Effects of vehicles and enhancers on transdermal delivery of clebopride

Rhee, Yun-Seok; Huh, Jai-Yong; Park, Chun‐Woong; Nam, Tae-Young; Yoon, Koog-Ryul; Chi, Sang-Cheol; Park, Eun-Seok

doi:10.1007/bf02980252

Cited by 27 publications

(13 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The presentation of enhancers, in equilibrium with HEM, at their highest thermodynamic activity resembles a number of topical preparations composed of drugs, volatile solvents, and chemical enhancers [3–7]. These topical preparations include gels, topical aerosols, and spray systems that contain volatile solvent(s) such as ethanol and/or water which evaporates upon application leaving the active drug and chemical enhancer on the skin surface.…”

Section: Introductionmentioning

confidence: 99%

Effects of solvent deposited enhancers on transdermal permeation and their relationship with Emax

Ibrahim

2009

Journal of Controlled Release

View full text Add to dashboard Cite

Many topical pharmaceuticals such as aerosols, topical sprays, and hydro-alcoholic and polymer based gels contain chemical enhancers. The objectives of the present study were to (a) determine the enhancement effects induced by enhancers deposited from a volatile solvent on human epidermal membrane (HEM) upon transdermal permeation enhancement, (b) compare these enhancement factors with Emax, and (c) examine the relationship between enhancer-induced permeation enhancement and stratum corneum equilibrium uptake enhancement. In this study, HEM was treated with enhancer/ethanol (enhancer dissolved in ethanol). After the evaporation of ethanol, passive transport experiments were conducted using corticosterone (CS) as the model permeant. The uptake of another model corticosteroid, estradiol (E2β), into the intercellular lipid domain of stratum corneum after enhancer/ethanol treatment was also determined. The results show a correlation between Emax and the enhancement effect of most enhancers when the enhancers were deposited on the skin using the volatile solvent ethanol. The data suggest that the CS transport rate limiting domain was likely the same as the intercellular lipid domain probed by E2β uptake. The correlation between steady-state permeation enhancement and uptake enhancement into the intercellular lipid domain suggests that the permeation enhancement mechanism is primarily due to enhancement of permeant partitioning into the transport rate limiting domain.

show abstract

Section: Introductionmentioning

confidence: 99%

Effects of solvent deposited enhancers on transdermal permeation and their relationship with Emax

Ibrahim

2009

Journal of Controlled Release

View full text Add to dashboard Cite

show abstract

“…However, it increased in the latter stage after in situ film formation. Ethanol has been reported as the effective enhancer with many other transdermal formulations, especially in skin or cell experiments [39][40][41] . It could change the mobility of the components in cell membranes to increase cell permeability for transdermal enhancer.…”

Section: Entrapment and In Vitro Release Of Nicotine From Film Forminmentioning

confidence: 99%

Transdermal nicotine mixed natural rubber-hydroxypropylmethylcellulose film forming systems for smoking cessation:in vitroevaluations

Pichayakorn

Suksaeree

Boonme

et al. 2014

Pharmaceutical Development and Technology

View full text Add to dashboard Cite

Novel film forming polymeric dispersions for transdermal nicotine delivery were prepared from deproteinized natural rubber latex (DNRL) blended with hydroxypropylmethylcellulose (HPMC) and dibutyl phthalate (DBP) or glycerin (GLY) as plasticizer. The preliminary molecular compatibility of ingredients was observed by Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry characterizations. All film forming polymeric dispersions were elegant in appearance and smooth in texture without agglomeration. Their pH was 7-8. In addition, their viscosity and spreadability showed good characteristics depended on HPMC and plasticizers blended. The transparent in situ dry films with good strength and elasticity were also confirmed by peeling-off. The nicotine release from them revealed an initial fast release that was similar to the release from a concentrated nicotine solution, and followed by slow release pattern from the in situ films. GLY blended formulation produced a higher amount of nicotine permeation through the in vitro pig skin than DBP blends. Ethanol mixing also enhanced nicotine permeation, but it affected the integrity of in situ films. The nicotine release and skin permeation kinetics were by a diffusion mechanism that was confirmed by the Higuchi's model. These formulations were safe without producing any severe skin irritation. However, for the stability they needed to be stored at 4 °C in tightly sealed containers.

show abstract

“…NMP is a common polar aprotic solvent miscible with most of the common solvents, including water and alcohols. Its effect on the enhancement of penetration of a number of drugs was investigated; it is also often used as a cosolvent with other solvents or enhancers …”

Section: Azone‐like Enhancersmentioning

confidence: 99%

“…Its effect on the enhancement of penetration of a number of drugs was investigated; it is also often used as a cosolvent with other solvents or enhancers. [181][182][183][184] Yoneto et al studied enhancer effects of a series of alkyl homologues of N-alkylpyrrolidin-2-ones 68 (RQC 2 H 5 -RQC 12 H 25 ), see Figure 20, on transdermal penetration of steroid hormones (b-estradiol, corticosterone, and hydrocortisone) through the hairless mouse skin in vitro. N-octylpyrrolidin-2-one (68, RQC 8 H 17 ) was estimated as the most effective; it showed the same effect at 600 times less concentration in comparison with N-ethylpyrrolidin-2-one (68, RQC 2 H 5 ).…”

Section: C-lactams/pyrrolidine Analoguesmentioning

confidence: 99%

Azone analogues: classification, design, and transdermal penetration principles

Jampílek

Brychtova

2010

Medicinal Research Reviews

View full text Add to dashboard Cite

The development in the field of pharmaceutical dosage forms results in the discovery of additional highly sophisticated drug delivery systems that allow maintaining a constant level of the active substance in an organism. Transdermal therapeutic systems are an excellent alternative to conventional pharmaceutical dosage forms. However, the application of transdermal drug delivery faces the problem of insufficient or no penetration of active pharmaceutical substances through the skin. This review article describes the possible fundamental mechanisms of penetration through the skin barrier and refers to the classification of skin penetration enhancers. Azone-like enhancers are considered in detail and classified according to their structure on the basis of medicinal chemistry approaches. The article also provides a review of original transdermal penetration enhancers prepared in our laboratory and discusses the relationship between the chemical structure of the described Azone analogues and their penetration activity (SAR/QSAR).

show abstract

Effects of vehicles and enhancers on transdermal delivery of clebopride

Cited by 27 publications

References 33 publications

Effects of solvent deposited enhancers on transdermal permeation and their relationship with Emax

Effects of solvent deposited enhancers on transdermal permeation and their relationship with Emax

Transdermal nicotine mixed natural rubber-hydroxypropylmethylcellulose film forming systems for smoking cessation:in vitroevaluations

Azone analogues: classification, design, and transdermal penetration principles

Contact Info

Product

Resources

About