scholarly journals Ion-Pair Compounds of Strychnine for Enhancing Skin Permeability: Influencing the Transdermal Processes In Vitro Based on Molecular Simulation

2021 ◽  
Vol 15 (1) ◽  
pp. 34
Author(s):  
Lili He ◽  
Di Xiong ◽  
Lan Ma ◽  
Yan Liang ◽  
Teng Zhang ◽  
...  
Keyword(s):  
Molecular Simulation ◽  
Skin Permeation ◽  
Ion Pair ◽  
Skin Permeability ◽  
Energy Curve ◽  
Molar Ratios ◽  
In Vitro Permeation ◽  
Intercellular Lipid ◽  
Better Than

This research aimed to explore how Strychnine (Str) ion-pair compounds affect the in vitro transdermal process. In order to prevent the influence of different functional groups on skin permeation, seven homologous fatty acids were selected to form ion-pair compounds with Str. The in vitro permeation fluxes of the Str ion-pair compounds were 2.2 to 8.4 times that of Str, and Str-C10 had the highest permeation fluxes of 42.79 ± 19.86 µg/cm2/h. The hydrogen bond of the Str ion-pair compounds was also confirmed by Fourier Transform Infrared (FTIR) Spectroscopy, Nuclear Magnetic Resonance (NMR) Spectroscopy and molecular simulation. In the process of molecular simulation, the intercellular lipid and the viable skin were represented by ceramide, cholesterol and free fatty acid of equal molar ratios and water, respectively. It was found by the binding energy curve that the Str ion-pair compounds had better compatibility with the intercellular lipid and water than Str, which indicated that the affinity of Str ion-pair compounds and skin was better than that of Str and skin. Therefore, it was concluded that Str ion-pair compounds can be distributed from the vehicle to the intercellular lipid and viable skin more easily than Str. These findings broadened our knowledge about how Str ion-pair compounds affect the transdermal process.

In Vitro Skin Permeation Methodology for Over-The-Counter Topical Dermatologic Products

2019 ◽  
pp. 216847901987533 ◽  
Author(s):  
Luke Oh ◽  
Sojeong Yi ◽  
Da Zhang ◽  
Soo Hyeon Shin ◽  
Edward Bashaw
Keyword(s):  
Product Life Cycle ◽  
Skin Permeation ◽  
Systemic Exposure ◽  
Skin Permeability ◽  
Over The Counter ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Study Sites

For topically applied over-the-counter (OTC) products, the association of unwanted systemic exposure and adverse events may be difficult to ascertain without a recognition or determination of in vivo absorption. Evaluation of skin permeability using a validated in vitro permeation methodology can provide important information for both initial formulation selection and reformulation during the product life cycle. Additionally, a comparison of permeation rates between formulations using a validated methodology could reduce the number of nonclinical studies needed as part of reformulation. However, many in vitro permeation tests (IVPTs) have produced results with high variability and low reproducibility between study sites. It is unclear if this is due to a lack of a standardized protocol, or lack of control of multiple key experimental factors including skin source, preparation, receptor fluid, and study design. This review presents the authors perspective on the potential regulatory utility of IVPT and proposes steps to improve the accuracy and reproducibility of IVPT. The focus of this review is on topical dermatologic drugs with an initial emphasis on the OTC marketplace where reformulations are more common.

scholarly journals Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Skin Permeability ◽  
Puva Therapy ◽  
Ultraviolet A ◽  
3T3 Fibroblasts ◽  
Skin Delivery

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.

scholarly journals EFFECT OF MENTHOL ON THE TRANSDERMAL PERMEATION OF ACECLOFENAC FROM MICROEMULSION FORMULATION

2019 ◽  
pp. 117-122
Author(s):  
Abdul Baquee Ahmed ◽  
Gouranga Das
Keyword(s):  
Droplet Size ◽  
Skin Permeation ◽  
Peak Height ◽  
Skin Permeability ◽  
Permeability Barrier ◽  
Microemulsion Formulation ◽  
Transdermal Permeation ◽  
Ir Studies ◽  
Ft Ir

Objective: The aim of this investigation was to enhance the transdermal permeation of aceclofenac (ACF) from microemulsion formulation using menthol as a natural permeation enhancer. Methods: Microemulsion containing 2% w/v of ACF was prepared by a titration method with different concentration of oil, surfactant and co-surfactant. The prepared microemulsion was evaluated for droplet size, viscosity, pH and in vitro skin permeation studies. Menthol at 3-8% w/w was added to the selected microemulsion formulation and their effect on skin permeation was evaluated across rat epidermis using modified Keshary-Chien diffusion cell. The Fourier transform infrared spectroscopy (FT-IR) was performed to understand the regulation action of menthol in the skin permeability barrier. Results: The average droplet size of the microemulsion was found to be 89.4±2.12 to 175.2±3.10 nm. The transdermal flux of the microemulsion containing 8% w/w menthol showed 2.9 fold increases in transdermal flux of ACF compared with the formulation without menthol. Result of FT-IR studies showed decrease in peak height of the symmetric and asymmetric C-H stretching vibrations may be because of the extraction of the stratum corneum (SC) lipids and the alteration of the skin permeability barrier. Conclusion: This result suggests that menthol significantly enhanced the transdermal permeation of ACF and may be an effective natural penetration enhancer for transdermal delivery of the drug.

scholarly journals EFFECT OF HYDROPHILIC AND HYDROPHOBIC POLYMER MATRIX ON THE TRANSDERMAL DRUG DELIVERY OF ETHINYLESTRADIOL AND MEDROXYPROGESTERONE ACETATE

2019 ◽  
Vol 11 (1) ◽  
pp. 210
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Medroxyprogesterone Acetate ◽  
Ethyl Cellulose ◽  
Skin Permeation ◽  
Eudragit Rs ◽  
Hydrophobic Polymer ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Eudragit Rl

Objective: The aims of the present study were to develop different matrix patches with various ratios of hydrophilic and hydrophobic polymer combinations such as ethyl cellulose (EC) and polyvinylpyrrolidone (PVP) and eudragit RL 100 (ERL) and eudragit RS 100 (ERS) containing ethinylestradiol and medroxyprogesterone acetate and to perform physicochemical characterization and in vitro permeation studies through rat skin.Methods: Six formulations (F1 to F6) were developed by varying the concentration of both hydrophilic and hydrophobic polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro, skin permeation profiles of ethinylestradiol and medroxyprogesterone acetate from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell. The physicochemical compatibility of the drug and the polymers was studied by differential scanning calorimetry.Results: The results suggested no physicochemical incompatibility between the drug and the polymers. In vitro permeation studies were performed by using Franz diffusion cells, patches coded as F3 (ethyl cellulose: polyvinylpyrrolidone, 7.5:2.5) and F6 (eudragit RL 100 (ERL) and eudragit RS 100 (ERS), 8:2) can be chosen for further in vivo studies. The results followed Higuchi kinetics (r = 0.9953-0.9979), and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro skin permeation studies of 85.64% (for F3) and 88.62% (for F6) of ethinylestradiol and medroxyprogesterone acetate.Conclusion: The developed transdermal patches are stable, non-irritating and had increased efficacy of ethinylestradiol and medroxyprogesterone acetate and therefore had a good potential for antifertility treatment.

scholarly journals Detection of Raspberry Ketone after Percutaneous Absorption of Rhododendrol-Containing Cosmetics and Its Mechanism of Formation

Cosmetics ◽  
2021 ◽  
Vol 8 (4) ◽  
pp. 97
Author(s):  
Lihao Gu ◽  
Akio Fujisawa ◽  
Kazuhisa Maeda
Keyword(s):  
Liquid Chromatography ◽  
High Performance ◽  
Skin Permeation ◽  
Skin Permeability ◽  
Mechanism Of Formation ◽  
Raspberry Ketone ◽  
Heat Treated ◽  
Unknown Substance ◽  
In Vitro Skin Permeation

Here, we aimed to elucidate the mechanism of rhododendrol (RD)-induced leukoderma. We investigated the skin permeability of RD in an aqueous solution and in different cosmetic formulations (lotion and emulsion) in an in vitro skin permeation study. The samples were analyzed using high-performance liquid chromatography (HPLC), and an unknown substance appeared on the spectrum. For identification, we analyzed various possible substances, such as raspberry ketone (RK) and rhododendrol quinone, using HPLC and then compared the detected absorption spectra and further verified the matched components using liquid chromatography–mass spectrometry. The unknown substance was found to be RK. To clarify the mechanism of formation of RK, we conducted a 24-hour skin permeation test on heat-treated skin. By quantifying the RK in the samples using HPLC, we observed that an enzyme in the skin seemed to be the cause of RK generation and that the components of the emulsion formulation could also be a cause. To investigate the enzyme, we reacted alcohol dehydrogenase with RD and observed that it was one of the converting enzymes. As RK has been reported to be a substance that causes leukoderma, the intraepidermal metabolism of RD to RK may be one of the mechanisms of susceptibility to leukoderma.

scholarly journals Biorelevant In Vitro Skin Permeation Testing and In Vivo Pharmacokinetic Characterization of Lidocaine from a Nonaqueous Drug-in-Matrix Topical System

2021 ◽  
Vol 22 (6) ◽  
Author(s):  
Emileigh Greuber ◽  
Kip Vought ◽  
Kalpana Patel ◽  
Hiroaki Suzuki ◽  
Kazuhiro Usuda ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Skin Permeation ◽  
Mouse Skin ◽  
Pharmacokinetic Profile ◽  
Hplc Method ◽  
Skin Permeability ◽  
Open Label ◽  
Drug Load

AbstractRecently, lidocaine topical systems utilizing nonaqueous matrices have been developed and provide efficient lidocaine delivery through the skin, such that lower concentrations of drug provide equivalent or greater drug delivery than drug-in-matrix hydrogel lidocaine patches. This study characterizes drug delivery from a nonaqueous lidocaine topical system with increasing drug load both in vitro and in vivo. Topical systems formulated with either 1.8% or 5.4% lidocaine were applied to healthy volunteers’ backs (n = 15) for 12 h in a single-center, open-label, four-treatment, four-period crossover pharmacokinetic study. Subjects were dosed with either three 1.8% systems or one, two, or three 5.4% systems in each period. Blood was collected for up to 48 h, and plasma lidocaine levels were measured with a validated HPLC method. In parallel, human and mouse skin models characterized the in vitro skin permeation profile. The pharmacokinetic profile was linear between one, two, and three lidocaine 5.4% applications. Application of three lidocaine 1.8% systems (108 mg lidocaine) was bioequivalent to one lidocaine 5.4% system (108 mg lidocaine). Both topical systems remained well adhered to the skin and irritation was mild. The 5.4% system had approximately threefold higher skin permeability than the 1.8% system in the mouse and human skin models. The results indicate increasing the drug load by three times results in triple the drug delivery both in vivo and in vitro. The relationship between the in vitro permeation and in vivo absorption correlates and is nonlinear.

scholarly journals The Effect of Cream and Gel Vehicles on the Percutaneous Absorption and Skin Retention of a New Eugenol Derivative With Antioxidant Activity

2021 ◽  
Vol 12 ◽  
Author(s):  
Edyta Makuch ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Steam Distillation ◽  
Skin Permeation ◽  
Biologically Active ◽  
Skin Permeability ◽  
Skin Accumulation ◽  
Radical Reduction ◽  
Skin Retention

The effect of cream and gel vehicles containing clove water on skin permeability was compared for a new eugenol derivative (eugenyl dichloroacetate—EDChA) with antioxidant activity. In vitro permeation experiments were conducted in a Franz cell with porcine skin. The cumulative mass and skin accumulation of EDChA were investigated and compared. The antioxidative capacity of the studied vehicles was determined by using the diphenylpicrylhydrazyl (DPPH) free radical reduction method. The antioxidant activity (evaluated with DPPH, ABTS, and the Folin–Ciocalteu methods) of the fluid that penetrated through the pig skin and of the fluid obtained after the skin extraction, were also determined. For comparison, eugenol was also tested. The results of this work could contribute to the development of vehicles with antioxidant potential estimated after 24 h of conducting the experiment, which indicates long-term protection against reactive oxygen species (ROS) in the deeper layers of the skin. The waste water from the clove buds steam distillation -contains several valuable biologically active compounds, and its use is environmentally friendly. We observed that gel vehicles were the best enhancer of skin permeation for both eugenol and its derivative. In most cases, -similar cumulative masses of eugenol and its ester were found in the acceptor fluid. The accumulation of EDChA was higher for cream vehicles in relation to the parent eugenol when applied onto the skin. The greatest amounts of eugenol were accumulated in the skin when these compounds were used in gel vehicles.

scholarly journals Use of Curcuma longa in cosmetics: extraction of curcuminoid pigments, development of formulations, and in vitro skin permeation studies

2014 ◽  
Vol 50 (4) ◽  
pp. 885-893 ◽  
Author(s):  
Gisele Mara Silva Gonçalves ◽  
Gustavo Henrique da Silva ◽  
Pedro Paulo Barros ◽  
Silvana Mariana Srebernich ◽  
Cecilia Toyoko Cavalcanti Shiraishi ◽  
...  
Keyword(s):  
Curcuma Longa ◽  
Skin Permeation ◽  
Cell System ◽  
Skin Permeability ◽  
Topical Formulations ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Anti Inflammatory ◽  
The Stability

Curcuma longais a ginger family aromatic herb (Zingiberaceae) whose rhizomes contain curcuminoid pigments, including curcumin, a compound known for its anti-inflammatory effects. The objective of this study was to obtain curcuminoid-rich extracts, develop topical formulations thereof, and assess the stability and skin permeation of these formulations. Curcuma longa extracts were obtained and used to develop formulations. Skin permeation studies were conducted in a modified Franz diffusion cell system, and skin retention of curcuminoid pigments was quantified in pig ear membrane. Prepared urea-containing gel-cream formulations were unstable, whereas all others had satisfactory stability and pseudoplastic rheological behavior. The amount of curcuminoid pigments recovered from the receptor solution was negligible. The skin concentration of curcuminoid pigments retained was positive (>20 µg/g of skin, mostly in the stratum corneum), considering the low skin permeability of curcumin. We conclude that development of topical formulations containing curcumin or Curcuma longaextract is feasible, as long as adjuvants are added to improve preservation and durability. The formulations developed in this study enabled penetration of curcumin limited to the superficial layers of the skin and then possibly without a risk of systemic action, thus permitting local use as a topical anti-inflammatory.

scholarly journals The Effect of Alkyl Chain Number in Sucrose Surfactant on the Physical Properties of Quercetin-Loaded Deformable Nanoliposome and Its Effect on In Vitro Human Skin Penetration

Nanomaterials ◽  
2018 ◽  
Vol 8 (8) ◽  
pp. 622 ◽  
Author(s):  
In Ki Hong ◽  
Ji Hoon Ha ◽  
Sangkeun Han ◽  
Hakhee Kang ◽  
Soo Nam Park
Keyword(s):  
Human Skin ◽  
Alkyl Chain ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Skin Permeability ◽  
Non Invasive ◽  
Edge Activator

Non-invasive skin penetration of a drug is increased by an edge activator, which enhances the nanoliposome deformability. The objective of this study was to investigate the role of the alkyl chain number of sucrose surfactants as an edge activator in elastic nanoliposomes. In addition, the physicochemical properties of the elastic nanoliposomes were characterized and an in vitro human skin permeation study was performed. Elastic nanoliposomes that were composed of sucrose monostearate (MELQ), sucrose distearate (DELQ), and sucrose tristearte (TELQ) were prepared using a thin-film hydration method. Particle size and entrapment efficiency of elastic nanoliposomes increased proportionally with an increase in the amounts and the numbers of the stearate in sucrose surfactant. Deformability of elastic nanoliposomes was indicated as DELQ > MELQ > TELQ and the same pattern was revealed through the in vitro human skin permeability tests. These results suggest that the number of alkyl chains of sucrose surfactant as edge activator affects the physicochemical property, stability, and skin permeability in elastic nanoliposome. Our findings give a valuable platform for the development of elastic nanoliposomes as skin drug delivery systems.

scholarly journals Olive Oil/Pluronic Oleogels for Skin Delivery of Quercetin: In Vitro Characterization and Ex Vivo Skin Permeability

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1808
Author(s):  
Mohammed Elmowafy ◽  
Arafa Musa ◽  
Taghreed S. Alnusaire ◽  
Khaled Shalaby ◽  
Maged M. A. Fouda ◽  
...  
Keyword(s):  
Olive Oil ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Pluronic F127 ◽  
Skin Permeability ◽  
Scanning Calorimetry ◽  
Skin Delivery ◽  
In Vitro Characterization ◽  
Accelerated Stability

The main objective of this study was to prepare and characterize oleogel as potential carrier for quercetin skin delivery. The formulations were prepared by adding olive oil (5–30%) to Pluronic F127 hydrogel and were evaluated for particle size, zeta potential, viscosity in vitro quercetin release and stability, and were compared with that of Pluronic F127 hydrogel. The selected formulation was characterized for its interaction possibility, ex vivo skin permeation and skin histological changes and safety. The particle sizes ranged from 345.3 ± 5.3 nm to 401.5 ± 2.8 nm, and possessed negative charges. The viscosities of the formulations were found in the range of 6367–4823 cps with inverse proportionality to olive oil percentage while the higher percentages showed higher quercetin release. Percentages of 25% and 30% olive oil showed instability pattern under the conditions of accelerated stability studies. Differential scanning calorimetry verified the existence of quercetin in micellar aggregation and the network in the case of hydrogel and oleogel respectively. Ex vivo skin permeation showed an improved skin permeation of quercetin when 20% olive oil containing oleogel was used. Skin histology after 10 days of application showed stratum corneum disruption and good safety profile. Based on these findings, the proposed oleogel containing 20% olive oil denotes a potential carrier for topical delivery of quercetin.

Sign in / Sign up

Export Citation Format

Share Document