Lipid-protein-partitioning (LPP) theory of skin enhancer activity: finite dose technique

Goodman, Michael Wayne; Barry, Brian W.

doi:10.1016/0378-5173(89)90260-3

Cited by 91 publications

(43 citation statements)

References 16 publications

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“…Isopropyl myristate affects the lipids of the SC and the partition coefficient between the SC and vehicle of both drug and solvent (Lane et al, 2012). It was demonstrated that the use of cosolvent in combination with a potential penetration enhancer may offer synergistic enhancement (Arellano et al, 1998;Goodman & Barry, 1989).…”

Section: Discussionmentioning

confidence: 99%

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

et al. 2014

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Over the years, research has focused on strategies to increase benefit/risk ratio of corticoids. However, vehicles intended for topical glucocorticoids delivery with an improved benefit/risk ratio are still on demand. The aim of this work was the in vitro and in vivo characterization of cold processed oil-in-water (o/w) emulsions intended for mometasone furoate (MF) delivery to induce drug targeting to upper skin strata, decreasing adverse effects. Two o/w emulsions, containing 0.1% of MF, were developed differing in the glycol used (2-methyl-2,4-pentanediol -PT and ethoxydiglycol -TC emulsions). In vitro permeation studies revealed that these emulsions are suitable vehicles for the delivery of MF containing ingredients which are responsible for a drastically increased on the permeability coefficients of MF from a theoretical value of 1.18 Â 10 À4 cm/h to 5.20 Â 10 À4 AE 2.05 Â 10 À4 cm/h and 6.30 Â 10 À4 AE 2.94 Â 10 À4 cm/h, for PT and TC, respectively. The tape stripping results showed that the amount of drug that reached the viable skin layers was very low (1.99 %) and the amount that remained in the stratum corneum (SC) was 10.61%. The in vivo studies showed that the developed formulations decreased the edema and erythema in mice skin in more that 90%, assuring, at least, the same anti-inflammatory effect compared with the commercial cream. PT placebo demonstrated to contribute to restore the skin barrier by increasing the amount of lipids within the human skin.

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Section: Discussionmentioning

confidence: 99%

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

et al. 2014

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“…A large number of fatty acids and their esters have been used as permeation enhancers. Oleic acid has been shown to be effective as a permeation enhancer for many drugs, for example increasing the fl ux of salicylic acid 28-fold and 5-fluorouracil flux 56-fold, through human skin membranes in-vitro (11,12). It has also been used for ketoprofen (13), fl urbiprofen (14), 5-FU, estradiol (12), zalcitabine, didanosine, zidovudine (15), etc.…”

Section: Introductionmentioning

confidence: 99%

Formulation, optimization, and evaluation of a transdermal patch of heparin sodium

Patel

Gaiakwad

Patel

2014

DD^|^T

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“…A large number of fatty acids and their esters have been used as permeation enhancers. Oleic acid has been shown to be effective as a permeation enhancer for many drugs, for example increasing the flux of salicylic acid 28-fold and 5-fluorouracil flux 56-fold, through human skin membranes in-vitro [13,14]. It has also been used for ketoprofen [15], flurbiprofen [16], 5-FU, estradiol [14], zalcitabine, didanosine, zidovudine [17], etc.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of transdermal patch of aceclofenac.

Patel¹,

Patel²,

Baria³

2009

Int. J. Drug Del.

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Abstract:The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r 2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin.

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Lipid-protein-partitioning (LPP) theory of skin enhancer activity: finite dose technique

Cited by 91 publications

References 16 publications

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

Mometasone furoate-loaded cold processed oil-in-water emulsions:in vitroandin vivostudies

Formulation, optimization, and evaluation of a transdermal patch of heparin sodium

Formulation and evaluation of transdermal patch of aceclofenac.

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