paw edema, pain, motor deficits and histological signs of inflammation; its effect was comparable to diclofenac gel. Conclusion: Hemantane gel alleviates FCA-induced arthritis in rats, and its effect is comparable to diclofenac gel.

Background and Aim: Marine seaweeds are a valuable source of bioactive ingeredients with the possibility of different effects in cosmeceutical industries such as skin health products. One of the main characteristics of the skin is moisture which plays an important role in maintaining metabolism, enzymatic activity, mechanical properties, appearance and protective barrier. The objective of the present study was to formulate the water extract of brown algae Sargassum tenerrimum with antioxidant and antibacterial properties as a moisturizing cream to evaluate physicochemical stability and microbial growth. Methods: Algae were collected from the Persian Gulf intertidal zone and was washed with seawater, then transferd to Seafood Processing Laboratory in Gorgan University of Agricultural Sciences and Natural Resources for extraction process, after that formulation of 1% moisturizing cream was made at Center for Research and Training in Skin Diseases and LeprosyTehran University of Medical Scinces. Statistical analysis of antibacterial properties of water extract was performed by SPSS software version 22 and one way ANONA was used to analyse the data. The comparison between the means were investigated by Duncan’s test used for measuring significant differences at 5 percent level. Finally, the charts were created by using Excel software. The results of the study were reported as mean ± standard deviation. Results: According to the results, the prepared 1% cream was completely stable and homogeneous in room temperature and oven for 6 months and successfully passed microbial tests. Conclusion: In view of the above mentioned, the manufactured cream efficacy was well done and can be introduce as a skin moisturizing agent. [ABSTRACT FROM AUTHOR]

Suitable human models for the development and characterization of topical compounds for inflammatory skin diseases such as atopic dermatitis are not readily available to date. We describe here the development of a translational model involving healthy human skin mimicking major aspects of AD and its application for the characterization of topical Janus kinase inhibitors. Full thickness human abdominal skin obtained from plastic surgery stimulated in vitro with IL4 and IL13 shows molecular features of AD. This is evidenced by STAT6 phosphorylation assessed by immunohistochemistry and analysis of skin lysates. Broad transcriptome changes assessed by AmpliSeq followed by gene set variation analysis showed a consistent upregulation of gene signatures characterizing AD in this model. Topical application of experimental formulations of compounds targeting the JAK pathway to full thickness skin normalizes the molecular features of AD induced by IL4 and IL13 stimulation. The inhibitory effects of topical JAK inhibitors on molecular features of AD are supported by pharmacokinetic analysis. The model described here is suited for the characterization of topical compounds for AD and has the potential to be extended to other inflammatory skin diseases and pathophysiological pathways. [ABSTRACT FROM AUTHOR]

Ibrutinib (IBR) is a tyrosine kinase inhibitor investigated for treating solid and non-solid tumors. Considering the advantages that a topical application of IBR could generate in terms of dose reduction and side effects in skin cancer treatment, this paper presents a simple and selective HPLC method for determining IBR concentration in in vitro skin permeation studies to support the development of topical formulations. The method uses a reversed-phase C18 column and a mobile phase composed of acetonitrile and 0.01 mol/L phosphoric acid at pH 3.5 (35:65 v/v), flowing at 1.0 mL/min. The oven temperature was set at 35 °C, the injection volume was 20 μL, and UV drug detection was performed at 259 nm. The validation procedure certified that this method was selective for IBR determination even when extracted from human or porcine skin matrices. The method was linear over a range of 0.2 to 15.0 μg/mL, precise, robust, and accurate, with recovery rates from the skin layers higher than 89.5 ± 5.9% for the porcine skin and higher than 92.0 ± 0.2% for the human skin. The limits of detection and quantification were 0.01 and 0.02 μg/mL, respectively. The method showed, therefore, to be adequate for use in further skin permeation studies employing IBR topical formulations. [ABSTRACT FROM AUTHOR]

Psoriasis, a prevalent inflammatory skin disorder affecting a significant percentage of the global population, poses challenges in its management, necessitating the exploration of novel cost-effective and widely accessible therapeutic options. This study investigates the potential of ursolic acid (UA), a triterpenoid known for its anti-inflammatory and pro-apoptotic properties, in addressing psoriasis-related inflammation and keratinocyte hyperproliferation. The research involved in vitro models employing skin and immune cells to assess the effects of UA on psoriasis-associated inflammation. The presented research demonstrates the limiting effects of UA on IL-6 and IL-8 production in response to the inflammatory stimuli and limiting effects on the expression of psoriatic biomarkers S100A7, S100A8, and S100A9. Further, the study reveals promising outcomes, demonstrating UA's ability to mitigate inflammatory responses and hyperproliferation of keratinocytes by the induction of non-inflammatory apoptosis, as well as a lack of the negative influence on other cell types, including immune cells. Considering the limitations of UA's poor solubility, hybrid systems were designed to enhance its bioavailability and developed as hybrid nano-emulsion and bi-gel topical systems to enhance bioavailability and effectiveness of UA. One of them in particular–bi-gel–demonstrated high effectiveness in limiting the pathological response of keratinocytes to pro-psoriatic stimulation; this was even more prominent than with ursolic acid alone. Our results indicate that topical formulations of ursolic acid exhibit desirable anti-inflammatory activity in vitro and may be further employed for topical psoriasis treatment. [ABSTRACT FROM AUTHOR]

Recently, vast efforts towards sustainability have been made in the pharmaceutical industry. In conventional oil-in-water (O/W) cream formulations, various petroleum-based excipients, namely mineral oil and petrolatum, are commonly used. Natural or synthetic excipients, derived from vegetable sources, were explored as alternatives to petroleum-based excipients in prototype topical creams, with 1% (w/w) lidocaine. A conventional cream comprised of petroleum-derived excipients was compared to creams containing sustainable excipients in terms of key quality and performance attributes, physicochemical properties, and formulation performance. The petrolatum-based control formulation had the highest viscosity of 248.0 Pa·s, a melting point of 42.7°C, a low separation index at 25°C of 0.031, and an IVRT flux of 52.9 µg/cm2/h. Formulation SUS-4 was the least viscous formulation at 86.9 Pa·s, had the lowest melting point of 33.6°C, the highest separation index of 0.120, and the highest IVRT flux of 139.4 µg/cm2/h. Alternatively, SUS-5 had a higher viscosity of 131.3 Pa·s, a melting point of 43.6°C, a low separation index of 0.046, and the lowest IVRT flux of 25.2 µg/cm2/h. The cumulative drug permeation after 12 h from SUS-4, SUS-5, and the control were 126.2 µg/cm2, 113.8 µg/cm2, and 108.1 µg/cm2, respectively. The composition of the oil-in-water creams had influence on physicochemical properties and drug release; however, skin permeation was not impacted. Sustainable natural or synthetic excipients in topical cream formulations were found to be suitable alternatives to petroleum-based excipients with comparable key quality attributes and performance attributes and should be considered during formulation development. [ABSTRACT FROM AUTHOR]

Ibrutinib (IBR) is a tyrosine kinase inhibitor investigated for treating solid and non-solid tumors. Considering the advantages that a topical application of IBR could generate in terms of dose reduction and side effects in skin cancer treatment, this paper presents a simple and selective HPLC method for determining IBR concentration in in vitro skin permeation studies to support the development of topical formulations. The method uses a reversed-phase C18 column and a mobile phase composed of acetonitrile and 0.01 mol/L phosphoric acid at pH 3.5 (35:65 v/v), flowing at 1.0 mL/min. The oven temperature was set at 35 °C, the injection volume was 20 μL, and UV drug detection was performed at 259 nm. The validation procedure certified that this method was selective for IBR determination even when extracted from human or porcine skin matrices. The method was linear over a range of 0.2 to 15.0 μg/mL, precise, robust, and accurate, with recovery rates from the skin layers higher than 89.5 ± 5.9% for the porcine skin and higher than 92.0 ± 0.2% for the human skin. The limits of detection and quantification were 0.01 and 0.02 μg/mL, respectively. The method showed, therefore, to be adequate for use in further skin permeation studies employing IBR topical formulations.

The objective of this study was to investigate the cutaneous delivery of cannabidiol (CBD) from aqueous formulations developed for the targeted local treatment of dermatological conditions. CBD was formulated using a proprietary colloidal drug delivery system (VESIsorb®) into an aqueous colloidal solution at 2% (ACS 2%) and two colloidal gels (CG 1% and CG 2%, which contained 1% and 2% CBD, respectively). Two basic formulations containing CBD (5% in propylene glycol (PG 5%) and a 6.6% oil solution (OS 6.6%)) and two marketed CBD products (RP1 and RP2, containing 1% CBD) were used as comparators. Cutaneous delivery and cutaneous biodistribution experiments were performed using human abdominal skin (500–700 µm) under infinite- and finite-dose conditions with 0.5% Tween 80 in the PBS receiver phase. The quantification of CBD in the skin samples was performed using a validated UHPLC-MS/MS method and an internal standard (CBD-d3). The cutaneous deposition of CBD under finite-dose conditions demonstrated the superiority of CG 1%, CG 2%, and ACS 2% over the marketed products; CG 1% had the highest delivery efficiency (5.25%). Cutaneous biodistribution studies showed the superiority of the colloidal systems in delivering CBD to the viable epidermis, and the upper and lower papillary dermis, which are the target sites for the treatment of several dermatological conditions. [ABSTRACT FROM AUTHOR]

The identification of natural remedies for the management of the skin aging process is an increasingly growing issue. In this context, ursolic acid (UA), a ubiquitous molecule, mainly contained in Annurca apple (AA) fruit, has demonstrated valuable cosmetic potential. To this end, in the current study, the AA oleolite (AAO, extract in sunflower oil containing 784.40 ± 7.579 µg/mL of UA) was evaluated to inhibit porcine elastase enzymatic reactions through a validated spectrophotometric method. AAO has shown a valuable capacity to contrast the elastase enzyme with a calculated IC50 of 212.76 mg/mL, in comparison to UA (IC50 of 135.24 μg/mL) pure molecules and quercetin (IC50 of 72.47 μg/mL) which are used as positive controls. In this context and in view of the valuable antioxidant potential of AAO, its topical formulation with 2.5% (w/w) AAO was tested in a placebo-controlled, double-blind, two-arm clinical study on 40 volunteers. Our results indicated that after 28 days of treatment, a significant reduction of the nasolabial fold (−7.2 vs. baseline T0, p < 0.001) and forehead wrinkles (−5.3 vs. baseline T0, p < 0.001) were registered in combination with a valuable improvement of the viscoelastic skin parameters, where skin pliability/firmness (R0) and gross elasticity (R2) were significantly ameliorated (−13% vs. baseline T0, p < 0.001 for R0 and +12% vs. baseline T0, p < 0.001 for R2). Finally, considering the positive correlation between skin elasticity and hydration, the skin moisture was evaluated through the estimation of Trans epidermal water loss (TEWL) and skin conductance. [ABSTRACT FROM AUTHOR]

Purpose: N-methyl-D-aspartate (NMDA) receptors that are expressed by T-cells modulate T-cell proliferation, cytotoxicity and cell migration toward chemokines. Several studies have shown an anti-inflammatory effect of NMDA receptor antagonists. This study compares the effect of the noncompetitive low-affinity NMDA receptor antagonist N-(2-adamantyl)-hexamethyleneimine hydrochloride (hemantane) in a topical formulation (gel) with the cyclooxygenase (COX) inhibitor diclofenac in a topical formulation (gel) in rats with arthritis induced by Freund's Complete Adjuvant (FCA). Methods: On day 14 after an FCA injection into the left hind paw, rats with contralateral hind paw edema were selected for further investigation (29/65). They were treated with 5% hemantane gel or 1% diclofenac gel applied locally to hind paws daily for 2 weeks starting 14 days after the FCA injection. Rats with arthritis were examined hind paw edema, hyperalgesia, and motor deficits; their body weight and hematological parameters were recorded. The rats were euthanized on day 28, followed by histological examination of the ankle joint (HE stain). Results: Rats with arthritis exhibited hind paw inflammation and hyperalgesia, motor deficits, changes of hematological parameters, reduced weight gain and spleen hypertrophy. Histological examination of the ankle joint revealed degenerative-dystrophic lesions of the cartilaginous tissue, proliferative inflammation of the synovium, edema and lymphocytic/macrophage infiltration of periarticular tissues. Hemantane gel reduced hind paw edema, pain, motor deficits and histological signs of inflammation; its effect was comparable to diclofenac gel. Conclusion: Hemantane gel alleviates FCA-induced arthritis in rats, and its effect is comparable to diclofenac gel. [ABSTRACT FROM AUTHOR]

Enhancement of orthodontic tooth movement (OTM) through local administration of biofunctional molecules has become increasingly significant, particularly for adult patients seeking esthetic and functional improvements. This comprehensive systematic review analyzes the efficacy of various biofunctional molecules in modulating OTM, focusing on the method of administration and its feasibility, especially considering the potential for topical application. A search across multiple databases yielded 36 original articles of experimental human and animal OTM models, which examined biofunctional molecules capable of interfering with the biochemical reactions that cause tooth movement during orthodontic therapy, accelerating the OTM rate through their influence on bone metabolism (Calcitriol, Prostaglandins, Recombinant human Relaxin, RANKL and RANKL expression plasmid, growth factors, PTH, osteocalcin, vitamin C and E, biocompatible reduced graphene oxide, exogenous thyroxine, sclerostin protein, a specific EP4 agonist (ONO-AE1-329), carrageenan, and herbal extracts). The results indicated a variable efficacy in accelerating OTM, with Calcitriol, Prostaglandins (PGE1 and PGE2), RANKL, growth factors, and PTH, among others, showing promising outcomes. PGE1, PGE2, and Calcitriol experiments had statistically significant outcomes in both human and animal studies and, while other molecules underwent only animal testing, they could be validated in the future for human use. Notably, only one of the animal studies explored topical administration, which also suggests a future research direction. This review concluded that while certain biofunctional molecules demonstrated potential for OTM enhancement, the evidence is not definitive. The development of suitable topical formulations for human use could offer a patient-friendly alternative to injections, emphasizing comfort and cost-effectiveness. Future research should focus on overcoming current methodological limitations and advancing translational research to confirm these biomolecules’ efficacy and safety in clinical orthodontic practice.

A classical emulsion formulation based on petrolatum and mineral oil as the internal phase with emulsifier wax as a typical topical emulsion cream was investigated for the effect of process parameters on drug product quality and performance attributes. The Initial Design of Experiment (DoE) suggested that an oil phase above 15%, coupled with less than 10% emulsifying wax, resulted in less stable emulsions. Different processing parameters such as homogenization speed, duration, cooling rate, and final temperature showed minimal influence on properties and failed to improve stability. The final DoE suggested that the optimal emulsion stability was achieved by introducing a holding period midway through the cooling stage after solvent addition. Within the studied holding temperature range (25–35 °C), a higher holding temperature correlated with increased emulsion stability. However, the application of shear during the holding period, using a paddle mixer, adversely affected stability by disrupting the emulsion microstructure. IVRT studies revealed that the release of lidocaine was higher in the most stable emulsion produced at a holding temperature of 35 °C compared to the least stable emulsion produced at a holding temperature of 25 °C. This suggests that a holding temperature of 35 °C improves both the stability and active release performance. It appears that a slightly higher holding temperature, 35 °C, allows a more flexible and stable emulsifying agent film around the droplets facilitating stabilization of the emulsion. This study offers valuable insights into the relationship between process parameters at various stages of manufacture, microstructure, and various quality attributes of emulsion cream systems. The knowledge gained will facilitate improved design and optimization of robust manufacturing processes, ensuring the production of the formulations with the desired critical quality attributes.

The use of plants to treat diseases and heal wounds is a custom that dates back thousands of years and is a legacy of ancient civilizations. Although a significant proportion of the planet's plant biodiversity is found on the American continent, there are very few pharmaceutical products developed from it. This work aimed to develop and characterize topical formulations (gels and emulgels), including a combination of plant extracts with recognized antibacterial activity. Hydroalcoholic extracts of Lippia turbinata Griseb. and Lippia alba (Mill.) N. E. Brown were obtained by leaching. The excipients used were Carbopol® 934 and 940, Sepigel® 305, sodium carboxymethylcellulose, methylcellulose, propylene glycol, and ethanol. The finished product was characterized by properties: organoleptic characteristics, extensibility, pH, texture profile, permeation performance, and microbiological quality. Then, they were subjected to stability studies in different conditions of temperature and humidity. They had a characteristic smell of plant species, color brown, without the presence of lumps, and with good extensibility. The gels had an in vitro permeation of porcine skin of up to 30% and low retention in the epithelium (<15%). They did not present microbial contamination and were stable for six months. Of the gels formulated, the gel with Sepigel® 4% (w/w) presented a better appearance. These results demonstrate the feasibility of transporting non-hydro soluble extracts in a gel formulation. All formulations are appropriate to preserve the antibacterial effect of original extracts. They maintain stability over time without the use of antimicrobial preservatives. [ABSTRACT FROM AUTHOR]

Industrial hemp (Cannabis sativa L.), due to its bioactive compounds (terpenes and cannabinoids), has gained increasing interest in different fields, including for medical purposes. The evaluation of the safety profile of hemp essential oil (EO) and its encapsulated form (nanoemulsion, NE) is a relevant aspect for potential therapeutic applications. This study aimed to evaluate the toxicological effect of hemp EOs and NEs from cultivars Carmagnola CS and Uso 31 on three cell lines selected as models for topical and inhalant administration, by evaluating the cytotoxicity and the cytokine expression profiles. Results show that EOs and their NEs have comparable cytotoxicity, if considering the quantity of EO present in the NE. Moreover, cells treated with EOs and NEs showed, in most of the cases, lower levels of proinflammatory cytokines compared to Etoposide used as a positive control, and the basal level of inflammatory cytokines was not altered, suggesting a safety profile of hemp EOs and their NEs to support their use for medical applications. [ABSTRACT FROM AUTHOR]

The manufacturing process for ointments typically involves a series of heating, cooling, and mixing steps. Precise control of the level of mixing through homogenization and the cooling rate, as well as temperature at different stages, is important in delivering ointments with the desired quality attributes, stability, and performance. In this work, we investigated the influence of typical plant processing conditions on the microstructure, stability, and sensorial properties of a model ointment system through a Design of Experiments (DoE) approach. Homogenization speed at the cooling stage after the addition of the solvent (propylene glycol, PG) was found to be the critical processing parameter that affects stability and the rheological and sensorial properties of the ointment. A lower PG addition temperature was also found to be beneficial. The stabilization of the ointment at a lower PG addition temperature was hypothesized to be due to more effective encapsulation by crystallizing mono- and diglycerides at the lower temperature. The in vitro release profiles were found to be not influenced by the processing parameters, suggesting that for the ointment platform studied, processing affects the microstructure, but the effects do not translate into the release profile, a key performance indicator. Our systematic study represents a Quality-by-Design (QbD) approach to the design of a robust manufacturing process for delivering stable ointments with the desired performance attributes and properties. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Faculty of Pharmacy of Ankara University / Ankara Üniversitesi Eczacilik Fakültesi Dergisi is the property of Ankara University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Psoriasis, a prevalent inflammatory skin disorder affecting a significant percentage of the global population, poses challenges in its management, necessitating the exploration of novel cost-effective and widely accessible therapeutic options. This study investigates the potential of ursolic acid (UA), a triterpenoid known for its anti-inflammatory and pro-apoptotic properties, in addressing psoriasis-related inflammation and keratinocyte hyperproliferation. The research involved in vitro models employing skin and immune cells to assess the effects of UA on psoriasis-associated inflammation. The presented research demonstrates the limiting effects of UA on IL-6 and IL-8 production in response to the inflammatory stimuli and limiting effects on the expression of psoriatic biomarkers S100A7, S100A8, and S100A9. Further, the study reveals promising outcomes, demonstrating UA’s ability to mitigate inflammatory responses and hyperproliferation of keratinocytes by the induction of non-inflammatory apoptosis, as well as a lack of the negative influence on other cell types, including immune cells. Considering the limitations of UA’s poor solubility, hybrid systems were designed to enhance its bioavailability and developed as hybrid nano-emulsion and bi-gel topical systems to enhance bioavailability and effectiveness of UA. One of them in particular–bi-gel–demonstrated high effectiveness in limiting the pathological response of keratinocytes to pro-psoriatic stimulation; this was even more prominent than with ursolic acid alone. Our results indicate that topical formulations of ursolic acid exhibit desirable anti-inflammatory activity in vitro and may be further employed for topical psoriasis treatment.

The use of probiotics has gained increasing attention as a strategy for wound healing to decrease microbial resistance to disinfectants and antibiotics. This study aimed to investigate the potential of a non-medicinal topical cocktail of probiotic bacteria (CPB) in promoting wound healing in dogs using in vitro scratch assay. Canine Progenitors Epidermal Keratinocytes (CPEK) were exposed to a prototype product formulated with CPB (PPP), non-formulated CPB, and the vehicle. The viability of CPB and CPEK cells was first evaluated in the co-culture model. Then, wound closure was analyzed over time. The CPB required a minimum concentration of 75 CFU/mL for better viability with CPEK. While the CPEK preserved 100% of their viability when PPP was diluted to up to 75,000 CFU/mL. At higher concentrations, the viability of CPEK was reduced by the concomitant effect of the non-formulated CPB and the vehicle. The formulated and non-formulated CPB and the vehicle seem to lead to a dose-dependent increase in cell migration compared to the control. Importantly, at the concentration of 750,000 CFU/mL, the PPP showed a 20% increase in wound closure. Taken together, our findings suggest the potential beneficial effects of the probiotic-based topical cocktail (PPP) on wound healing. However, to confirm and validate these effects, further experiments are necessary to provide more robust evidence and allow us to confidently establish the potential beneficial effects of the probiotic bacteria (CPB) in promoting wound healing. [ABSTRACT FROM AUTHOR]

Background: Antibiotic resistance is a major concern, especially in hidradenitis suppurativa (HS). However, antibiotics form a cornerstone in its treatment. Topical clindamycin is known to cause bacterial resistance but is still advised as monotherapy for the treatment of mild to moderate HS. Methods: This is a randomized, controlled, assessor-blinded, intra-patient pilot trial to compare the clinical efficacy of clindamycin-benzoyl peroxide gel with clindamycin lotion in patients with mild to moderate HS. Two contralateral body sites were randomized for treatment in each patient. The primary outcome was the difference in the International Hidradenitis Suppurativa Severity Score (IHS4) between the two groups after 12 weeks. Secondary objectives were feasibility of the intra-patient design, efficacy within treatment groups, effect on HS pain, HS itch, patient satisfaction, antibiotic resistance, and the prolonged efficacy after 16 weeks. Results: Ten patients were included, resulting in two groups of 10 treated body sites. No significant differences were found between the two groups for all measurements after 12 or 16 weeks, while both therapies led to an improvement in the IHS4, pain, and itch scores. A significant decrease was observed in the IHS4 for both the clindamycin lotion (−1.5; p < 0.05) and the clindamycin-benzoyl peroxide gel (−2; p < 0.01) after 16 weeks, and the pain scores were reduced from 7 to 2.5, p < 0.01 and 6.5 to 3, p = 0.03, respectively. Using the IHS4-55, we identified 50% of patients as responders in both groups after 12 weeks. The intra-patient design, however, unexpectedly appeared to hinder the inclusion of patients. Conclusion: Clindamycin-benzoyl peroxide gel showed favorable clinical efficacy results, similar to clindamycin lotion, suggesting that it could replace clindamycin lotion in the treatment of mild to moderate HS and to prevent antibiotic resistance. A larger controlled trial is needed to validate these results. [ABSTRACT FROM AUTHOR]

Copyright of Immunology Quarterly / Immunológiai Szemle is the property of Medicina Konyvkiado Zrt. and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Cristina García-Millan,1 Ander Pino,2 Rita Rodrigues,1 Gonzalo Segurado-Miravalles,1,3 Adrián Alegre-Sánchez,1 Pedro Jaén,1,3 Eduardo Anitua2 1Grupo de Dermatología Pedro Jaén, Madrid, Spain; 2BTI Biotechnology Institute, Vitoria, Spain; 3University Hospital Ramon y Cajal, Madrid, SpainCorrespondence: Eduardo Anitua, BTI Biotechnology Institute, Jacinto Quincoces 39, Vitoria, Spain, Email eduardo@fundacioneduardoanitua.orgBackground: Although the underlying pathophysiology of sensitive skin remains unknown, it presents clinical symptoms like erythema, burning and dryness associated with other inflammatory dermatoses such as dermatitis or rosacea.Objective: The aim of the present report was to provide preliminary data about the efficacy of Endoret-Serum (ES) as an autologous therapy for the topical management of sensitive skin alterations.Materials and Methods: Five patients underwent a daily topical ES treatment that was maintained for three months. Clinical assessment was carried out using validated dermatological surveys (DLQI, IGA, Likert, PGI-I). Additionally, skin hydration measurement and high-resolution topographic and reflectance confocal imaging analysis were carried out.Results: No adverse events were observed during the treatment. At the end of the follow-up period, surveys highlighted a significant therapeutic effect compared to baseline. Skin hydration was also improved, and topographic images showed a decrease in patient’s underlying inflammatory and vascular condition.Conclusion: This preliminary report suggests that Endoret-Serum may be useful in the management of clinical symptoms derived from sensitive skin alterations.Keywords: platelet-rich plasma, growth factors, sensitive skin, topical formulation, case report

Wound treatment is one of the most prevalent concerns and economic burden in healthcare system. Because of antibacterial and re-epithelialization properties, trimethyl chitosan (TMC) has the potential to be used in wound healing dressing. Hyaluronic acid (HA), the main component of the extracellular matrix is capable to activate specific cell signals involved in fibroblast proliferation and new vessel formation, improving the quality of the scars. LL37 peptide promotes wound healing, angiogenesis and also has potential antimicrobial properties. Hence, we aimed to fabricate LL37 encapsulated in TMC-HA composite as a novel topical wound dressing and evaluated its efficacy to accelerate wound closure in an animal model. Composites were optimized based on physical properties such as, porosity, swelling, biodegradation, and mechanical properties. The release of LL37 from the optimized composite (3:3 v/v) was completed during 8 h using bicinchoninic acid assay (BCA) protein quantification kit. LL37-loaded TMC-HA composites displayed antimicrobial activity against Staphylococcus aureus and Pseudomonas aeruginosa. Animal experiments demonstrated the complete wound healing in the group that received LL37-loaded TMC-HA following 16 days of treatment. Based on histological studies, the formation of advanced granulation tissue with significantly higher collagen deposition and re-epithelialized tissues were observed in LL37-loaded TMC-HA-treated wounds. In conclusion, we successfully developed a biodegradable wound healing dressing that promoted healing processes in mice wound model contributed to simultaneous positive effects of the polymers and LL37. [ABSTRACT FROM AUTHOR]

α-Aminophosphonates are organophosphorus compounds with an obvious similarity with α-amino acids. Owing to their biological and pharmacological characteristics, they have attracted the attention of many medicinal chemists. α-Aminophosphonates are known to exhibit antiviral, antitumor, antimicrobial, antioxidant and antibacterial activities, which can all be important in pathological dermatological conditions. However, their ADMET properties are not well studied. The aim of the current study was to provide preliminary information about the skin penetration of three preselected α-aminophosphonates when applying them as topical cream formulations in static and dynamic diffusion chambers. The results indicate that aminophosphonate 1a, without any substituent in the para position, shows the best release from the formulation and the highest absorption through the excised skin. However, based on our previous study, the in vitro pharmacological potency was higher in the case of para-substituted molecules 1b and 1c. The particle size and rheological studies revealed that the 2% cream of aminophosphonate 1a was the most homogenous formulation. In conclusion, the most promising molecule was 1a, but further experiments are proposed to uncover the possible transporter interactions in the skin, optimize the topical formulations and improve PK/PD profiles in case of transdermal delivery. [ABSTRACT FROM AUTHOR]

Hesperetin is a flavanone glycoside abundantly available in citrus fruits. Hesperetin is known to have various pharmacological activities, including anti-oxidant, anti-inflammatory, anti-allergic etc. In this current study, a simple, isocratic, fast, accurate and robust high-performance liquid chromatographic analytical method was developed for the estimation of hesperetin in a topical gel. A good chromatographic separation was achieved with an inertsil ODS 3V column with acetonitrile and acidified water as mobile phase. The method was validated over a linearity range of 25 to 2500 ng/ml following regulatory guidelines for various parameters, including specificity, system suitability, linearity, accuracy, precision and robustness. A topical gel containing hesperetin was prepared using Carbopol as a gel-forming agent. The total drug content of this formulation was determined using the validated high-performance liquid chromatographic method. The validated method was found to be linear over the selected range. Limit of detection and limit of quantitation was calculated as 1.61 and 4.89 ng/ml respectively. The method was found to be precise with % relative standard deviation of less than 1 % for intraday precision and less than 2 % for inter-day precision experiments. The method was also found to be robust, with small and deliberate changes in various method parameters. The drug content of topical gel formulation was found to be more than 98 % when analyzed using the validated high-performance liquid chromatographic method. The developed method will be useful for the routine quantitative analysis of hesperetin in topical gel formulations. [ABSTRACT FROM AUTHOR]

The development of new antimicrobial formulations for the treatment of animal infectious dermatitis is important as current antimicrobial treatments can have undesirable effects. The purpose of this study was to examine the in vitro antimicrobial activity of an Eryngium foetidum L. ethanolic extract against a bacterium, Staphylococcus pseudintermedius; a yeast, Malassezia pachydermatis; and three dermatophytes, Microsporum canis, Microsporum gypseum, and Trichophyton mentagrophytes; all of which are the most common animal skin pathogens causing dermatitis. A viscous semi-solid crude extract was obtained at a yield of 30.6% dry weight. Quantitative analysis of the chemical constituents of the extract by spectrophotometry revealed 3.62 mg GAE/g extract of total phenolic, 1.77 mg CE/g extract of total flavonoid, and 10.11 mg/g extract of total carotenoid contents. HPLC-DAD analysis of the carotenoid content showed that β-carotene and lutein were present at 5.17 and 4.43 mg/g extract, respectively. Antimicrobial activity by broth microdilution test found that the E. foetidum extract had MIC, MBC and MFC values in the range of 6.25 to 25.0 mg/ml; and the time-kill test indicated that this effect was both dose and time dependent. Ointment formulations containing the extract at concentrations of 5, 7.5 and 10% w/w had high microbicidal activity against the tested pathogens and retained their activity and physical properties after repeated freeze-thaw cycles. The results of this study show the potential of E. foetidum extract to be developed as a novel antimicrobial formulation for treatment of infectious dermatitis in pets. [ABSTRACT FROM AUTHOR]

The objective of this study was to investigate the cutaneous delivery of cannabidiol (CBD) from aqueous formulations developed for the targeted local treatment of dermatological conditions. CBD was formulated using a proprietary colloidal drug delivery system (VESIsorb®) into an aqueous colloidal solution at 2% (ACS 2%) and two colloidal gels (CG 1% and CG 2%, which contained 1% and 2% CBD, respectively). Two basic formulations containing CBD (5% in propylene glycol (PG 5%) and a 6.6% oil solution (OS 6.6%)) and two marketed CBD products (RP1 and RP2, containing 1% CBD) were used as comparators. Cutaneous delivery and cutaneous biodistribution experiments were performed using human abdominal skin (500–700 µm) under infinite- and finite-dose conditions with 0.5% Tween 80 in the PBS receiver phase. The quantification of CBD in the skin samples was performed using a validated UHPLC-MS/MS method and an internal standard (CBD-d3). The cutaneous deposition of CBD under finite-dose conditions demonstrated the superiority of CG 1%, CG 2%, and ACS 2% over the marketed products; CG 1% had the highest delivery efficiency (5.25%). Cutaneous biodistribution studies showed the superiority of the colloidal systems in delivering CBD to the viable epidermis, and the upper and lower papillary dermis, which are the target sites for the treatment of several dermatological conditions.

Silybum marianum has been used for centuries by herbalists and physicians to treat different forms of liver diseases. It contains flavonoid, which has antioxidant, anti-inflammatory, antifibrotic and anticancer properties. The objective of this research was to develop a silymarin-based mucoadhesive gel for prolonged release in oral mucosa and to evaluate the same by using in vitro drug release kinetic models and ex vivo methods for drug permeation using chicken buccal mucosa. The mucoadhesive gel was formulated in different trials by varying the concentration of silymarin and polymer. Out of 10 formulation trials, the F10 optimized trial was characterized for in vitro physicochemical parameters such as pH, homogeneity, viscosity, stability, drug content, in vitro drug release, in vitro antioxidant assay and ex vivo permeation study. Trial 10 was chosen as the best trial formulation among the other trials and was marked as an optimal trial. The physicochemical properties observed were pH to be 6.4 ± 0.01, the gel free of lumps, spreadability of 23.75 ± 0.03 and drug content of 32.77 ± 0.20 mg/g. It had no physiological changes such as color shift or fluid exudate segregation after 6 months of storage at room temperature. In vitro drug release established the presence of a non-fickian mechanism and demonstrated dose-dependent antioxidant activity. Ex vivo findings indicated 21.97 ± 0.18% release, proving that the gel can permeate through the oral mucosal membrane. Our future research will concentrate on expanding the therapeutic scope by developing the formulation trial F10 to a nanoformulation and conducting clinical trials for its potential use in various oral diseases. [ABSTRACT FROM AUTHOR]

Black locust flowers are the source of a significant amount of antioxidants that can be useful against free radicals formed on the skin after the environmental factors. Having in mind these facts, the ultrasound-assisted extraction of antioxidants from plant materials was previously developed. The aim of this study was to prepare a topical formulation based on the extract of black locust flowers. The extract enriched with antioxidants was prepared using the ultrasound-assisted extraction using 60% (v/v) ethanol at 60 °C and a liquidto-solid ratio of 10 mL/g for 30 min. The two topical formulations in the form of o/w emulsion at different concentrations of the extract (1% and 2%) were prepared by a hot-hot emulsification process. The product quality was estimated and concluded that the emulsion is white in the semi-solid state. The formulations can have adequate application properties due to their present ingredients, which do not leave a greasy film on the skin. The pH value of the prepared formulations was according to the allowed range for the application to the skin. The proper choice of ingredients enabled the achievement of satisfactory formulation stability. The formulations can be microbiologically safe to use for human purposes. A better antimicrobial activity against the investigated microorganism strains showed the formulation with higher content of the extract so it can be selected as an adequate for further analysis. [ABSTRACT FROM AUTHOR]

Docosanol is the only US Food and Drug Administration (FDA) approved over-the-counter topical product for treating recurrent oral-facial herpes simplex labialis. Validated analytical methods for docosanol are required to demonstrate the bioequivalence of docosanol topical products. A gas chromatography/selected ion monitoring mode mass spectrometry (GC/SIM-MS) method was developed and validated for docosanol determination in biological samples. Docosanol and isopropyl palmitate (internal standard) were separated on a high-polarity GC capillary column with (88% cyanopropy)aryl-polysiloxane employed as the stationary phase. The ions of m/z 83 and 256 were selected to monitor docosanol and isopropyl palmitate, respectively; the total run time was 20 min. The GC/SIM-MS method was validated in accordance with US FDA guidelines, and the results met the US FDA acceptance criteria. The docosanol calibration standards were linear in the 100–10000 ng/mL concentration range (R2>0.994). The recoveries for docosanol from the receptor fluid and skin homogenates were >93.2% and >95.8%, respectively. The validated method was successfully applied to analyze ex vivo human cadaver skin permeation samples. On applying Abreva® cream tube and Abreva® cream pump, the amount of docosanol that penetrated human cadaver skin at 48 h was 21.5 ± 7.01 and 24.0 ± 6.95 ng/mg, respectively. Accordingly, we concluded that the validated GC/SIM-MS was sensitive, specific, and suitable for quantifying docosanol as a quality control tool. This method can be used for routine analysis as a cost-effective alternative to other techniques.

Superficial pyoderma is a common skin disease caused by coagulase-positive staphylococci, especially Staphylococcus pseudintermedius and Staphylococcus aureus. The therapeutic use of antibiotics has many unwanted impacts, and the incidence of drug-resistant strains is increasing. Therefore, the aims of this non-inferior randomized controlled trial were to determine the effectiveness of 5% w/w clove essential oil lipid-based spray in treating superficial pyoderma in dogs, compared to 2% w/v chlorhexidine gluconate spray, and to evaluate the potential skin irritation of the clove oil spray formulation. The results demonstrated that the therapeutic effect of the clove essential oil spray was non-inferior to chlorhexidine gluconate spray when applied topically 2 times a day for 15 days. The clinical lesion index scores of dogs treated with clove essential oil spray were reduced by 66.87% on day 10 and 83.73% on day 15 after initiating treatment, with no adverse effects. The skin irritation test showed that clove essential oil spray did not induce erythema or edema at the tested sites. This report suggests that a lipid-based clove essential oil spray formulation is a suitable alternative topical treatment for canine superficial pyoderma.

Industrial hemp (Cannabis sativa L.), due to its bioactive compounds (terpenes and cannabinoids), has gained increasing interest in different fields, including for medical purposes. The evaluation of the safety profile of hemp essential oil (EO) and its encapsulated form (nanoemulsion, NE) is a relevant aspect for potential therapeutic applications. This study aimed to evaluate the toxicological effect of hemp EOs and NEs from cultivars Carmagnola CS and Uso 31 on three cell lines selected as models for topical and inhalant administration, by evaluating the cytotoxicity and the cytokine expression profiles. Results show that EOs and their NEs have comparable cytotoxicity, if considering the quantity of EO present in the NE. Moreover, cells treated with EOs and NEs showed, in most of the cases, lower levels of proinflammatory cytokines compared to Etoposide used as a positive control, and the basal level of inflammatory cytokines was not altered, suggesting a safety profile of hemp EOs and their NEs to support their use for medical applications.

Objective: Microemulgel is composed of aqueous phase, lipophilic phase, along with surfactant and co-surfactant, a suitable gelling agent is also incorporated. The drug Ibuprofen is non-steroidal anti-inflammatory drug. Its oral administration associated with many GIT, hepatic and renal problems. The main objective of the study was to formulate a stable topical microemulgel of ibuprofen in order to achieve the highest bioavailability with least side effects. Method: Pseudo ternary phase diagram was constructed in order to get the suitable concentrations of lipophilic phase, surfactant and co-surfactant. Phase titration method was used to prepare microemulsion, with surfactant and co-surfactant in a ratio of 2:1 respectively, along with gelling agent to form microemulgel. Formulations were evaluated to check appearance, pH, flowability, particle size, drug content, spreadability, drug release and skin irritation. Results: The globule size of microemulsion was 400 nm and zeta potential was -14 mV showing acceptable stability. Formulated emulgel showed good physical characteristics, suitable pH of 6.4 for skin. The drug content was 98.474%. The stability study showed that the ibuprofen was stable in phosphate buffer pH of 6.8. The carbopol 940 as a gelling agent showed high release rate values. The release rate of the optimized formulation, F1 was 94% and it followed Korsmeyer Peppas model (n=0.467). Conclusion: The prepared formulation was cost-effective because of promising highest bioavailability. The results suggest the potential use of developed microemulgel is mainly for topical delivery of ibuprofen, ensuring the safe use.

[Display omitted] • Effects of lycopene-based emulgel on biophysical parameters of human skin were evaluated. • Potent antioxidant potential of lycopene halted the cascade of free radical-related subsequent reactions in the skin. • Skin hydration and elasticity were significantly increased, while melanin, erythema, and sebum were considerably reduced. • Results proved the consumer acceptability for aging and oxidative stress-related skin disorders. Carotenoids, including lycopene, are promising antioxidants that sequester free radicals and counterbalance oxidative stress, preventing cardiovascular diseases, cancer, photo-damage, and decelerating aging. Fabricating the antioxidant effective and stable topical formulations with efficient skin penetration and preserving their activity by minimizing the oxidative damage due to ionization, pH extremes, high storage temperature, and metal ions, has been challenging. Herein, we developed a lycopene-based topical emulgel and investigated its impact on biophysical parameters of human skin using non-invasive in vivo techniques and sensory evaluation for consumer acceptability to bottleneck the demerits of conventional formulations. The results demonstrated that the designed formulation significantly enhanced the skin hydration and elasticity, p-value < 0.05, whereas erythema, melanin and sebum contents were considerably reduced, p-value < 0.05, when compared with placebo formulation over 12 weeks. These findings were attributed to the potent antioxidant potential of lycopene that was preserved in the stable formulation, halting the cascade of free radical-related subsequent reactions in the skin. To the best of our knowledge, there is no report about the topical effects of lycopene-based emulgel in human volunteers. Besides, the average scores by the volunteers concerning sensory evaluation at the end of the 12th week of the study indicated that the formulation will be commercially acceptable by the consumers. We believe that formulation will be valuable commercially in promoting the treatment of topical infections, such as acne, and oxidative stress-related skin disorders, and decelerating the aging process. [ABSTRACT FROM AUTHOR]

The review's goal is to make and survey a drug gel made of both normal and counterfeit polymers. Gel measurements structures function admirably as medication conveyance techniques since they accommodate exact medication discharge control and natural security for the drugs. Various physicochemical parts of the gel that influence its attributes are likewise explored. We have accumulated sources from recently distributed examination and survey articles. We gathered data from 20-25 papers. Drug gel is surveyed for its capacity to gel, for its solidarity, for its bioadhesion, for its spreadability, for microbiological research, and for in vitro discharge. Because of our exploration, we have arrived at the resolution that skin medicine conveyance is an engaging procedure for both nearby and foundational medicines and is regularly utilized in the administration of provocative ailments such dermatological illnesses and outer muscle wounds. The perils associated with the different conditions of retention, for example, pH changes, the presence of proteins, and gastric exhausting time, are kept away from by effective arrangement, alongside the dangers and burdens of intravenous treatment and gastrointestinal infections. Furthermore, the medication has a higher bioavailability and acts at the activity site right away. The gel not entirely settled to be an extremely encouraging option for skin or transdermal treatment. To completely grasp the course of drug gel-incited wound recuperating, more examination should be finished. [ABSTRACT FROM AUTHOR]

The main objective of this investigation was to formulate Fluconazole microsponge by quasi emulsion solvent diffusion technique in order to provide sustained release. Microsponge was formulated by quasi emulsion solvent diffusion technique with varied drug-polymer ratios. Ethyl cellulose and Eudragit L-100 was used as a polymers and polyvinyl alcohol was used as a surfactant for the preparation of external phase. The prepared microsponges were characterized by Fourier transform infrared spectroscopy, particle size analysis, and evaluated for pH, spreadability, viscosity, surface morphology, drug content, entrapment efficiency, in vitro drug release, skin irritation test, antifungal activity as well. The formulated microsponges are spherical with a porous surface and 6.8 µm of mean particle size. The microsponges were then integrated into the carbopol gel. The In vitro drug release results showed that microsponges with 1:1 drug-polymer ratios were more effective to make a prolonged drug release of 89.318 % at the end of 8 hours. Consequently the formed microsponge-based gel of fluconazole would be a confident decision for formal treatment for protected and powerful treatment of fungal infections. [ABSTRACT FROM AUTHOR]