Methods to Evaluate Skin Penetration In Vitro

Zsikó, Stella; Csányi, Erzsébet; Kovács, Anita; Budai-Szűcs, Mária; Gácsi, Attila; Berkó, Szilvia

doi:10.3390/scipharm87030019

Cited by 101 publications

(71 citation statements)

References 110 publications

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“…Trans-Resveratrol (RSV), α-Cyclodextrin (α-CD), β-Cyclodextrin (β-CD), Glyceryl Stearate (35)(36)(37)(38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50), and Soy Lecithin were purchased from A.C.E.F. (Fiorenzuola D'Arda, Italy); Labrasol (PEG-8 Caprylic/Capric Glycerides), Gelucire 62/05, Labrafil M-1944, Labrafil M-2130, Isostearyl Isostearate, and Tefose 1500 were kindly supplied from Gattefossè (Saint-Priest, France); 1-Hexadecanol (EXA), R-(+)-Limonene (LIM), and Bovine Serum Albumin (BSA) were purchased from Sigma-Aldrich Chemie (Steinheim, Germany).…”

Section: Methodsmentioning

confidence: 99%

“…According to the definition of a cosmetic product, no drug or functional substance within the formulation must reach the systemic circulation; hence, the ability of RSV present in both solution and microspheres to cross the heat-separated porcine epidermis was tested by the Franz type cell assay [44]. Since the RSV has very low solubility in water of 0.05 mg/mL [45], several buffer solutions containing solubilizing agents were tested, to increase the RSV concentration gradient on the sides of the epidermis, as it represents the main driving force for the passive diffusion of drugs (Table 3).…”

Section: Evaluation Of Rsv Solubility In Aqueous Solutionmentioning

confidence: 99%

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Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

et al. 2020

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The development of efficacious means of delivering antioxidant polyphenols from natural sources for the treatment of skin diseases is of great interest for many cosmetic and pharmaceutical companies. Resveratrol (RSV) and Limonene (LIM) have been shown to possess good anti-inflammatory and antibacterial properties against Staphylococcus aureus infections responsible for many skin disorders, such as acne vulgaris. In this study, solid lipid microparticles are designed as composite vehicles capable of encapsulating a high amount of trans-RSV and enhancing its absorption through the stratum corneum. A microparticulate system based on mixture of PEGylate lipids, long-chain alcohols and LIM is able to entrap RSV in an amorphous state, increasing its half-life and avoiding inactivation due to isomerization phenomena, which represents the main drawback in topical formulations. Particles have been characterized in term of shape, size distribution and drug loading. Antimicrobial tests against S. aureus have highlighted that empty microspheres possess per se antimicrobial activity, which is enhanced by the presence of LIM, demonstrating that they can represent an interesting bactericide vehicle for RSV administration on the skin.

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Section: Methodsmentioning

confidence: 99%

Section: Evaluation Of Rsv Solubility In Aqueous Solutionmentioning

confidence: 99%

Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

et al. 2020

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“…In 2018, European Medicines Agency's draft guideline on quality and equivalence of topical products has recommended the use of synthetic membranes to better understand and characterize performance of a finished topical dosage form [34]. Moreover, synthetic membranes are inexpensive and easily resourced with superior data reproducibility [35,36]. Therefore, for our studies, Strat-M ® was used as a diffusion membrane.…”

Section: In-vitro Permeation Studiesmentioning

confidence: 99%

Evaluation of Formulation Parameters on Permeation of Ibuprofen from Topical Formulations Using Strat-M® Membrane

et al. 2020

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Topical drug delivery is an attractive alternative to conventional methods because of advantages such as non-invasive delivery, by-pass of first pass metabolism, and improved patient compliance. However, several factors such as skin, physicochemical properties of the drug, and vehicle characteristics influence the permeation. Within a formulation, critical factors such as concentration of drug, physical state of drug in the formulation, and organoleptic properties affect the flux across the skin. The aim of the study was to develop and investigate topical semisolid preparations (creams and gels) with ibuprofen as the model drug and investigate the effect of various formulation parameters on the in-vitro performance across the Strat-M® membrane using flow-through cells. In addition, the physical stability of the developed formulations was investigated by studying viscosity, pH, and appearance. All the formulations developed in the study had appealing appearance with smooth texture and no signs of separation. Viscosity and pH of the formulations were acceptable. Cumulative amount of drug permeated at the end of 24 h was highest for clear gel (3% w/w ibuprofen; F6: 739.6 ± 36.1 µg/cm2) followed by cream with high concentration of ibuprofen in suspended form (5% w/w; F3: 320.8 ± 17.53 µg/cm2), emulgel (3% w/w ibuprofen; F5: 178.5 ± 34.5 µg/cm2), and cream with solubilized ibuprofen (3% w/w; F2A: 163.2 ± 9.36 µg/cm2). Results from this study showed that permeation of ibuprofen was significantly influenced by formulation parameters such as concentration of ibuprofen (3% vs. 5% w/w), physical state of ibuprofen (solubilized vs. suspended), formulation type (cream vs. gel), mucoadhesive agents, and viscosity (high vs. low). Thus, findings from this study indicate that pharmaceutical formulation scientists should explore these critical factors during the early development of any new topical drug product in order to meet pre-determined quality target product profile.

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“…25 However, it encounters skin permeation disadvantages since it can only accept a limited type of drugs due to the effect of the stratum corneum layer, which can only stretch to a thickness of 40 μm. 80 Notable mechanisms adopted to increase skin permeation include electroporation, permeation enhancement, iontophoresis, microneedles, nanocarriers, and jet injectors. 25…”

Section: Liposomal Transdermal Drug Delivery Systemsmentioning

confidence: 99%

<p>Development, Characterization and Use of Liposomes as Amphipathic Transporters of Bioactive Compounds for Melanoma Treatment and Reduction of Skin Inflammation: A Review</p>

Castañeda-Reyes

Perea-Flores

Dávila-Ortíz

et al. 2020

IJN

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The skin is the largest organ in the human body, providing a barrier to the external environment. It is composed of three layers: epidermis, dermis and hypodermis. The most external epidermis is exposed to stress factors that may lead to skin conditions such as photo-aging and skin cancer. Some treatments for skin disease utilize the incorporation of drugs or bioactive compounds into nanocarriers known as liposomes. Liposomes are membranes whose sizes range from nano to micrometers and are composed mostly of phospholipids and cholesterol, forming similar structures to cell membranes. Thus, skin treatments with liposomes have lower toxicity in comparison to traditional treatment routes such as parenteral and oral. Furthermore, addition of edge activators to the liposomes decreases the rigidity of the bilayer structure making it deformable, thereby improving skin permeability. Liposomes are composed of an aqueous core and a lipidic bilayer, which confers their amphiphilic property. Thus, they can carry hydrophobic and hydrophilic compounds, even simultaneously. Current applications of these nanocarriers are mainly in the cosmetic and pharmaceutic industries. Nevertheless, new research has revealed promising results regarding the effectiveness of liposomes for transporting bioactive compounds through the skin. Liposomes have been well studied; however, additional research is needed on the efficacy of liposomes loaded with bioactive peptides for skin delivery. The objective of this review is to provide an up-to-date description of existing techniques for the development of liposomes and their use as transporters of bioactive compounds in skin conditions such as melanoma and skin inflammation. Furthermore, to gain an understanding of the behavior of liposomes during the process of skin delivery of bioactive compounds into skin cells.

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Methods to Evaluate Skin Penetration In Vitro

Cited by 101 publications

References 110 publications

Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

Evaluation of Formulation Parameters on Permeation of Ibuprofen from Topical Formulations Using Strat-M® Membrane

<p>Development, Characterization and Use of Liposomes as Amphipathic Transporters of Bioactive Compounds for Melanoma Treatment and Reduction of Skin Inflammation: A Review</p>

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