Role of n-methyl Pyrrolidone in the Enhancement of Aqueous Phase Transdermal Transport

Lee, Philip J.; Langer, Robert; Shastri, V. Prasad

doi:10.1002/jps.20291

Cited by 61 publications

(35 citation statements)

References 23 publications

(18 reference statements)

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“…It was found that the cumulative permeation amount ranged from 795.0Ϯ3.89 to 891.8Ϯ2.86 mg/ cm 2 , Js ranged from 71.14Ϯ3.54 to 85.39Ϯ2.90 mg/cm 2 /h and lag time ranged from 0.11Ϯ0.02 to 0.25Ϯ0.01 h demonstrated that the permeation parameters of granisetron hydrochloride nanoemulsion were markedly affected by the content of NMP in the nanoemulsion system. For granisetron nanoemulsion containing NMP, there was a significant difference in lag time, cumulative amount and the skin permeation rate in comparison with the control group (nanoemulsion without NMP) (pϽ0.025), while no markedly change in the skin permeation parameters between nanoemulsion contain- These results were consistent with previous study reported that, 24,29,30) the permeation effect of nanoemulsion containing hydrophobic or hydrophilic drugs was markedly enhanced in the existence of NMP in the nanoemulsion system, in comparison with control group (without NMP). In other words, these results indicated that NMP was a more effective transdermal enhancer.…”

Section: Effect Of the Content Of Nmp On Skin Permeationsupporting

confidence: 90%

Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

Zheng¹,

Zhao

Wei

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Section: Effect Of the Content Of Nmp On Skin Permeationsupporting

confidence: 90%

Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

Zheng¹,

Zhao

Wei

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Whereas, the fourth endotherm (T 4 ) produced a very sharp and prominent peak at 114 C which is attributed to stratum corneum proteins (Yamane et al 1995;Vaddi et al 2002b;Narishetty and Panchagnula 2004a). The first endotherm (having the lowest enthalpy) is attributed to sebaceous secretions (Lee et al 2005) or surface contamination and to minor structural rearrangement of lipid bilayer and is some time completely removed by lipid extracting solvents (Yamane et al 1995). The second and the third endotherms T 2 and T 3 appear due to the melting of stratum corneum lipids and the fourth endotherm T 4 has been assigned to intracellular keratin denaturation.…”

Section: Discussionmentioning

confidence: 99%

The application of anethole, menthone, and eugenol in transdermal penetration of valsartan: Enhancement and mechanistic investigation

Ahad

Aqil

Ali

2015

Pharmaceutical Biology

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Context:The main barrier for transdermal delivery is the obstacle property of the stratum corneum. Many types of chemical penetration enhancers have been used to breach the skin barrier; among the penetration enhancers, terpenes are found as the most highly advanced, safe, and proven category. Objective: In the present investigation, the terpenes anethole, menthone, and eugenol were used to enhance the permeation of valsartan through rat skin in vitro and their enhancement mechanism was investigated. Materials and methods: Skin permeation studies of valsartan across rat skin in the absence and the presence of terpenes at 1% w/v, 3% w/v, and 5% w/v in vehicle were carried out using the transdermal diffusion cell sampling system across rat skin and samples were withdrawn from the receptor compartment at 1, 2, 3, 4, 6, 8, 10, 12, and 24 h and analysed for drug content by the HPLC method. The mechanism of skin permeation enhancement of valsartan by terpenes treatment was evaluated by Fourier transform infrared spectroscopy (FTIR) analysis and differential scanning calorimetry (DSC). Results: All the investigated terpenes provided a significant (p50.01) enhancement in the valsartan flux at a concentration of 1%, and less so at 3% and 5%. The effectiveness of terpenes at 1% concentration was in the following order: anethole4menthone4eugenol with 4.4-, 4.0-, and 3.0-fold enhancement ratio over control, respectively. DSC study showed that the treatment of stratum corneum with anethole shifted endotherm down to lower melting point while FTIR studies revealed that anethole produced maximum decrease in peak height and area than other two terpenes. Conclusion: The investigated terpenes can be successfully used as potential enhancers for the enhancement of skin permeation of lipophilic drug. ARTICLE HISTORY

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“…It has been reported to increase the solubility and permeability of several drugs (1)(2)(3)(4). It has low toxicity both orally and parenterally (5).…”

Section: Introductionmentioning

confidence: 99%

Solubility Improvement of Drugs using N-Methyl Pyrrolidone

Narazaki²,

et al. 2008

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Abstract. The solubilization efficiency of N-methyl pyrrolidone (NMP) has been determined and compared to that of ethanol and propylene glycol for 13 poorly soluble drugs. NMP is found to be a more efficient solubilizer for all the drugs studied. The solubility enhancement as high as about 800-fold is obtained in 20% v/v NMP solution as compared to water. The mechanism of drug solubilization by NMP has also been investigated. It is proposed that NMP enhances drug solubility by simultaneously acting as a cosolvent and a complexing agent. A mathematical model is used to estimate the drug solubility in NMP-water mixture, according to which the total solubility enhancement is a sum of the two effects. This model describes the experimental data well and is more accurate than other models. A large and uniform reduction in the surface tension of water as a function of NMP concentration demonstrates its cosolvent effect. The complexation is supported by the fact that it's strength is affected by the temperature and the polarity of the medium. A strong correlation exists between log K ow of the drugs and the cosolvency coefficients. The correlation between log K ow and the complexation coefficients is weak suggesting that factors such as molecular shape and aromaticity of the drug molecule are significant in determining the complexation strength. This has been confirmed by the absence of a significant complexation between NMP and linear drug-like solutes.

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Role of n-methyl Pyrrolidone in the Enhancement of Aqueous Phase Transdermal Transport

Cited by 61 publications

References 23 publications

Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

The application of anethole, menthone, and eugenol in transdermal penetration of valsartan: Enhancement and mechanistic investigation

Solubility Improvement of Drugs using N-Methyl Pyrrolidone

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