Ibuprofen delivery into and through the skin from novel oxidized cellulose-based gels and conventional topical formulations

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Abstract

The delivery of ibuprofen into and through the skin from novel formulations containing TEMPO-oxidized cellulose nanofibril-based (TOCN) gels was compared to that from two conventional and commercially available products. The gels were evaluated in-vitro (using both silicone membranes, and pig skin) and in-vivo in human volunteers. All gels showed consistent behaviour in a standard in vitro release test. The stratum corneum (SC) uptake and skin penetration of ibuprofen in vitro from the novel gels and the marketed formulations were generally comparable even though the drug loading in the TOCN-based vehicles was only 20% of that in the ‘reference’ products. In vivo, the new gels appeared to enhance drug uptake into the SC following a relatively short application time, again matching the performance of the commercial formulations. Taken together, the results of this research provide proof-of-concept for the idea that the sustainable, oxidised cellulose gels may provide more efficient drug delivery into and through the skin, thereby improving drug utilisation and reducing potential adverse effects when such formulations are applied chronically over large skin areas.
LanguageEnglish
Pages238-243
Number of pages6
JournalInternational Journal of Pharmaceutics
Volume514
DOIs
StatusPublished - 30 Nov 2016

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oxidized cellulose
Ibuprofen
Gels
Skin
Cornea
Pharmaceutical Preparations
Drug Utilization
Silicones
Volunteers
Swine
Membranes
Research

Cite this

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title = "Ibuprofen delivery into and through the skin from novel oxidized cellulose-based gels and conventional topical formulations",
abstract = "The delivery of ibuprofen into and through the skin from novel formulations containing TEMPO-oxidized cellulose nanofibril-based (TOCN) gels was compared to that from two conventional and commercially available products. The gels were evaluated in-vitro (using both silicone membranes, and pig skin) and in-vivo in human volunteers. All gels showed consistent behaviour in a standard in vitro release test. The stratum corneum (SC) uptake and skin penetration of ibuprofen in vitro from the novel gels and the marketed formulations were generally comparable even though the drug loading in the TOCN-based vehicles was only 20{\%} of that in the ‘reference’ products. In vivo, the new gels appeared to enhance drug uptake into the SC following a relatively short application time, again matching the performance of the commercial formulations. Taken together, the results of this research provide proof-of-concept for the idea that the sustainable, oxidised cellulose gels may provide more efficient drug delivery into and through the skin, thereby improving drug utilisation and reducing potential adverse effects when such formulations are applied chronically over large skin areas.",
author = "Duygu Celebi and Karen Edler and Janet Scott and Richard Guy",
year = "2016",
month = "11",
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T1 - Ibuprofen delivery into and through the skin from novel oxidized cellulose-based gels and conventional topical formulations

AU - Celebi, Duygu

AU - Edler, Karen

AU - Scott, Janet

AU - Guy, Richard

PY - 2016/11/30

Y1 - 2016/11/30

N2 - The delivery of ibuprofen into and through the skin from novel formulations containing TEMPO-oxidized cellulose nanofibril-based (TOCN) gels was compared to that from two conventional and commercially available products. The gels were evaluated in-vitro (using both silicone membranes, and pig skin) and in-vivo in human volunteers. All gels showed consistent behaviour in a standard in vitro release test. The stratum corneum (SC) uptake and skin penetration of ibuprofen in vitro from the novel gels and the marketed formulations were generally comparable even though the drug loading in the TOCN-based vehicles was only 20% of that in the ‘reference’ products. In vivo, the new gels appeared to enhance drug uptake into the SC following a relatively short application time, again matching the performance of the commercial formulations. Taken together, the results of this research provide proof-of-concept for the idea that the sustainable, oxidised cellulose gels may provide more efficient drug delivery into and through the skin, thereby improving drug utilisation and reducing potential adverse effects when such formulations are applied chronically over large skin areas.

AB - The delivery of ibuprofen into and through the skin from novel formulations containing TEMPO-oxidized cellulose nanofibril-based (TOCN) gels was compared to that from two conventional and commercially available products. The gels were evaluated in-vitro (using both silicone membranes, and pig skin) and in-vivo in human volunteers. All gels showed consistent behaviour in a standard in vitro release test. The stratum corneum (SC) uptake and skin penetration of ibuprofen in vitro from the novel gels and the marketed formulations were generally comparable even though the drug loading in the TOCN-based vehicles was only 20% of that in the ‘reference’ products. In vivo, the new gels appeared to enhance drug uptake into the SC following a relatively short application time, again matching the performance of the commercial formulations. Taken together, the results of this research provide proof-of-concept for the idea that the sustainable, oxidised cellulose gels may provide more efficient drug delivery into and through the skin, thereby improving drug utilisation and reducing potential adverse effects when such formulations are applied chronically over large skin areas.

UR - http://dx.doi.org/10.1016/j.ijpharm.2016.09.028

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DO - 10.1016/j.ijpharm.2016.09.028

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JO - International Journal of Pharmaceutics

T2 - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

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