scholarly journals In Vitro Skin Retention of Crisaborole after Topical Application

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 491
Author(s):  
Adriana Fantini ◽  
Anna Demurtas ◽  
Sara Nicoli ◽  
Cristina Padula ◽  
Silvia Pescina ◽  
...  
Keyword(s):  
Stratum Corneum ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Skin Layer ◽  
Hair Follicles ◽  
Relative Distribution ◽  
Phosphodiesterase 4 ◽  
Receptor Compartment ◽  
Drug Partitioning

Crisaborole, a nonsteroidal phosphodiesterase 4 inhibitor, represents the first nonsteroidal medication approved for the treatment of atopic dermatitis in over a decade. In this work, crisaborole skin permeation and retention was studied in vitro from a 2% ointment using porcine skin as barrier. Crisaborole was also characterized in terms of thermal behavior, solubility, and logP. Control experiments were performed also on tape stripped skin to clarify the role of stratum corneum in drug partitioning and permeation across the skin. The results obtained indicate that crisaborole accumulates into the skin in considerable amounts after application of a topical lipophilic ointment. Crisaborole shows more affinity for the dermis compared to the epidermis despite its relatively high value of partition coefficient; stratum corneum analysis revealed a low affinity of the drug for this skin layer. Skin penetration across hair follicles or sebaceous glands can be a reason for the high dermis retention and is worth further investigation. The comparison with data obtained from a solution in acetonitrile suggests that the formulation plays a certain role in determining the relative distribution of crisaborole in the skin layers and in the receptor compartment.

scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

scholarly journals In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

2012 ◽  
Vol 48 (4) ◽  
pp. 811-817 ◽  
Author(s):  
Luís Antônio Dantas Silva ◽  
Stephânia Fleury Taveira ◽  
Eliana Martins Lima ◽  
Ricardo Neves Marreto
Keyword(s):  
Stratum Corneum ◽  
Topical Therapy ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Drug Accumulation ◽  
Uniform Size ◽  
Liquid Chromatographic Method ◽  
Systemic Side Effects ◽  
Liquid Chromatographic

Clobetasol propionate (CP) is a potent topical corticosteroid that causes several cutaneous and systemic side effects. In the present work, CP was encapsulated in nanostructured lipid carriers (NLCs) to increase drug retention in the outer skin layers and improve the safety of topical therapy. NLCs were prepared using a microemulsion technique with a mixture of lecithin, taurodeoxycholate, stearic acid, and oleic acid. In vitro penetration studies were performed in a modified Franz-type diffusion cell, and porcine ears were used as a model of human skin. A simple and sensitive liquid chromatographic method was developed and validated for clobetasol determination in different skin layers. NLCs presented uniform size distribution, high zeta potentialand entrapment efficiency values (> 98%). The analytical procedure was validated according to FDA guidelines. Clobetasol recoveries from skin samples were higher than 85%, with no interference of skin components and NLC ingredients. In experiments, after 6 h, a higher drug accumulation in the stratum corneum arising from NLCs compared to aqueous CP solution was observed. Thus, the NLCs demonstrated high potential for targeting CP to the skin and ensuring drug accumulation in the stratum corneum.

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 Enhancement of the Antioxidant and Skin Permeation Properties of Eugenol by the Esterification of Eugenol to New Derivatives

2020 ◽  
Author(s):  
EDYTA MAKUCH ◽  
Anna Nowak ◽  
Andrzej Günther ◽  
Robert Pełech ◽  
Łukasz Kucharski ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Skin Permeation ◽  
Radical Scavenging ◽  
Skin Penetration ◽  
Dichloroacetic Acid ◽  
Pig Skin ◽  
High Level

Abstract The aim of the study was to determine the antioxidant activity and assess the lipophilicity and skin penetration of eugenyl chloroacetate (EChA), eugenyl dichloroacetate (EDChA), and eugenyl trichloroacetate (ETChA). Identification of the obtained products was based on gas chromatography (GC), infrared spectroscopy (FTIR/ATR), gas chromatography coupled with mass spectrometry (GC-MS), and the analysis of 13C-NMR and 1H-NMR spectra. The antioxidative capacity of the derivatives obtained was determined by the DPPH free radical reduction method, while the octanol/water partition coefficient (shake-flask method) was tested to determine the lipophilicity of these compounds. In the next stage of testing EDChA and ETChA–(compounds characterized by the highest degree of free radical scavenging), the penetration of DPPH through pig skin and its accumulation in the skin were evaluated. For comparison, penetration studies of eugenol alone as well as dichloroacetic acid (DChAA) and trichloroacetic acid (TChAA) were also carried out. The antioxidant activity (DPPH, ABTS, and Folin–Ciocalteu methods) of the fluid that penetrated through pig skin was also evaluated. The in vitro pig skin penetration study showed that eugenol derivatives are particularly relevant for topical application. The obtained derivatives were characterized by a high level of antioxidant activity estimated after 24 hours of conducting the experiment, which indicates long-term protection against reactive oxygen species (ROS) in the deeper layers of the skin.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

Effect of Various Nonionic Surfactants Incorporated in Liposomes on Dermal Delivery of Hydrophilic Compound

2014 ◽  
Vol 1060 ◽  
pp. 12-16
Author(s):  
Worranan Rangsimawong ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Nonionic Surfactants ◽  
Skin Permeation ◽  
Physicochemical Characteristic ◽  
Skin Penetration ◽  
Tween 20 ◽  
Negative Surface ◽  
Negative Surface Charge ◽  
Dermal Delivery ◽  
Hydrophilic Compound

Various surfactants-containing vesicles have been widely used as a carrier in drug delivery to enhance skin penetration of encapsulated therapeutic agents. The purpose of this study was to investigate the effect of nonionic surfactants-containing liposome vesicles on the penetration of hydrophilic compounds through the porcine skin. Ultradeformable liposomes composed of phosphatidylcholine (PC), cholesterol (Chol) and various surfactants e.g. Tween 20, Labrasol and Gelucire 44/14) were prepared as NaFI carrier. The physicochemical characteristic of liposomes and in vitro skin penetration were investigated. The particle size of surfactant-containing liposome vesicles showed smaller particle sizes (36 to 54 nm) than conventional liposome (CLs) and had negative surface charge. The EE% and LE% order of surfactants incorporated in liposome formulations were: Labrasol liposomes (LALs) > Gelucire 44/14 liposomes (GELs) > Tween20 liposomes (TWLs) > CLs. The flux of NaFI from ultradeformable liposomes was significantly higher than from CLs. Among various liposomes, Labrasol containing ultradeformable liposomes showed the highest skin permeation in 24 h, and their flux was significantly higher (p < 0.05) than the flux of CLs. The result suggests that the surfactant-containing liposomes were small and deformable vesicles due to incorporating of an edge activators. In addition, surfactants could act as a penetration enhancer to promote dermal delivery of NaFI.

Aqueous-Based Nanoemulsion Containing (-)-α-Bisabolol for Topical Treatment of Skin burns

2021 ◽  
Vol 01 ◽  
Author(s):  
Edson A. T. Almeida ◽  
Ricardo Ferreira-Nunes ◽  
Beatriz R. L. Aguiar ◽  
Paula E. D. dos Reis ◽  
Tais Gratieri ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Topical Treatment ◽  
Ternary Phase Diagram ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Hot Water ◽  
Intact Skin ◽  
Hot Plate ◽  
Promising Alternative

Background: α-Bisabolol (BIS) is a sesquiterpene extracted from chamomile flowers, which has been used to topically treat burnt skin has been reported. High lipophilicity of BIS, however, is a problem for both skin application and washing. Objective: The present study aimed to prepare and characterize a stable and safe aqueous-based nanoemulsion to incorporate BIS and favor skin penetration focusing on skin burns' topical treatment. Method: Oil-in-water nanoemulsions were obtained from a pseudo-ternary phase diagram. The selected nanoemulsion was characterized (droplet size, PDI, and zeta potential), and the stability was assessed for 60 days at 6ºC and room temperature. The irritability of the formulation was determined by HET-CAM. Skin permeation studies were carried out in vitro intact skin, hot water burn skin, and hot plate burn skin. Results: The nanoemulsion incorporated 1% (w/w) BIS, presented droplets' size of 14.0±0.8 nm (PDI= 0.13±0.02), the zeta potential of +7.5±1.9 mV, and was physically stable over 60 days. The HET-CAM did not show any irritability process provided by the nanoformulation. In the skin permeation experiments, when compared to an oily control solution of BIS, nanoemulsion increased 3.7-fold penetration of the drug in intact skin, likely because the nanoformulation acted as an absorption drug enhancer. On a hot water burn skin model, the increase in drug penetration was 1.7-fold, and in the hot plate burn skin, it was 2.3-fold. Conclusion: The nanoemulsion seems to be a promising alternative for skin burns' topical treatment using this natural active substance.

scholarly journals Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

RSC Advances ◽  
2018 ◽  
Vol 8 (48) ◽  
pp. 27464-27469 ◽  
Author(s):  
Mónika Bakonyi ◽  
Attila Gácsi ◽  
Szilvia Berkó ◽  
Anita Kovács ◽  
Erzsébet Csányi
Keyword(s):  
Stratum Corneum ◽  
Skin Penetration ◽  
Penetration Enhancer ◽  
Stratum Corneum Lipid ◽  
Stratum Corneum Lipid Liposomes ◽  
Lipid Liposomes

The aim of this work was to investigate the applicability of stratum corneum lipid liposomes as in vitro skin models for studying skin penetration enhancer effect of Kolliphor RH40 and Transcutol.

scholarly journals The Influence of Formulation and Excipients on Propranolol Skin Permeation and Retention

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Cristina Padula ◽  
Sara Nicoli ◽  
Silvia Pescina ◽  
Patrizia Santi
Keyword(s):  
Skin Permeation ◽  
Skin Penetration ◽  
Infantile Hemangioma ◽  
Skin Surface ◽  
Time Frame ◽  
Systemic Absorption ◽  
Therapeutic Drug ◽  
Topical Formulations ◽  
Skin Retention

The objective of this work was to study in vitro propranolol permeation and skin retention after topical application of different semisolid vehicles, with the final aim of developing new topical formulations intended for the treatment of infantile hemangioma, able to produce therapeutic drug levels in the skin, avoiding systemic absorption. Propranolol ointments, creams, and gels were prepared and tested on pig skin, an accepted model of human skin. From the results obtained in the present work it is clear that the permeation of propranolol across the skin is a poor predictor of its skin retention, at least in the time-frame considered. With an application time of 4 h, reasonably close to the permanence time of a semisolid formulation on the skin surface, the best performance (high retention and low skin penetration) was obtained with lipophilic formulations, in particular with a lipophilic cream containing olive oil. Hydrophilic formulations, such as gels, are characterized by a significant permeation across the skin, probably leading to systemic side effects, accompanied by a limited skin retention. Overall, the results obtained in the present work pose the basis for the development of new topical formulations, containing propranolol, with better performance and reduced systemic absorption.

scholarly journals Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

2015 ◽  
Vol 51 (1) ◽  
pp. 85-90 ◽  
Author(s):  
Edileia Bagatin ◽  
Tais Aleriana Lucon Wagemaker ◽  
Nelson dos Reis Aguiar Júnior ◽  
Mirela Donato Gianeti ◽  
Erika Maria Berardo Gonçalves ◽  
...  
Keyword(s):  
High Performance ◽  
Standard Treatment ◽  
Skin Penetration ◽  
Aqueous Methanol ◽  
In Vitro Permeation ◽  
Receptor Compartment ◽  
Chemical Peeling ◽  
Deep Layers ◽  
Franz Diffusion Cells

Tretinoin is used in the management of acne and it is part of a gold standard treatment for photoaging. It has also been reported as an agent for superficial chemical peeling in highly concentrated formulations with few considerations about skin penetration. The aim of this study was to evaluate the influence of drug concentration and vehicles currently used on skin penetration of tretinoin. In vitro permeation tests were carried out using Franz diffusion cells fitted with porcine ear skin and 10% aqueous methanol in the receptor compartment. Formulations studied, cream or hydroalcoholic dispersion, containing 0.25%, 1% and 5% of tretinoin were placed in the donor compartment for six hours. Tretinoin concentration in skin layers was measured by high performance liquid chromatography. The largest amount of tretinoin from both vehicles was detected in stratum corneum with significant differences among the three concentrations. The hydroalcoholic dispersion was the best vehicle. Significant amounts of tretinoin were found even in deep layers of epidermis. The formulation with 0.25% tretinoin showed better results when considered the amount of tretinoin on skin in terms of percentage. Finally, skin penetration of tretinoin was influenced by vehicle and concentration of this drug used in formulation.

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