Topical oleo-hydrogel preparation of ketoprofen with enhanced skin permeability

Gye Ju Rhee, Jong Soo Woo, Sung Joo Hwang, Young Wook Lee, Chang Hyun Lee

Research output: Contribution to journalArticle

30 Citations (Scopus)

Abstract

In an attempt to improve the skin penetration of ketoprofen, various transdermal formulations were prepared, and their in vitro skin permeability and in vivo percutaneous absorption were evaluated. In vitro permeation studies were performed using a modified Franz cell diffusion system in which permeation parameters such as cumulative amount at 8 hr Q(8hr), steady-state flux J(ss), or lag time t(L) were determined. In the in vivo percutaneous absorption study using the hairless mouse, maximum concentration C(max) and area under the curve at 24 hr AUC(24h) were measured. The optimal transdermal formulation (oleo-hydrogel formulation) of ketoprofen showed a Q(8hr) value of 227.20 μg/cm2, a J(ss) value of 29.61 μg/cm2/hr, and a t(L) value of 0.46 hr. The Q(8hr) and J(ss) values were about 10-fold (p < .01) higher than those (Q(8hr) = 19.61 μg/cm2; J(ss) = 2.66 μg/cm2/hr) from the K-gel and about 3.5-fold (p < .01) than those (Q(8hr) = 60.00 μg/cm2; J(ss) = 7.99 μg/cm2/hr) of the K-plaster. In the in vivo percutaneous absorption, the C(max) (6.82 μg/ml) and AUC(24h) (55.74 μg · hr/ml) values of the optimal formulation were significantly (p < .01) higher than those of K-gel and K- plaster. The relative bioavailability of the oleo-hydrogel following transdermal administration in reference to oral administration was about 37%, and the C(max) value (4.73 μg/cm2) in the hypodermis following topical administration was much higher than those from the conventional products (C(max) of K-gel and K-plaster were 0.92 ± 0.19 μg/cm2 and 1.27 ± 0.37 μg/cm2, respectively). These data demonstrate that the oleo-hydrogel formulation of ketoprofen was more beneficial than conventional products (K- gel and K-plaster) in enhancing transdermal permeation and skin absorption of ketoprofen. Furthermore, there was a good correlation between in vitro permeation parameters and in vivo percutaneous absorption parameters.

Original languageEnglish
Pages (from-to)717-726
Number of pages10
JournalDrug Development and Industrial Pharmacy
Volume25
Issue number6
DOIs
Publication statusPublished - 1999 Jun 1

Fingerprint

Skin Absorption
Ketoprofen
Plaster
Hydrogel
Permeation
Permeability
Skin
Gels
Area Under Curve
Cutaneous Administration
Hairless Mouse
Topical Administration
Subcutaneous Tissue
Fluxes
Biological Availability
Oral Administration
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

Cite this

Rhee, Gye Ju ; Woo, Jong Soo ; Hwang, Sung Joo ; Lee, Young Wook ; Lee, Chang Hyun. / Topical oleo-hydrogel preparation of ketoprofen with enhanced skin permeability. In: Drug Development and Industrial Pharmacy. 1999 ; Vol. 25, No. 6. pp. 717-726.
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abstract = "In an attempt to improve the skin penetration of ketoprofen, various transdermal formulations were prepared, and their in vitro skin permeability and in vivo percutaneous absorption were evaluated. In vitro permeation studies were performed using a modified Franz cell diffusion system in which permeation parameters such as cumulative amount at 8 hr Q(8hr), steady-state flux J(ss), or lag time t(L) were determined. In the in vivo percutaneous absorption study using the hairless mouse, maximum concentration C(max) and area under the curve at 24 hr AUC(24h) were measured. The optimal transdermal formulation (oleo-hydrogel formulation) of ketoprofen showed a Q(8hr) value of 227.20 μg/cm2, a J(ss) value of 29.61 μg/cm2/hr, and a t(L) value of 0.46 hr. The Q(8hr) and J(ss) values were about 10-fold (p < .01) higher than those (Q(8hr) = 19.61 μg/cm2; J(ss) = 2.66 μg/cm2/hr) from the K-gel and about 3.5-fold (p < .01) than those (Q(8hr) = 60.00 μg/cm2; J(ss) = 7.99 μg/cm2/hr) of the K-plaster. In the in vivo percutaneous absorption, the C(max) (6.82 μg/ml) and AUC(24h) (55.74 μg · hr/ml) values of the optimal formulation were significantly (p < .01) higher than those of K-gel and K- plaster. The relative bioavailability of the oleo-hydrogel following transdermal administration in reference to oral administration was about 37{\%}, and the C(max) value (4.73 μg/cm2) in the hypodermis following topical administration was much higher than those from the conventional products (C(max) of K-gel and K-plaster were 0.92 ± 0.19 μg/cm2 and 1.27 ± 0.37 μg/cm2, respectively). These data demonstrate that the oleo-hydrogel formulation of ketoprofen was more beneficial than conventional products (K- gel and K-plaster) in enhancing transdermal permeation and skin absorption of ketoprofen. Furthermore, there was a good correlation between in vitro permeation parameters and in vivo percutaneous absorption parameters.",
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Topical oleo-hydrogel preparation of ketoprofen with enhanced skin permeability. / Rhee, Gye Ju; Woo, Jong Soo; Hwang, Sung Joo; Lee, Young Wook; Lee, Chang Hyun.

In: Drug Development and Industrial Pharmacy, Vol. 25, No. 6, 01.06.1999, p. 717-726.

Research output: Contribution to journalArticle

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T1 - Topical oleo-hydrogel preparation of ketoprofen with enhanced skin permeability

AU - Rhee, Gye Ju

AU - Woo, Jong Soo

AU - Hwang, Sung Joo

AU - Lee, Young Wook

AU - Lee, Chang Hyun

PY - 1999/6/1

Y1 - 1999/6/1

N2 - In an attempt to improve the skin penetration of ketoprofen, various transdermal formulations were prepared, and their in vitro skin permeability and in vivo percutaneous absorption were evaluated. In vitro permeation studies were performed using a modified Franz cell diffusion system in which permeation parameters such as cumulative amount at 8 hr Q(8hr), steady-state flux J(ss), or lag time t(L) were determined. In the in vivo percutaneous absorption study using the hairless mouse, maximum concentration C(max) and area under the curve at 24 hr AUC(24h) were measured. The optimal transdermal formulation (oleo-hydrogel formulation) of ketoprofen showed a Q(8hr) value of 227.20 μg/cm2, a J(ss) value of 29.61 μg/cm2/hr, and a t(L) value of 0.46 hr. The Q(8hr) and J(ss) values were about 10-fold (p < .01) higher than those (Q(8hr) = 19.61 μg/cm2; J(ss) = 2.66 μg/cm2/hr) from the K-gel and about 3.5-fold (p < .01) than those (Q(8hr) = 60.00 μg/cm2; J(ss) = 7.99 μg/cm2/hr) of the K-plaster. In the in vivo percutaneous absorption, the C(max) (6.82 μg/ml) and AUC(24h) (55.74 μg · hr/ml) values of the optimal formulation were significantly (p < .01) higher than those of K-gel and K- plaster. The relative bioavailability of the oleo-hydrogel following transdermal administration in reference to oral administration was about 37%, and the C(max) value (4.73 μg/cm2) in the hypodermis following topical administration was much higher than those from the conventional products (C(max) of K-gel and K-plaster were 0.92 ± 0.19 μg/cm2 and 1.27 ± 0.37 μg/cm2, respectively). These data demonstrate that the oleo-hydrogel formulation of ketoprofen was more beneficial than conventional products (K- gel and K-plaster) in enhancing transdermal permeation and skin absorption of ketoprofen. Furthermore, there was a good correlation between in vitro permeation parameters and in vivo percutaneous absorption parameters.

AB - In an attempt to improve the skin penetration of ketoprofen, various transdermal formulations were prepared, and their in vitro skin permeability and in vivo percutaneous absorption were evaluated. In vitro permeation studies were performed using a modified Franz cell diffusion system in which permeation parameters such as cumulative amount at 8 hr Q(8hr), steady-state flux J(ss), or lag time t(L) were determined. In the in vivo percutaneous absorption study using the hairless mouse, maximum concentration C(max) and area under the curve at 24 hr AUC(24h) were measured. The optimal transdermal formulation (oleo-hydrogel formulation) of ketoprofen showed a Q(8hr) value of 227.20 μg/cm2, a J(ss) value of 29.61 μg/cm2/hr, and a t(L) value of 0.46 hr. The Q(8hr) and J(ss) values were about 10-fold (p < .01) higher than those (Q(8hr) = 19.61 μg/cm2; J(ss) = 2.66 μg/cm2/hr) from the K-gel and about 3.5-fold (p < .01) than those (Q(8hr) = 60.00 μg/cm2; J(ss) = 7.99 μg/cm2/hr) of the K-plaster. In the in vivo percutaneous absorption, the C(max) (6.82 μg/ml) and AUC(24h) (55.74 μg · hr/ml) values of the optimal formulation were significantly (p < .01) higher than those of K-gel and K- plaster. The relative bioavailability of the oleo-hydrogel following transdermal administration in reference to oral administration was about 37%, and the C(max) value (4.73 μg/cm2) in the hypodermis following topical administration was much higher than those from the conventional products (C(max) of K-gel and K-plaster were 0.92 ± 0.19 μg/cm2 and 1.27 ± 0.37 μg/cm2, respectively). These data demonstrate that the oleo-hydrogel formulation of ketoprofen was more beneficial than conventional products (K- gel and K-plaster) in enhancing transdermal permeation and skin absorption of ketoprofen. Furthermore, there was a good correlation between in vitro permeation parameters and in vivo percutaneous absorption parameters.

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