Nasal absorption of ondansetron in rats: an alternative route of drug delivery

Hussain, Anwar; Dakkuri, Adnan; Itoh, Soichi

doi:10.1007/s002800051014

Cited by 34 publications

(15 citation statements)

References 6 publications

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“…Sustained-release formulations may enable the ondansetron dosing-frequency to be reduced, and therefore increase patient compliance. Rectal (Hsyu et al 1994) and nasal (Hussain et al 2000) absorption of ondansetron have been reported. The transdermal administration of drugs bypasses the first-pass effect, minimizes inter-and intra-patient variation and provides steadystate plasma concentration of the drug and long-term therapy from a single dose.…”

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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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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“…Daily injections of small doses of PTH, which cause brief plasma pulses of the hormone, stimulate bone growth in various species and, most important, in osteoporotic women (20). Therefore, alternative noninvasive approaches that may result in short plasma pulses of the hormone are preferable for chronic administration of the drug for treatment of bone disorders.…”

Section: In Vivo Studiesmentioning

confidence: 99%

Intranasal Delivery of Recombinant Human Parathyroid Hormone [hPTH (1–34)], Teriparatide in Rats

et al. 2004

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The aim of this study was to explore the nasal route as an alternative to daily subcutaneous injections of hPTH (1-34). Anesthetized rats were surgically prepared and nasally dosed with aqueous solutions of hPTH (1-34). Plasma samples were assayed by radioimmunoassay and data generated fit to two-(intravenous) and one-(intranasal) compartment pharmacokinetic models using WinNonlin. The toxicity of hPTH (1-34) solution administered to the rats was assessed by screening its effect on transepithelial electrical resistance, potential difference, paracellular marker permeation, tissue viability, and protein leakage using the EpiAirway tissue model. The intranasal absorption of hPTH (1-34) was rapid; the absorption rate constants (alpha) were 33.2+/-24 h(-1) [without bovine serum albumin (BSA)] and 9.8+/-5.1 h(-1) (with 1% BSA). The maximum plasma concentrations (Cmax): 151+/-24 pg/mL (without BSA) and 176+/-37 (with 1% BSA) were attained within approximately 15 min. The intranasal bioavailabilities (Fabs) were 12.1+/-3.4% (without BSA) and 17.6+/-1.5% (with 1% BSA). The hPTH (1-34) formulation administered to the rats had no detrimental effect on the EpiAirway tissue epithelial electrical parameters and functional integrity. Based on the results of this study, the nasal route appears to be a prospective alternative to subcutaneous injections of hPTH (1-34).

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“…delivery of antiemetics, alternative delivery routes for OND have been studied. Transdermal [91][92][93][94] and nasal routes [95][96][97][98][99][100][101] are the most attractive routes. Besides, colon delivery of OND was investigated [102].…”

Section: Ondansetronmentioning

confidence: 99%

Nasal route: an alternative approach for antiemetic drug delivery

Özsoy

Güngör

2011

Expert Opinion on Drug Delivery

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Due to its superiorities, the nasal route could be considered as an attractive alternative to oral and parenteral routes. To overcome the barrier properties of the nasal epithelium and to enhance transport of antiemetic drugs, several approaches, including permeation enhancers, in situ gel formulations and micro- and nanoparticulate systems, have been evaluated. The results obtained are promising and indicate that nasal formulations of some antiemetic drugs may enter the market in the near future.

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Nasal absorption of ondansetron in rats: an alternative route of drug delivery

Cited by 34 publications

References 6 publications

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

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

Intranasal Delivery of Recombinant Human Parathyroid Hormone [hPTH (1–34)], Teriparatide in Rats

Nasal route: an alternative approach for antiemetic drug delivery

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