Development of a Novel Simple Gel Formulation Containing an Ion-Pair Complex of Diclofenac and Phenylephrine.

Abstract:

BACKGROUND AND AIM:Since the pharmacological effects of diclofenac (DF) are short-lived because of its short half-life, prolongation of the pharmacological effect in a topical formulation is needed for more appropriate clinical use. For the enhancement of dermal accumulation and prolongation of the pharmacological effect of drugs, the aim of this study was to develop a simple gel formulation containing an ion-pair complex of DF and phenylephrine (PHE), which induce constriction of the vascular smooth muscles. MATERIALS AND METHODS:The ion-pair complex was prepared by mixing sodium DF and an ethanolic solution of PHE. The formed complex was characterized by powder X-ray diffraction (PXRD) and Fourier-transform infrared (FT-IR) spectroscopy. The ion-pair complex for the gel formulation was prepared by mixing an equimolar concentration of 50% 1,3-butylene glycol and distilled aqueous solution of 2% xanthan gum, which was characterized by proton nuclear magnetic resonance (1H-NMR). Skin permeation and accumulation of DF and PHE were evaluated by in vitro and in vivo studies. RESULTS:From the results of PXRD and FT-IR, it was suggested that new crystalline peaks formed by the ion-pair complex and their complex interacted with the carboxyl group in DF and the amino group in PHE. In the gel formulation, the ion-pair complexes were detected by 1H-NMR. The ion-pair complex enhanced the accumulation of DF in the skin in the in vitro study. On the other hand, PHE accumulation in the dermis increased with the ion-pair complex, as exhibited by the in vivo study. CONCLUSION:A new gel formulation containing the ion-pair complex of DF and PHE was developed, which improved the accumulation of DF in skin.

journal_name

Skin Pharmacol Physiol

authors

Uchino T,Miyazaki Y,Ishikawa A,Kagawa Y

doi

10.1159/000501734

subject

Has Abstract

pub_date

2019-01-01 00:00:00

pages

318-327

issue

6

eissn

1660-5527

issn

1660-5535

pii

000501734

journal_volume

32

pub_type

杂志文章
  • Influence of bathing or washing on skin barrier function in newborns during the first four weeks of life.

    abstract:BACKGROUND AND OBJECTIVES:After birth, skin barrier function is in state of flux and at risk of dysfunction. In a prospective clinical study, we compared the effects of 2 standard cleansing procedures on skin barrier function in newborns. METHODS:Fifty-seven healthy full-term neonates aged < or = 48 h were randomly as...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000235552

    authors: Garcia Bartels N,Mleczko A,Schink T,Proquitté H,Wauer RR,Blume-Peytavi U

    更新日期:2009-01-01 00:00:00

  • Sirtuins in Skin and Skin Cancers.

    abstract::The sirtuins are a family of proteins that comprise class III of the histone deacetylases. These NAD+-dependent proteins have been found to be intricately involved in a variety of important and skin-relevant cellular functions and processes, including aging, UV damage response, oxidative stress, and wound repair. In a...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,评审

    doi:10.1159/000477417

    authors: Garcia-Peterson LM,Wilking-Busch MJ,Ndiaye MA,Philippe CGA,Setaluri V,Ahmad N

    更新日期:2017-01-01 00:00:00

  • The Influence of Reactive Oxygen Species and Glucocorticoids on Dry Skin in a Mouse Model of Arthritis.

    abstract:BACKGROUND:Dry skin induced by rheumatoid arthritis (RA) causes itching, which negatively influences a patient's quality of life. We previously reported that mast cells are related to dry skin in arthritic mice. However, the mechanism of mast cell activation is unclear. In this study, we examined the mechanism underlyi...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000488250

    authors: Goto K,Hiramoto K,Kawakita M,Yamaoka M,Ooi K

    更新日期:2018-01-01 00:00:00

  • The Effect of Glycation on Epidermal Lipid Content, Its Metabolism and Change in Barrier Function.

    abstract:BACKGROUND/AIMS:Advanced glycation end products, which are linked to both aging and hyperglycemia, cause marked functional and structural alterations in human skin. Though it is well known that the metabolism of glucose is closely associated with that of fatty acid (FA), sharing the same energy-yielding reaction pathwa...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000448121

    authors: Yokota M,Tokudome Y

    更新日期:2016-01-01 00:00:00

  • Lycopene and Melatonin: Antioxidant Compounds in Cosmetic Formulations.

    abstract:BACKGROUND:The use of antioxidants has become a common practice in the development of antiaging cosmetics. OBJECTIVE:The aim of this study was to evaluate the clinical efficacy of cosmetic formulations containing lycopene and melatonin antioxidants. METHOD:Thirty-six healthy women from 32 to 65 years were enrolled in...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000508673

    authors: Marchena AM,Franco L,Romero AM,Barriga C,Rodríguez AB

    更新日期:2020-01-01 00:00:00

  • Thermal behaviour of human stratum corneum. A differential scanning calorimetry study at high scanning rates.

    abstract:PURPOSE:To use high-speed differential scanning calorimetry (DSC) in the identification of transitions in human stratum corneum (SC). Several scanning rates (100 degrees C/min to 400 degrees C/min) are used. RESULTS:Eight transitions from 0 to 120 degrees C are detected in a significant number of samples. Most of thes...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000092593

    authors: Silva CL,Nunes SC,Eusébio ME,Pais AA,Sousa JJ

    更新日期:2006-01-01 00:00:00

  • The antimicrobial peptides psoriasin (S100A7) and koebnerisin (S100A15) suppress extracellular matrix production and proliferation of human fibroblasts.

    abstract:BACKGROUND/AIMS:Keloids result from aberrations in the normal wound healing cascade and can lead to pruritus, contractures and pain. The underlying mechanisms of excessive scarring are not yet understood, and most therapeutic strategies remain unsatisfactory. Psoriasin (S100A7) and koebnerisin (S100A15) are released by...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000363579

    authors: Gauglitz GG,Bureik D,Zwicker S,Ruzicka T,Wolf R

    更新日期:2015-01-01 00:00:00

  • Monitoring the distribution of surfactants in the stratum corneum by combined ATR-FTIR and tape-stripping experiments.

    abstract::Combined ATR-FTIR (attenuated total reflection-Fourier transform infrared) spectroscopy and tape-stripping experiments in vitro on porcine ear skin were used to investigate the spatial distribution of different surfactants in the stratum corneum (SC). To reveal a possible connection between the size of the formed mice...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000368444

    authors: Hoppel M,Holper E,Baurecht D,Valenta C

    更新日期:2015-01-01 00:00:00

  • Cutaneous carotenoids: the mirror of lifestyle?

    abstract::Carotenoids could serve as marker substances of the antioxidant status of the human skin. In the present study, an optical skin scanner was used to analyse the carotenoid concentration obtained from 4 volunteers over a period of 13 days. The measurements were taken daily at different time points. In addition, the volu...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000357222

    authors: Lademann J,Köcher W,Yu R,Meinke MC,Na Lee B,Jung S,Sterry W,Darvin ME

    更新日期:2014-01-01 00:00:00

  • Drug release and skin penetration from solid lipid nanoparticles and a base cream: a systematic approach from a comparison of three glucocorticoids.

    abstract::Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoest...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000324053

    authors: Schlupp P,Blaschke T,Kramer KD,Höltje HD,Mehnert W,Schäfer-Korting M

    更新日期:2011-01-01 00:00:00

  • Comparison of the Skin Penetration of 3 Metabolically Stable Chemicals Using Fresh and Frozen Human Skin.

    abstract:BACKGROUND:The Cosmetics Europe ADME Task Force is developing in vitro and in silico tools for predicting skin and systemic concentrations after topical application of cosmetic ingredients. There are conflicting reports as to whether the freezing process affects the penetration of chemicals; therefore, we evaluated whe...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000475472

    authors: Jacques-Jamin C,Duplan H,Rothe H,Vaillant O,Eilstein J,Grégoire S,Cubberley R,Lange D,Ellison C,Klaric M,Hewitt N,Schepky A

    更新日期:2017-01-01 00:00:00

  • In vivo assessment of Ectoin: a randomized, vehicle-controlled clinical trial.

    abstract::The aim of the study was to assess an Ectoin formulation with regard to the antiageing properties. The study was designed as a monocentric, randomized, double-blind application test, in order to ensure the compatibility and the efficacy of Ectoin in comparison to a vehicle emulsion. A total of 104 voluntary healthy fe...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000103204

    authors: Heinrich U,Garbe B,Tronnier H

    更新日期:2007-01-01 00:00:00

  • The Preventive Effect of Coffee Compounds on Dermatitis and Epidermal Pigmentation after Ultraviolet Irradiation in Mice.

    abstract:BACKGROUND:Ultraviolet (UV) irradiation is well known to promote inflammation and pigmentation of skin. UVB mainly affects dermatitis and pigmentation. Coffee contains a number of polyphenols, such as caffeic acid (CA) and chlorogenic acid (CGA) but their in vivo bioactivity for photobiology remains unclear. METHODS:C...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000455237

    authors: Yamate Y,Hiramoto K,Sato EF

    更新日期:2017-01-01 00:00:00

  • Ex vivo cutaneous absorption assessmentof a stabilized ascorbic acid formulation using a microdialysis system.

    abstract:BACKGROUND:Reactive oxygen species generated by ultraviolet light result in photocarcinogenic and photoaging changes in the skin. Antioxidants protect the skin from these insults. OBJECTIVE:The aim of this study was to determine the ex vivo ascorbic acid penetration and its degradation in the skin after its topical ap...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000081115

    authors: Leveque N,Muret P,Makki S,Mac-Mary S,Kantelip JP,Humbert P

    更新日期:2004-11-01 00:00:00

  • Methods for the evaluation of the protective efficacy of sunscreen products.

    abstract::The objective of the present investigation was to examine the utilization of optical and spectroscopic methods for the noninvasive characterization of Anthelios XL Fluide Extreme (SPF 50+), an exemplary sunscreen, concerning its homogeneity of distribution on the skin, its spectroscopic properties and its overall prot...

    journal_title:Skin pharmacology and physiology

    pub_type: 临床试验,杂志文章

    doi:10.1159/000343576

    authors: Vergou T,Patzelt A,Schanzer S,Meinke MC,Weigmann HJ,Thiede G,Sterry W,Lademann J,Darvin ME

    更新日期:2013-01-01 00:00:00

  • The combined effects of extracts containing carotenoids and vitamins E and C on growth and pigmentation of cultured human melanocytes.

    abstract::In the present study, we investigated the effects of tomato extract (TE) containing lycopene and palm fruit extract (PE) rich in carotenoids on the growth and pigmentation of melanocyte cultures of Caucasian origin. The extracts were tested at different concentrations and in combination with vitamins E and C. Melanocy...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000080217

    authors: Smit N,Vicanova J,Cramers P,Vrolijk H,Pavel S

    更新日期:2004-09-01 00:00:00

  • Brian Barry: innovative contributions to transdermal and topical drug delivery.

    abstract::Brian Barry published over 300 research articles across topics ranging from colloid science, vasoconstriction and the importance of thermodynamics in dermal drug delivery to exploring the structure and organisation of the stratum corneum barrier lipids and numerous strategies for improving topical and transdermal drug...

    journal_title:Skin pharmacology and physiology

    pub_type: 传,历史文章,杂志文章

    doi:10.1159/000351946

    authors: Williams AC

    更新日期:2013-01-01 00:00:00

  • Cutaneous estradiol permeation, penetration and metabolism in pig and man.

    abstract:AIM AND METHODS:Drug development in dermatotherapy and also development of transdermal therapeutic systems (TTS) demand high-predictive in vitro models to estimate drug levels in skin and systemic uptake. Here we compare three ready-to-use models, reconstructed human epidermis, split porcine skin and the perfused porci...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000081683

    authors: Mahmoud A,Haberland A,Dürrfeld M,Heydeck D,Wagner S,Schafer-Korting M

    更新日期:2005-01-01 00:00:00

  • How Confocal Is Confocal Raman Microspectroscopy on the Skin? Impact of Microscope Configuration and Sample Preparation on Penetration Depth Profiles.

    abstract:BACKGROUND/AIMS:The aim of the study was to elucidate the effect of sample preparation and microscope configuration on the results of confocal Raman microspectroscopic evaluation of the penetration of a pharmaceutical active into the skin (depth profiling). METHODS:Pig ear skin and a hydrophilic formulation containing...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000444806

    authors: Lunter DJ

    更新日期:2016-01-01 00:00:00

  • Influence of Buffers of Different pH and Composition on the Murine Skin Barrier, Epidermal Proliferation, Differentiation, and Inflammation.

    abstract::The pH of the skin is tightly regulated by endogenous buffering systems. We examined the influence of buffers of different pH and composition on skin barrier repair, pH, inflammation, and epidermal thickness/proliferation/differentiation. After tape-stripping in hairless mice buffers with pH 4-7 were applied in patch ...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000501976

    authors: Proksch E,Soeberdt M,Neumann C,Kilic A,Reich H,Abels C

    更新日期:2019-01-01 00:00:00

  • Skin irritation and sensitization: mechanisms and new approaches for risk assessment. 1. Skin irritation.

    abstract::Cutaneous irritation presents a major health problem with serious social and occupational impact. The interaction between an irritant and the human skin depends on multiple factors: the intrinsic properties and the nature of the irritant itself, and specific individual- and environment-related variables. The main path...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,评审

    doi:10.1159/000131077

    authors: Fluhr JW,Darlenski R,Angelova-Fischer I,Tsankov N,Basketter D

    更新日期:2008-01-01 00:00:00

  • Full-body skin mapping for six biophysical parameters: baseline values at 16 anatomical sites in 125 human subjects.

    abstract:BACKGROUND/AIM:The skin, as the outermost organ, protects against exogenous hazards (outside-in barrier) and prevents the loss of essential parts of the body (inside-out barrier). The epidermal barrier exerts several functions with specific morphological elements. Regional differences in skin functions are well known. ...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000330721

    authors: Kleesz P,Darlenski R,Fluhr JW

    更新日期:2012-01-01 00:00:00

  • Overcoming the stratum corneum: the modulation of skin penetration. A review.

    abstract::It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not ...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,评审

    doi:10.1159/000091978

    authors: Trommer H,Neubert RH

    更新日期:2006-01-01 00:00:00

  • Downmodulatory effects of the antihistaminic drug bepotastine on cytokine/chemokine production and CD54 expression in human keratinocytes.

    abstract::Bepotastine besilate is an antihistaminic drug of the second generation with superior clinical responses. In this study, we investigated whether bepotastine modulates the production of cytokines/chemokines and the expression of CD54 in human epidermal keratinocytes. The production of IL-1alpha, CXCL10, and CCL17 and t...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000183924

    authors: Kobayashi M,Kabashima K,Nakamura M,Tokura Y

    更新日期:2009-01-01 00:00:00

  • Metrics and clinical relevance of percutaneous penetration and lateral spreading.

    abstract:BACKGROUND:Percutaneous penetration of urea in vivo in man has been documented. If urea can penetrate the skin, it may also move laterally. Lateral spreading of topical substances leads to unpredictable penetration dynamics and increased skin surface area exposure. METHODS:The ability of urea, a low molecular-weight h...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000363148

    authors: Vieille-Petit A,Blickenstaff N,Coman G,Maibach H

    更新日期:2015-01-01 00:00:00

  • Molecular basis for the regenerative properties of a secretion of the mollusk Cryptomphalus aspersa.

    abstract::A screen for natural products bearing pharmacological properties has yielded a secretion of the mollusk Cryptomphalus aspersa (SCA), which possesses skin-regenerative properties. In this report, we outline some of the cellular and molecular effects underlying this observation. First, we found that SCA contained antiox...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000109084

    authors: Brieva A,Philips N,Tejedor R,Guerrero A,Pivel JP,Alonso-Lebrero JL,Gonzalez S

    更新日期:2008-01-01 00:00:00

  • Response analysis of stimulating efficacy of polihexanide in an in vitro wound model with respiratory ciliary epithelial cells.

    abstract::In animal wound models, accelerated wound closure has been shown by use of polihexanide applied in antimicrobially effective concentrations. Additionally, an increased ATP production of keratinocytes in vitro induced by polihexanide was demonstrated and interpreted as a stimulatory effect on cell proliferation. Based ...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000319602

    authors: Roth C,Beule AG,Kramer A,Hosemann W,Kohlmann T,Scharf C

    更新日期:2010-01-01 00:00:00

  • In search for new antipsoriatic agents: NAD topical composition.

    abstract::The aim of the study was to examine the effectiveness of the oxidized form of nicotinamide adenine dinucleotide (NAD(+)), adenosine precursor, in 37 patients suffering from psoriasis. As NAD(+) is known to be relatively unstable, the second goal was to establish the proper conditions for the satisfactory stability of ...

    journal_title:Skin pharmacology and physiology

    pub_type: 临床试验,杂志文章

    doi:10.1159/000096170

    authors: Wozniacka A,Szajerski P,Adamus J,Gebicki J,Sysa-Jedrzejowska A

    更新日期:2007-01-01 00:00:00

  • Sesquiterpene-Enriched Extract of Curcuma aeruginosa Roxb. Retards Axillary Hair Growth: A Randomised, Placebo-Controlled, Double-Blind Study.

    abstract:BACKGROUND:Sesquiterpenes in Curcuma aeruginosa Roxb. inhibit steroid 5α-reductase and dihydrotestosterone production, and reverse androgenic alopecia. This study sought to show that a high sesquiterpene C. aeruginosa extract (CA-ext) retards axillary hair growth in women. METHODS:Thirty women (age 20-52 years) were r...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000486136

    authors: Srivilai J,Nontakhot K,Nutuan T,Waranuch N,Khorana N,Wisuthiprot W,Scholfield CN,Champachaisri K,Ingkaninan K

    更新日期:2018-01-01 00:00:00

  • The antioxidant role of paraoxonase 1 and vitamin E in three autoimmune diseases.

    abstract:PURPOSE OF THE STUDY:To investigate the role of paraoxonase 1 (PON1) and vitamin E in the pathogenesis of some autoimmune diseases, and to correlate their levels with the disease activity. PROCEDURES:This randomized case control study was performed on 60 subjects: 45 patients [suffering from psoriasis, vitiligo and al...

    journal_title:Skin pharmacology and physiology

    pub_type: 杂志文章

    doi:10.1159/000342124

    authors: Ramadan R,Tawdy A,Abdel Hay R,Rashed L,Tawfik D

    更新日期:2013-01-01 00:00:00