Effect of Ointment Bases on Topical and Transdermal Delivery of Salicylic Acid in Rats: Evaluation by Skin Microdialysis

Murakami, Teruo; Yoshioka, Makiko; Okamoto, Ichiro; Yumoto, Ryoko; Higashi, Yasuhiko; Okahara, Kayo; Yata, Noboru

doi:10.1111/j.2042-7158.1998.tb03305.x

Cited by 27 publications

(15 citation statements)

References 18 publications

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“…Murakami et al . () found a highly variable effect when examining effects of five ointment bases with salicylic acid on intact and tape‐stripped dorsal rat skin. They showed a 46.2‐fold increase for the water‐soluble ointment (polyethylene glycols), compared with only a 2‐fold increase for the poloid and hydrophilic poloid ointments vs no increase for the white petroleum ointment and rather a decrease for the absorptive (oil‐type emulsion containing water) ointment.…”

Section: Mechnical Damage: Tape Stripping Abrasionmentioning

confidence: 99%

Percutaneous absorption in diseased skin: an overview

Chiang¹,

Tudela²,

Maibach³

2012

J of Applied Toxicology

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The stratum corneum's (SC) functions include protection from external hazardous environments, prevention of water loss and regulation of body temperature. While intact skin absorption studies are abundant, studies on compromised skin permeability are less common, although products are often used to treat affected skin. We reviewed literature on percutaneous absorption through abnormal skin models. Tape stripping is used to disrupt water barrier function. Studies demonstrated that physicochemical properties influence the stripping effect: water-soluble drugs are more affected. Abrasion did not affect absorption as much. Freezing is commonly used to preserve skin. It does not seem to modify water absorption, but still increases the penetration of compounds. Comparatively, heating the skin consistently increased percutaneous absorption. Removing SC lipids may increase percutaneous absorption of drugs. Many organic solvents are employed to delipidize. Delipidization with chloroform-methanol increased hydrophilic compound permeability, but not lipophilic. Acetone pre-treatment enhanced hydrophilic compound penetration. More data is needed to determine influence on highly lipophilic compound penetration. Sodium lauryl sulfate (SLS) induces irritant dermatitis and is frequently used as a model. Studies revealed that SLS increases hydrophilic compound absorption, but not lipophilic. However, skin irritation with other chemicals increases lipophilic penetration as much as hydrophilic. Animal studies show that UV exposure increases percutaneous absorption whereas human studies do not. Human studies show increased penetration in psoriatic and atopic dermatitis skin. The data summarized here begin to characterize flux alteration associated with damaged skin. Understanding the degree of alteration requires interpretation of involved conditions and the enlarging of our database to a more complete physicochemical spectrum.

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Section: Mechnical Damage: Tape Stripping Abrasionmentioning

confidence: 99%

Percutaneous absorption in diseased skin: an overview

Chiang¹,

Tudela²,

Maibach³

2012

J of Applied Toxicology

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“…To overcome this disadvantages, some studies were carried out related to the transdermal usage of it. 1,3,[21][22][23][24][25][26][27][28][29][30] Walkow and McGinity 25 studied the effect of physicochemical properties on the in vitro diffusion of salicylic acid (SA) through cellulose, dimethyl polysiloxane membranes and pig skin into a receptor phase of aqueous glycol, water and buffer solutions; they concluded that the SA diffusion was decreased as the receptor phase pH was lowered. Venkatesh et al 27 studied the in vitro release kinetics of SA from hydrogel patch formulations; they have determined that the release of SA followed the matrix diffusion controlled mechanism and the storage of the packaged formulations under ambient conditions for 9 months caused no change in the extent of SA release.…”

Section: Introductionmentioning

confidence: 99%

In vitro release of salicylic acid through poly(vinyl alcohol‐g‐itaconic acid) membranes

Asman¹,

Şanlı²,

Tuncel³

2007

J of Applied Polymer Sci

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In this study, itaconic acid (IA) was grafted on poly(vinyl alcohol) (PVA) at two different grafting percentages, 7.0% (w/w) and 14.0% (w/w), and membranes were prepared from the grafted copolymer (PVA-g-IA). Performances of PVA and PVA-g-IA membranes for the transdermal release of salicylic acid (SA) at in vitro conditions were investigated by using 2.0 mg/mL SA solutions. Effect of the pH on the release of SA was studied by keeping pH of donor and acceptor solutions in a range of (2.1-7.4). Permeation studies were also carried on at different SA concentrations. Effect of temperature on the release of SA was investigated in the temperature range of (32-39) (61)8C. Results showed that presence of IA decreased the release of SA from the PVA membranes and 73% SA was released at the end of 48 h at (32 6 1)8C from the IA-1 membranes. pH affected the release of SA through the grafted membranes and studies showed that release of SA was high with donor solution pH of 2.1. When the pH of donor and receiver solutions were kept at the same pH value, the overall SA% in permeate increased. Increase in concentration of SA decreased the release of SA for the studied membranes. Release of SA from PVA-g-IA membranes was temperature sensitive and increase in temperature from (32 6 1)8C to (39 6 1)8C increased the release percentage of SA by 24% (w/w). The overall activation energy for the permeation of SA through IA-1 membrane was found to be 22.97 kJ/mol.

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“…Data are presented as mean ± SD (n = 3). 19.63 ± 1.23 19.54 ± 1.18 The recovery and delivery of ACV through the microdialysis probe was studied, in which the microdialysis probes were perfused at different flow rates. The drug gradient cross the probe membrane was 1.0 µg/mL.…”

Section: Pharmacokinetic Investigation and Bioequivalence Assessmentmentioning

confidence: 99%

“…In the last decades, dermal microdialysis (DMD) has been used as a means of continuous sampling to monitor cutaneous drug absorption [15][16][17][18][19][20][21][22][23][24][25] . In this method, an ultrathin, semipermeable probe is inserted in the dermis, and is perfused with a buffer to collect diffused drugs through a semipermeable membrane.…”

Section: Research Articlementioning

confidence: 99%

Topical bioequivalence of acyclovir creams using dermal microdialysis in pigs: a new model to evaluate bioequivalence for topical formulations

Hui-lin¹,

Wang

Xu³

et al. 2011

Drug Development and Industrial Pharmacy

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The aim was to evaluate the bioequivalence of topically applied Acyclovir (ACV) creams using dermal microdialysis (DMD) in a pig model. Three ACV creams (3%), ACV1, ACV2 and ACV3, were topically administrated on the dorsum of pigs, and the DMD sampling technique was used to continuously collect microdialysate. The concentration of ACV in microdialysate was measured by HPLC and the concentration-time profiles were used to calculate pharmacokinetic parameters. The results showed that 90% confidence interval (CI) of the ratio of AUC(0-4 h) of ACV2 and ACV3 was between 88.2 and 105.7%, which was within the acceptance range (80-125%). Ninety percent CI of the ratio of C(max) of ACV2 and ACV3 was between 87.4 and 124.4%, which was within the acceptance range (80-125%). These data indicate that ACV2 and ACV3 used in this study were bioequivalent. This study demonstrates that the pig model coupled with DMD sampling can potentially provide a cost-effective strategy to evaluate topical drug delivery and its associated pharmacokinetic studies.

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Effect of Ointment Bases on Topical and Transdermal Delivery of Salicylic Acid in Rats: Evaluation by Skin Microdialysis

Cited by 27 publications

References 18 publications

Percutaneous absorption in diseased skin: an overview

Percutaneous absorption in diseased skin: an overview

In vitro release of salicylic acid through poly(vinyl alcohol‐g‐itaconic acid) membranes

Topical bioequivalence of acyclovir creams using dermal microdialysis in pigs: a new model to evaluate bioequivalence for topical formulations

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