Skin Permeation Research Articles

Improved Topical Delivery of Sorafenib-Meglumine Antimoniate: Elastic Nano-Liposomal Formulation for the Treatment of Cutaneous Leishmaniasis

Background: Cutaneous leishmaniasis (CL) is a widespread parasitic disease with significant health and social impacts. Current systemic treatments have severe side effects, highlighting the need for effective topical alternatives.Objective: This study aimed to develop and evaluate the effectiveness of sorafenib (SF) and meglumine antimoniate (MM) dual-loaded transferosomes (TRs) for topical treatment of CL.Methods: TRs were prepared using a thin film hydration method and incorporated into a carbopol gel. The formulations were characterized for vesicle size, zeta potential, entrapment efficiency, and deformability index. In vivo and ex vivo skin permeation studies were conducted, along with anti-leishmanial efficacy testing on an intramacrophage amastigote model using BALB/c mice.Results: The TRs exhibited a vesicle size of 186.1 ± 65.89 nm, zeta potential of -27.9 mV, and entrapment efficiency of 71.7 ± 3.9% for MM and 78.6 ± 4.2% for SF. Ex vivo studies showed enhanced skin permeation with cumulative permeation of 327.6 ± 29.4 µg/cm² for MM and 291.6 ± 28.3 µg/cm² for SF. In vivo results indicated a significant reduction in lesion size (0.1 ± 0.12 mm) and parasite load (2.7 ± 0.3 log scale).Conclusion: The MM-SF dual-loaded TRs demonstrated effective topical delivery and therapeutic potential for CL, providing a promising alternative to systemic treatments.

Chondroitin Sulfate for Cartilage Regeneration, Administered Topically Using a Nanostructured Formulation.

In the pharmaceutical sector, solid lipid nanoparticles (SLN) are vital for drug delivery incorporating a lipid core. Chondroitin sulfate (CHON) is crucial for cartilage health. It is often used in osteoarthritis (OA) treatment. Due to conflicting results from clinical trials on CHON's efficacy in OA treatment, there has been a shift toward exploring effective topical systems utilizing nanotechnology. This study aimed to optimize a solid lipid nanoparticle formulation aiming to enhance CHON permeation for OA therapy. A 3 × 3 × 2 Design of these experiments determined the ideal parameters: a CHON concentration of 0.4 mg/mL, operating at 20,000 rpm speed, and processing for 10 min for SLN production. Transmission electron microscopy analysis confirmed the nanoparticles' spherical morphology, ensuring crucial uniformity for efficient drug delivery. Cell viability assessments showed no significant cytotoxicity within the tested parameters, indicating a safe profile for potential clinical application. The cell internalization assay indicates successful internalization at 1.5 h and 24 h post-treatment. Biopharmaceutical studies supported SLNs, indicating them to be effective CHON carriers through the skin, showcasing improved skin permeation and CHON retention compared to conventional methods. In summary, this study successfully optimized SLN formulation for efficient CHON transport through pig ear skin with no cellular toxicity, highlighting SLNs' potential as promising carriers to enhance CHON delivery in OA treatment and advance nanotechnology-based therapeutic strategies in pharmaceutical formulations.

Optimizing Dermal Delivery of Linezolid for Treating Skin and Soft Tissue Infections: NLC-Based Gel Formulation Using Taguchi Design

Background: Uncomplicated skin and soft tissue infections account for approximately 200 million visits to ambulatory care settings annually. Linezolid (LNZ) is an oxazolidinone that has proven its effectiveness in combating skin and soft tissue infections caused by gram-positive pathogens. LNZ is administered via oral suspension, tablets, or an intravenous route in most in-stances. However, its extended therapy leads to undesirable side effects like diarrhoea, thrombo-cytopenia, myelosuppression, lactic acidosis, etc. and even life-threatening complications. The dermal administration of LNZ offers an alternative route, ensuring localized and sustained release at the site of infection. This approach may reduce systemic exposure and allow for lower doses compared to oral ingestion, which can decrease the risk of adverse effects. Objective: This research aimed to develop a nanostructured lipid carrier (NLC)-based gel for de-livering LNZ via the dermal route to treat uncomplicated skin and soft tissue infections. Methods: NLC were developed by high-shear homogenisation and sonication method using glyc-eryl trimyristate as a solid lipid and neem oil as a liquid lipid. The Taguchi design was employed to optimize NLCs using surfactant concentration (mg), drug-to-lipid ratio, and sonication time (sec) as independent variables. Their effect on particle size, zeta potential, and entrapment effi-ciency was studied. The optimized nanocarriers were developed into a gel product and evaluated for drug release, permeation, and antibacterial activity. Results: The optimised process parameters to attain outcomes were 2% surfactant, 1:1 drug-to-lipid ratio and 300 seconds of sonication. The resulting NLC had an average size of 191.2 ± 2.76 nm, a zeta potential of -30.7 ± 4.50 mV, and 84.89 ± 2.76% drug entrapment. NLC-based gel dis-played anomalous transport with a 90.16 % drug release. The gel showed a strong antibacterial effect against Staphylococcus aureus with a 7.57 ± 0.12 cm mean zone of inhibition. Ex-vivo skin permeation studies revealed 24.19 ± 0.19 % drug permeation and 64.46 ± 0.58% cutaneous depo-sition. NLC-based gel demonstrated a significant decrease in colony-forming units in infected an-imal models. Conclusion: The ex-vivo investigations demonstrated the presence of LNZ at the infection site, enhancing therapeutic effectiveness. In vitro and in-vivo findings illustrated the substantial anti-bacterial efficacy of LNZ NLC-based gel. The adoption of NLC-based gel exhibits promising po-tential as a carrier for dermal delivery of LNZ.

Formulation and Evaluation of Acyclovir Loaded Transferosomal Gel for Transdermal Drug Delivery

Background: A carrying structure for targeted transdermal drug delivery is a transferosome. These unique liposomes are made of an edge activator and phosphatidylcholine. The most common antiviral drug is acyclovir, a synthetic nucleotide nucleoside analog derived from guanine. It works well to cure the varicella-zoster virus and the virus that causes herpes simplex (HSV), primarily HSV-1 and HSV-2. But its skin permeability is minimal. Therefore, this work aimed to use transferosomes to prepare acyclovir so that it could pass through the skin's barrier function. Objective: This study uses a 32-factorial factorial design to develop a transferosomal gel containing acyclovir through thin-film hydration method for painless acyclovir delivery services for skin disease treatment. Material and Methods: The independent variables are the amount of phospholipid (X1) and tween 80 (X2), while the dependent variables are particle size (Y1) and percentage entrapment efficiency (Y2). To create an ideal formulation, the produced transferosomes were assessed for particle size, in vitro drug release amount, and entrapment efficiency (EE%). A Carbopol 934 gel basis was prepared using the optimized acyclovir transferosome formulation, and its drug concentration, pH, spreadability, viscosity, and stability were assessed. Results: With small particles ranging from 176.6 to 324.4 nm, the produced acyclovir transferosomes had a high EE% range from 66.34 to 76.42 %. According to the in vitro release study, there is a negative correlation between in vitro release and EE%. The formulation TF5, including 1%w/w of carbopol 940, provides a superior profile of drug absorption in vitro. Consequently, acyclovir can enter the skin as transferosomes and cross the stratum corneum barrier. Conclusion: Acyclovir can be transformed into a transfersomal gel, which will improve antiviral efficacy, get over the skin's protective layer, prevent adverse oral reactions, and eventually improve patient adherence. Keywords: Transferosome, Transdermal drug delivery system, Acyclovir, 32 Fractional factorial design, Carbopol 934

Green formulation of Menadione-loaded niosome as a skin-lightening preparation: In vitro/In vivo safety evaluation on Wistar rat

Purpose: In the present research, a green technique (an ultrasonic method) was used to synthesize menadione sodium bisulfite (MSB) niosome (Menasome) which is used to improve dermal delivery and increase anti-melanogenesis activities. Methods: Various cholesterol: surfactant (Chol: Sur) ratios were investigated to optimize the Menasomes. Photon correlation spectroscopy, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), transmission electron microscopy (TEM), and differential scanning calorimetry (DSC) were employed to characterize the solid state of MSB in nanoparticle form. Additionally, the optimized formulation was used to investigate ex-vivo skin absorption, in vivo skin irritation, in vitro cell survival, and anti-melanogenesis activity. Results: The results exhibited that increasing cholesterol (Chol) declined the average size of the Menasomes from 653.766±25.171 nm to 298.133±8.823 nm and increased entrapment efficiency 30.237±3.4204% to 83.616±2.550 %. The rat skin permeation study indicated that Menasome gel administered more MSB in dermal layers (439.000±36.190μg/cm2 or 23.827±1.964%) than MSB plain gel (286.200± 22.6μg/cm2 or 15.53±1.227%). In both the in vivo skin irritation test and the in vitro cytotoxicity experiment, the extended-release behavior of the enhanced Menasome demonstrated a minimal side effect profile. Furthermore, optimum Menasome inhibited melanin formation (37.426± 1.644% at 15μM) greater than free MSB (57.383±1.654%) considerably (p <0.05). Furthermore, Menasome 7 prevented L-dopa auto-oxidation in higher levels (95.140±2.439%) than pure MSB solution (83.953±1.629%). Conclusion: According to the study's findings, the prepared Menasome could be employed as a viable nanovehicle for MSB dermal delivery, a promising solution for the management of human hyperpigmentation disorders.

Energy-based methods and nanocarrier-based approaches for melasma treatment

Melasma is a chronic disease caused by excessive melanin production in the skin, affecting the quality of life, especially in women. As a kind of skin hyperpigmentation, it can be caused by sun exposure, genetics, hormones, drugs, or inflammation. Melasma treatment can be effective when the product penetrates well into the skin. As an essential skin barrier, the stratum corneum displays a significant role in topical and transdermal drug delivery. In this regard, numerous strategies have been developed to increase the skin permeability and efficiency of drugs. This review explores energy-based methods and nanocarrier-based approaches for melasma treatment, focusing on enhancing drug delivery to the viable epidermis and overcoming SC. Physical methods have some advantages like increasing the skin penetration and also some drawbacks, including frequent visits, high costs, and the need for advanced equipment and trained operators. Further, these methods are often combined with high energy and special technics. As an emerging physical-based method that could be used to treat patients with multiple medications, microneedle patch is drawing interest due to its ease of use, ability to pinpoint drug delivery, and fewer side effects. In addition, they can penetrate drug molecules into deeper layers of skin and provide more sustainable results compared to conventional methods. Nanocarrier-based systems like transferosome and ethosome (deformable liposomes) are also effective options for skin penetration and treating melasma and skin hyperpigmentation. Despite several benefits, such as high entrapment efficiency, good permeation, and increased bioavailability of drugs through the skin, their stability problems and limitations toward nanoparticle production on an industrial scale are the most significant drawbacks of this method. In the current review, we looked at the articles published between 2010 and August 2023 on energy-based methods and nanocarriers-based approaches have been used to treat melasma.

Enhanced diclofenac sodium delivery through advanced self-microemulsifying pectin-based transdermal patches

Diclofenac sodium (DCFNa) presents significant challenges in local pain relief due to its poor solubility and limited skin permeability. This study aimed to enhance the solubility and skin permeation of DCFNa by developing DCFNa-loaded self-microemulsifying drug delivery system (SMEDDS) embedded pressure-sensitive adhesive (PSA) patch. The solubility of DCFNa in various solvents was evaluated, and a ternary phase diagram was constructed to optimize the SMEDDS formulation. The transdermal patch, composed of pectin and polyacrylate, was optimized using a simplex lattice experimental design to achieve the desired adhesion strength and to select the most suitable patch for skin drug accumulation study. Clove oil, Tween® 80, and propylene glycol were identified as the appropriate oil, surfactant, and co-surfactant, respectively, for achieving highest DCFNa solubility. The SMEDDS was formed with a ratio of 5:35:60 (oil: Smix [1:1 surfactant: co-surfactant]: water), yielding nano-sized droplets (22.64 ± 0.74 nm) and significantly enhancing DCFNa solubility (329.62 ± 10.16 mg/mL) compared to phosphate buffer (5.03 ± 1.01 mg/mL). The DCFNa-loaded SMEDDS demonstrated a 9-fold increase in skin permeability compared to the DCFNa solution. The optimized PSA patch, containing 20 % pectin and 40 % polyacrylate, exhibited superior tacking and peel strength. Additionally, a 1 % DCFNa-loaded SMEDDS patch delivered twice greater drug accumulation in the skin and showed no skin irritation, maintaining better adhesion for up to 24 h compared to commercial patches.

In vitro assessment of skin permeation properties of enzymatically derived oil-based fatty acid esters of vitamin C.

Current topical formulations containing vitamin C face limitations in therapeutic effectiveness due to the skin's selective properties that impede drug deposition. Consequently, the widespread use of toxic and irritating chemical permeation enhancers is common. Hereby, we investigated enzymatically derived fatty acid ascorbyl esters (FAAEs) obtained using natural oils for their skin permeation properties using the Strat-M® skin model in a Franz cell diffusion study. By evaluating various cosmetic formulations without added enhancers, we found that emulgel is most suitable for enhancing the cutaneous and transdermal delivery of FAAEs. Furthermore, medium-chain coconut oil-derived FAAEs exhibited faster diffusion rates compared to sunflower oil-based FAAEs with long-side acyl residues, including the commonly applied ascorbyl palmitate. Experimental data were successfully fitted using the Peppas and Sahlin model, which accounted for a lag phase and the combined effect of Fickian diffusion and polymer relaxation. In the case of long-chain esters, the lag phase was prolonged, and the calculated effective diffusion coefficients (Deff) were lower compared to medium-chain FAAEs. Accordingly, the highest Deff value was observed for ascorbyl caprylate, being even 60 times higher than for ascorbyl palmitate. These results suggest the emerging potential of emulgel with incorporated coconut oil-derived FAAEs for efficiently delivering vitamin C into the skin.

Antinociceptive activity of transdermal nanostructured surfactant-based systems containing duloxetine hydrochloride

Duloxetine hydrochloride (DLX) is a serotonin and norepinephrine reuptake inhibitor that is effective in the treatment of chronic pain. However, the drug has several adverse reactions and extensive hepatic first-pass effect. This study aimed at developing surfactant-based formulations such as liquid crystals (LCs) and evaluating the influence of the formulations on DLX skin permeation and in vivo antinociceptive activity. Thereafter, the formulations were obtained using PEG-40 Hydrogenated Castor Oil, Tween 80, licuri oil and water. The systems selected showed isotropy, high viscosity and rheology suggestive of LCs. The systems presented ability to permeate DLX through the skin. ATR-FTIR demonstrated that formulations promoted lipid disorganization and modification of protein conformation, facilitating the drug diffusion through the stratum corneum. Moreover, the formulation loaded with DLX showed high antinociceptive activity in mice (tests of acetic acid-induced abdominal writhing, formalin and tail immersion) via the transdermal route. The antinociceptive activity was close to that of morphine (i.p.). In conclusion, the LC obtained proved to be a promising system for transdermal delivery of DLX and pain management.

A Self-Skin Permeable Doxorubicin Loaded Nanogel Composite as a Transdermal Device for Breast Cancer Therapy.

Modern drug delivery research focuses on developing biodegradable nanopolymer systems. The present study proposed a polymer-based composite nanogel as a transdermal drug delivery system for the pH-responsive targeted and controlled delivery of anticancer drug doxorubicin (DOX). Nanogels have properties of both hydrogels and nanomaterials. The β-cyclodextrin-based nanogels can enhance the loading capacity of poorly soluble drugs and promote a sustained drug release. The β-cyclodextrin-grafted methacrylic acid conjugated hyaluronic acid composite nanogel was successfully synthesized. β-Cyclodextrin was first grafted onto methacrylic acid. The composite nanogel-based drug carrier was prepared by controlled radical polymerization (CRP) of β-cyclodextrin-grafted methacrylic acid with hyaluronic acid. The doxorubicin-loaded carrier was characterized by Fourier transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, ultraviolet-visible (UV-vis) spectroscopy, zeta potential analysis, dynamic light scattering (DLS), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). The drug loading and release efficiencies were carried out at different pH levels. The maximum drug loading and encapsulation efficiencies of the synthesized final nanogel composite material at pH 8.0 were 86.44 ± 2.12 and 96.07 ± 2.01%, respectively. The DOX-loaded final material showed a 90.0 ± 2.6% release percentage of DOX at pH 5.5, whereas at pH 7.4, the release percentage of DOX was observed to be only 35.0 ± 0.3%. In vitro swelling, degradation, hemocompatibility, drug release kinetics, cytotoxicity, apoptosis, cell colocalization, skin irritation, and skin permeation studies, along with in vivo pharmacokinetic studies, were performed to prove the efficacy of the synthesized nanogel composite as a transdermal carrier for doxorubicin.

Peptide Drones Facilitating the Transdermal Delivery of Antitumor Proteins for Melanoma Treatment

AbstractTopical treatment offers a viable alternative for melanoma patients incompatible with surgical interventions. Herein, the study develops a skin‐penetrating peptide (SPP)‐based peptide drone (PD) for the transdermal delivery of antitumor proteins. To achieve cost‐effective therapeutics, Concanavalin A (ConA), which can be prepared through an extraction method, is loaded onto PDs. Compared with free proteins, ConA‐PD complexes (CPCs) demonstrate significantly greater skin permeation. Moreover, the CPCs exhibit potent anticancer activity both in vitro and in vivo, which substantially surpass the efficacy of the Aldara (imiquimod) cream. The CPC‐treated mouse skin remains clear, whereas Aldara cream induces side effects, including psoriasis‐like skin inflammation. The antimetastatic activity of the PD is identified as another advantage of CPC. The use of ConA as an anticancer agent has been significantly limited due to its high hepatotoxicity; however, the transdermal delivery strategy minimizes its hepatic absorption and, in turn, results in negligible hepatotoxicity. These results demonstrate the potential of the CPC as a novel therapeutic agent or an adjunct to other modalities for melanoma treatment, overcoming the limitations of existing materials while exhibiting superior efficacy.

Formulation, optimization and evaluation of ibuprofen loaded menthosomes for transdermal delivery

The study aimed to improve the transdermal permeation of IBU utilizing menthosomes as a vesicular carrier. IBU-loaded menthosomes were formulated by thin film hydration & optimized using 23 factorial designs (Design Expert® version 13 software). In vitro &ex vivo skin permeation analysis of IBU-encapsulated menthosomes was studied across the rat skin sample. In vivo pharmacodynamic activity was studied in an arthritis rat model. The optimized IBU-loaded menthosomes exhibited an optimum vesicle size of 214.2 ± 2.96 nm, Zeta potential of −21.1 ± 2.72 mV, (PDI) Polydispersity Index of 0.267 ± 0.018 with Entrapment efficiency (EE%) of 78.7 ± 2.73 %. The in vitro &ex vivo skin penetration study displayed enhanced release of drug of 77.02 ± 1.0 % and 40.91 ± 0.81 % respectively, compared to conventional liposomes. In vivo pharmacodynamic study on carrageenan-induced paw edema in Wistar albino rats demonstrated superior anti-inflammatory activity of the optimized IBU-encapsulated menthosomes (**p < 0.01) and effective inhibition of paw edema (34.04 ± 0.155 %). The formalin test indicated a significant analgesic effect of optimized formulation during the chronic phase of analgesia (*p < 0.05) compared to the control group. Thus, the developed and optimized drug-loaded menthosomes could serve as a suitable vesicular delivery carrier in enhancing the transdermal delivery of other NSAID drugs.

Skin deposition and permeation kinetics of cannabidiol and delta-9-tetrahydrocannabinol from cannabis extract containing gels

The study aimed to investigate the deposition and permeation characteristics of phytocannabinoids, namely delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD), from cannabis extract containing gels. Cannabis extract with 26.3 % CBD and 28.4 % THC was used. The impact of permeation enhancers, namely propylene glycol, diethylene glycol monoethyl ether (DEGEE), ethanol (EtOH), and terpenes (eucalyptol and menthol), was examined. All cannabis extract gels had a pH range of 6.71–6.81 and a viscosity range of 456.6–4068.7 mPa⋅s. The phytocannabinoid release from the gels followed Zero-order kinetics with a rate of 14.5–25.7 μg⋅h−1 for CBD and 10.0−22.6 μg⋅h−1 for THC. A gel containing 12.5 % DEGEE and 12.5 % EtOH exhibited the highest release rate. The initial skin deposition followed Zero-order kinetics and reached a maximum level after 4 h. Permeation of phytocannabinoids closely followed Higuchi kinetics, with a rate of 0.14–54.21 μg⋅h−1/2 for CBD and 0.23−67.02 μg⋅h−1/2 for THC. A gel containing 25 % DEGEE and 25 % EtOH exhibited the highest apparent skin partition coefficient (K) value, resulting in the greatest phytocannabinoid deposition and permeation. Terpene introduction (5 %) significantly reduced the release rate, K value, and total skin absorption of phytocannabinoids. These findings offer useful insights into selecting the appropriate vehicle for cannabis extract topical products.

Topical Delivery of Dual Loaded Nano-Transfersomes Mediated Chemo-Photodynamic Therapy against Melanoma via Inducing Cell Cycle Arrest and Apoptosis.

Melanoma is a malignant skin cancer associated with high mortality rates and drug resistance, posing a significant threat to human health. The combination of chemotherapy and photodynamic therapy (PDT) represents a promising strategy to enhance antitumor efficacy through synergistic anti-cancer effects. Topical delivery of chemotherapeutic drugs and photosensitizers (PS) offers a non-invasive and safe way to treat melanoma. However, the effectiveness of these treatments is often hindered by challenges such as limited skin permeability and instability of the PS. In this study, transfersomes (TFS) were designed to facilitate transdermal delivery of the chemotherapeutic drug 5-Fluorouracil (5-FU) and the PS Imperatorin (IMP) for combined chemo-photodynamic therapy for melanoma. The cytotoxic and phototoxic effects of TFS-mediated PDT (TFS-UVA) were investigated in A375 cells and nude mice. The study also demonstrated that TFS-UVA generated intracellular ROS, induced G2/ M phase cell cycle arrest, and promoted cell apoptosis. In conclusion, this study indicated that 5-FU/ IMP-TFS serves as an effective transdermal therapeutic strategy for chemo-PDT in treating melanoma.

Photodynamic Therapy as a Novel Therapeutic Modality Applying Quinizarin-Loaded Nanocapsules and 3D Bioprinting Skin Permeation for Inflammation Treatment.

Skin inflammation associated with chronic diseases involves a direct role of keratinocytes in its immunopathogenesis, triggering a cascade of immune responses. Despite this, highly targeted treatments remain elusive, highlighting the need for more specific therapeutic strategies. In this study, nanocapsules containing quinizarin (QZ/NC) were developed and evaluated in an in vitro model of keratinocyte-mediated inflammation, incorporating the action of photodynamic therapy (PDT) and analyzing permeation in a 3D skin model. Comprehensive physicochemical, stability, cytotoxicity, and permeation analyses of the nanomaterials were conducted. The nanocapsules demonstrated desirable physicochemical properties, remained stable throughout the analysis period, and exhibited no spectroscopic alterations. Cytotoxicity tests revealed no toxicity at the lowest concentrations of QZ/NC. Permeation and cellular uptake studies confirmed QZ/NC permeation in 3D skin models, along with intracellular incorporation and internalization of the drug, thereby enhancing its efficacy in drug delivery. The developed model for inducing the inflammatory process in vitro yielded promising results, particularly when the synthesized nanomaterial was combined with PDT, showing a reduction in cytokine levels. These findings suggest a potential new therapeutic approach for treating inflammatory skin diseases.

Sanguisorba officinalis L. ethanolic extracts and essential oil - chemical composition, antioxidant potential, antibacterial activity, and ex vivo skin permeation study.

Sanguisorba officinalis L. is classified as a medicinal plant and used in traditional medicine. The root of this plant is mainly used as a medicinal raw material, but the above-ground parts are also a valuable source of health-promoting biologically active compounds. The study aimed to evaluate the antioxidant activity and total polyphenol content (TPC) of extracts prepared in 70% and 40% aqueous ethanol solution (dry extract content 50-500g/L) from the aerial parts of S. officinalis. The essential oil was isolated from the tested raw material, and its composition was determined using GC-MS. Ethanolic extracts and essential oil have been tested for antibacterial activity. The extract in 70% v/v ethanol (dry extract content: 500g/L) was subjected to HPLC analysis for the content of selected phenolic acids and an ex vivo skin permeation study. The ability of these metabolites to permeate and accumulate in the skin was analysed. Extracts prepared at both ethanol concentrations showed similar antioxidant activity and TPC. Depending on the method, concentration of solvent, and dry extract content (50-500g/L), the activity ranged from 1.97 to 84.54g Trolox/L. TPC range of 3.80-37.04gGA/L. Gallic acid (424mg/L) and vanillic acid (270mg/L) had the highest concentrations among the phenolic acids analysed. Vanillic acid (10μg) permeates the skin at the highest concentration. The highest accumulation in the skin was found for 2,5-dihydroxybenzoic acid (53μg/g skin), 2,3-dihydroxybenzoic acid (45μg/g skin), and gallic acid (45μg/g skin). The tested ethanolic extracts exhibited antibacterial activity. Samples with a dry extract concentration of 500g/L showed the largest growth inhibition zones. The most sensitive strains to these extracts were P. aeruginosa (24mm), S. lutea (23mm), and S. pneumoniae (22mm). The smallest inhibition zones were observed for B. subtilis (17mm). The essential oil showed weaker antimicrobial activity (growth inhibition zone 8-10mm). The GC-MS method identified 22 major components of the essential oil, including aliphatic hydrocarbons, unsaturated terpene alcohols, aliphatic aldehydes, unsaturated and saturated fatty acids, sesquiterpene, phytyl ester of linoleic acid, nitrogen compound, phytosterol, terpene ketone, phenylpropanoids, aliphatic alcohol, diterpenoid, aromatic aldehyde, and aliphatic carboxylic acid. The conducted research has shown that ethanolic extracts from Sanguisorbae herba are a valuable source of compounds with antibacterial and antioxidant potential, including phenolic acids. The fact that selected phenolic acids contained in the tested extract have the ability to permeate and accumulate in the skin provides the basis for conducting extended research on the use of extracts from this plant raw material in cosmetic and pharmaceutical preparations applied to the skin.

Characterization, stability, and skin application of astaxanthin particulates

PurposeAstaxanthin (AX), commonly used for dermal applications, exhibits anti-inflammatory and antioxidant activities; however, it has poor water solubility. In this study, we investigated the physicochemical properties of AX-containing particulates formulated using the amphiphilic graft copolymer Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer: Sol) and polyethylene glycol-2000 (PEG 2000); in addition, the stability and skin applications of AX particulates were investigated.MethodsAX, Sol, and PEG were mixed by weight to prepare AX particles using the hydration method. The prepared particles were subjected to stability evaluations including particle size distribution, zeta potential estimation, and fluorescence spectroscopy as well as physical evaluations including 1H-1H NOESY NMR spectral measurement, powder X-ray diffraction, and differential scanning calorimetry. Functional evaluations included singlet oxygen scavenging, skin permeation test, and fluorescence microscopy.ResultsRelatively stable particles of Sol/AX and Sol/PEG 2000/AX, approximately 100 nm and 125 nm in size, respectively, were formed at a mixed weight ratio (9/1) of 0.1 M Ascorbic Acid solution (0.1 M ASC) and a mixed weight ratio (8/1/1) of 0.1 M ASC, respectively, at 25 °C after storage for 14 days under light-shielded condition. Stability evaluations revealed a decrease in fluorescence intensity and color fading for Sol/AX = 9/1 and Sol/PEG 2000/AX = 8/1/1 (dispersion medium: distilled water); however, no change in fluorescence intensity of AX was observed immediately after preparation in Sol/AX = 9/1 and Sol/PEG 2000/AX = 8/1/1 (dispersion medium: 0.1 M ASC). The fluorescence intensity of AX did not fluctuate significantly immediately after adjustment, and the particles remained stable, showing a bright orange color with time. NMR spectra of Sol/AX = 9/1 and Sol/PEG 2000/AX (dispersion medium: 0.1 M ASC) showed the interactions between the CH3 group e from Sol (1.8 ~ 2.0 ppm) and the CH groups H-15,11 from AX (6.7 ~ 6.8 ppm), 8’,12’ (6.4 ~ 6.5 ppm), H-10,14 (6.4 ~ 6.5 ppm), and 7,7’ (6.2 ~ 6.3 ppm), indicating the disappearance of cross peaks. Furthermore, new cross peaks were identified for the CH3 group e of Sol (1.8 ~ 2.0 ppm), the 7-membered ring z of Sol (1.5 ~ 1.8 ppm), the 5-membered ring S of ASC (3.5 ~ 3.6 ppm), the CH group T (3.8 ~ 3.9 ppm), and the CH group U (4.7 ppm). Fluorescence microscopy observations of microparticles formulated with Sol/PEG 2000/AX showed a slight improvement in skin penetration.ConclusionNew AX particulates were formed using Sol/PEG 2000/AX = 8/1/1, suggesting that Sol/PEG 2000/AX maintained the stability and improved the skin penetration of AX.

Nanotechnology: Current Developments, Applications and Patents for Non-invasive Topical Cosmetics and Dermatological Therapeutic Delivery

: Nanotechnology exhibits the advancement in the field of invention, by improving the potency of the formulation through the delivery of inventive solutions. To resolve several limita-tions related to conventional formulations, nanotechnology applications are increasing in the cosmetics and dermatological area. Cosmetic and dermatological preparations are considered a thriving branch of the body care arena and their usage has increased dramatically through the past years. Scientists are designing innovative delivery mechanisms and emerging innovations that are presently being utilized in the development of cosmetics. Inventive nanocarriers such as nio-somes, liposomes, microemulsions, nanoemulsions, solid-lipid nanoparticles, nanospheres, and nanostructured (lipid) carriers have substituted the use of traditional drug delivery. These innova-tive nanocarriers have the convenience of better skin permeation, sustained and controlled drug delivery, precise location, higher stability, and greater incorporated capability. Since the usage of cosmetics has increased, the usual delivery system has been substituted by modern delivery ap-proaches. The introduction of newer advancements and novel drug delivery systems make cos-metics and cosmeceuticals more popular with increased market share. This review article on nan-otechnology employed in cosmetics and dermatology emphasizes the numerous innovative nanocarriers designed for cosmetic and dermatologic drug delivery, their negative and positive aspects, and their toxicity.

Curcumin-loaded gold nanoparticles with enhanced antibacterial efficacy and wound healing properties in diabetic rats

Diabetic wounds pose a significant global health challenge. Although curcumin exhibits promising wound healing and antibacterial properties, its clinical potential is limited by low aqueous solubility, and poor tissue penetration. This study aimed to address these challenges and enhance the wound healing efficacy of curcumin by loading it onto gold nanoparticles (AuNPs). The properties of the AuNPs, including particle size, polydispersity index (PDI), zeta potential, percent drug entrapment efficiency (%EE) and UV–Vis spectra were significantly influenced by the curcumin/gold chloride molar ratio used in the synthesis of AuNPs. The optimal formulation (F2) exhibited the smallest particle size (41.77 ± 6.8 nm), reasonable PDI (0.59 ± 0.17), high %EE (94.43 ± 0.25 %), a moderate zeta potential (−8.44 ± 1.69 mV), and a well-defined surface Plasmon resonance peak at 526 nm. Formulation F2 was incorporated into Pluronic® F127 gel to facilitate its application to the skin. Both curcumin AuNPs solution and gel showed sustained drug release and higher skin permeation parameters compared with the free drug solution. AuNPs significantly enhanced curcumin’s antibacterial efficacy by lowering the minimum inhibitory concentrations and enhancing antibacterial biofilm activity against various Gram-positive and Gram-negative bacterial strains. In a diabetic wound rat model, AuNPs-loaded curcumin exhibited superior wound healing attributes compared to the free drug. Specifically, it demonstrated improved wound healing percentage, reduced wound oxidative stress, increased wound collagen deposition, heightened anti-inflammatory effects, and enhanced angiogenesis. These findings underscore the potential of AuNPs as efficacious delivery systems of curcumin for improved wound healing applications.

P19-17 Use of diverse human skin models in in vitro skin permeation testing of dermatological ingredients

P19-17 Use of diverse human skin models in in vitro skin permeation testing of dermatological ingredients