Ion Pair Formation as a Possible Mechanism for the Enhancement Effect of Lauric Acid on the Transdermal Permeation of Ondansetron

Dimas, Dimitrios A.; Dallas, Paraskevas; Rekkas, Dimitrios M.

doi:10.1081/pdt-200031449

Cited by 21 publications

(12 citation statements)

References 25 publications

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“…It has a molecular weight of 293 Da, a logP value of 2.07 and its pKa is about 7.4 [ 18 , 19 ]. The effects of various vehicles, delivery systems and enhancers on transdermal OND delivery have been reported in the literature [ 19 , 20 , 21 , 22 ], but there are a few reports indicating the possibility of developing transdermal film formulations of OND [ 22 , 23 , 24 , 25 ].…”

Section: Introductionmentioning

confidence: 99%

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

et al. 2013

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The aim of this study was to develop novel transdermal films of ondansetron HCl with high molecular weight chitosan as matrix polymer and 2-(2-ethoxy-ethoxy) ethanol (Transcutol®) as plasticizer. In this context, firstly the physicochemical properties of gels used to formulate transdermal films were characterized and, physicochemical properties and bioadhesiveness of the transdermal films prepared with chitosan gels were assessed. The impact of three different types of terpenes, namely limonene, nerolidol and eucalyptol on in vitro skin permeation of ondansetron from transdermal films were also examined. ATR-FTIR measurements were performed to investigate the effects of the chitosan film formulations on in vitro conformational order of stratum corneum intercellular lipids after 24 h permeation study. The results showed that the chitosan gels consisting of Transcutol® as plasticizer and terpenes as penetration enhancer may be used to prepare transdermal films of ondansetron due to the good mechanical properties and bioadhesiveness of the transdermal films. Eucalyptol (1%) showed higher permeation enhancer effect than the other terpenes and control. ATR-FTIR data confirmed that finding in which eucalyptol induced a blue shift in the both CH2 asymmetric and symmetric absorbance peak positions indicating increased lipid fluidity of stratum corneum.

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Section: Introductionmentioning

confidence: 99%

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

et al. 2013

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“…Thus, it is aimed at developing transdermal therapeutic systems for ondansetron hydrochloride for their possible use in the treatment of chemotherapy-induced nausea and vomiting in patients with cancer. In this context, a few reports appear in the literature indicating the possibility of developing transdermal formulations for ondansetron hydrochloride (Takahashi and Rytting 2001;Gwak et al 2003;Gwak et al 2004;Dimas et al 2004;Dimas et al 2004a). Thus, ondansetron hydrochloride is a good model drug for developing a membrane-controlled transdermal therapeutic systems (TTS).…”

Section: Introductionmentioning

confidence: 99%

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

et al. 2008

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The aim of this investigation was to study the effect of an ethanolwater solvent system and ehtanolic solution of menthol on the permeation of ondansetron hydrochloride across the rat epidermis in order to select a suitable ethanol-water vehicle and optimal concentration of menthol for the development of a transdermal therapeutic system. The solubility of ondansetron hydrochloride in ethanol, water and selected concenetrtaion of ethanol-water vehicles (20:80 v/v, 40:60 v/v and 60:40 v/v) was determined. The effect of these solvent vehicles, containing 1.5% w/v of ondansetron hydrochloride, on the in vitro permeation of the drug was studied across the rat epidermis. The highest permeation was observed from 60% v/v of ethanol-water vehicle that showed highest solubilty. Hence, the hydroxypropyl cellulose (HPC) (2% w/w) gel formulations containing 1.5% w/w of ondansetron hydrochloride and selected concentrations of menthol (0, 2, 4, 8 and 10% w/w) were prepared using 60% v/v of ethanol-water vehicle, and subjected to in vitro permeation of the drug across rat epidermis. The transdermal permeation of ondansetron hydrochloride was enhanced markedly by the addition of menthol to HPC gel drug reservoir formulations. A maximum flux of ondansetron hydrochloride (77.85 ± 2.85 μg/cm 2. h) was observed with a mean enhancement ratio of 13.06 when menthol was incorporated at a concentration of 8% w/w in HPC gels. However, there was no significant increase in the drug flux with 10% w/w menthol when compared to that obtained with 8% w/w of menthol in HPC gel formulations. The results suggest that 2% w/w HPC gel drug reservoir formulation, prepared with 60% v/v ethanol-water, containing 8% w/w of menthol provides an optimal transdermal permeation of ondansetron hydrochloride.

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“…[8][9][10] In this context, a few reports appear in the literature indicating the possibility of developing transdermal formulations for ondansetron hydrochloride. [12][13][14][15] Thus, ondansetron hydrochloride is a good model drug for developing a membrane-controlled TTS.…”

Section: Introductionmentioning

confidence: 99%

Studies on Optimizing In Vitro Transdermal Permeation of Ondansetron Hydrochloride Using Nerodilol, Carvone, and Limonene as Penetration Enhancers

Krishnaiah

Raju

Kumar

et al. 2008

Pharmaceutical Development and Technology

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The present investigation was carried out to formulate a terpene-based hydroxypropyl cellulose (HPC) gel drug reservoir system for its optimal transdermal permeation of ondansetron hydrochloride. The HPC gel formulations containing ondansetron hydrochloride (3% w/w) and selected concentrations of either nerodilol (0% w/w, 1% w/w, 2% w/w, 3% w/w, and 4% w/w), carvone (0% w/w, 2% w/w, 4% w/w, 8% w/w, and 10% w/w), or limonene (0% w/w, 2% w/w, 3% w/w, and 4% w/w) were prepared and subjected to in vitro permeation of the drug across rat epidermis. All the 3 terpene enhancers increased the transdermal permeation of ondansetron hydrochloride. The optimal transdermal permeation was observed with 3% w/w of nerodilol (175.3 ± 3.1 μg/ cm 2. h), 8% w/w of carvone (87.4 ± 1.6 μg/cm 2. h), or 3% w/w of limonene (181.9 ± 0.9 μg/cm 2. h). The enhancement ratio (ER) in drug permeability with 3% w/w nerodilol, 8% w/w carvone, and 3% w/w limonene were 21.6, 10.8, and 22.5, respectively, when compared with that obtained without a terpene enhancer (control). However, there was 1.04-, 2.09-, and 2.17-fold increase in the optimal drug flux obtained with carvone, nerodilol, and limonene, respectively, when compared with the desired drug flux (84 μg/cm 2. h). It was concluded that the HPC gel drug reservoir systems containing either 3% w/w nerodilol or 3% w/w limonene act as optimal formulations for use in the design of membrane-controlled transdermal therapeutic system (TTS) of ondansetron hydrochloride.

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Ion Pair Formation as a Possible Mechanism for the Enhancement Effect of Lauric Acid on the Transdermal Permeation of Ondansetron

Cited by 21 publications

References 25 publications

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

Studies on Optimizing In Vitro Transdermal Permeation of Ondansetron Hydrochloride Using Nerodilol, Carvone, and Limonene as Penetration Enhancers

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