Delivery of ibuprofen to the skin

Patel, Avnish; Bell, Mike; O’Connor, Clare M.; Inchley, Andrew; Wibawa, Judata I.; Lane, Majella E.

doi:10.1016/j.ijpharm.2013.09.019

Cited by 47 publications

(45 citation statements)

References 30 publications

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“…Therefore, it is important to design enhancement techniques to assist the dermal delivery of IBU, and several research has been done to develop the topical and transdermal IBU formulations 7 9 . These systems have been employed to improve the delivery of IBU through the skin, and it have been developed the different dermal formulations such as patches 7 , gels 8 and liposomes 9 incorporating various permeation enhancers. In addition, strategies using nanoparticles and nanocarriers have also been demonstrated 9 .…”

Section: Introductionmentioning

confidence: 99%

“…These systems have been employed to improve the delivery of IBU through the skin, and it have been developed the different dermal formulations such as patches 7 , gels 8 and liposomes 9 incorporating various permeation enhancers. In addition, strategies using nanoparticles and nanocarriers have also been demonstrated 9 . A number of groups have been studied the lipid nanocarriers for dermal drug delivery.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic Studies of Gel System Containing Ibuprofen Solid Nanoparticles

2016

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic Studies of Gel System Containing Ibuprofen Solid Nanoparticles

2016

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“…The drug, usually administered in its racemic form, 6 is relatively lipophilic (log P=4.0) with low water solubility (21 mg/L at 25°C). 6,7 The characteristics of the permeation of IBU through the human skin have been reported by a number of research groups. [8][9][10][11][12][13] Earlier studies revealed that the topical therapeutic effectiveness of a drug is a function both of its penetration through the skin and of its potency.…”

Section: Introductionmentioning

confidence: 99%

“…[8][9][10][11][12][13] Earlier studies revealed that the topical therapeutic effectiveness of a drug is a function both of its penetration through the skin and of its potency. 7 IBU is less potent than diclofenac, for example, but the higher flux of IBU through the skin means that it is a better candidate for topical delivery, although it is still difficult to achieve its effective permeation by transdermal delivery. 14 The aforementioned physicochemical properties of IBU have hampered the preparation of a formulation satisfying the requirements of a long-lasting treatment for a chronic disease such as OA.…”

Section: Introductionmentioning

confidence: 99%

Development of ibuprofen-loaded nanostructured lipid carrier-based gels: characterization and investigation of in vitro and in vivo penetration through the skin

Sütő¹,

Berkó²,

Kozma³

et al. 2016

IJN

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An ibuprofen-loaded nanostructured lipid carrier (IBU-NLC) was developed for enhanced skin penetration to improve the treatment of osteoarthritis and other musculoskeletal diseases. The mean particle size was 106 nm, with a spherical morphology, a smooth surface, and a zeta potential of −18.4 mV. X-ray diffraction studies revealed the amorphous state of the lipid matrix. Both Raman spectroscopy and Fourier transformation infrared analysis indicated no major shifts in the spectra of the formulations, which suggest rapid drug dissolution from the nanoparticles. The drug loading was 9.85%, and the entrapment efficiency was 98.51%. In vitro release of the NLC dispersion, in vitro permeation, and in vivo animal studies of IBU-NLC gel all confirmed that the permeation of IBU was significantly better than that of a reference after 6 hours. In conclusion, IBU-NLC gel is of great potential to enhance drug permeation through the skin and hence the efficacy of the treatment of chronic joint inflammation.

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“…17 COX-1 is responsible for the production of prostanoids (prostaglandins and thromboxanes) that control a range of physiological functions. 4 Ibuprofen is metabolized primarily in the liver, and <10% of a dose is excreted unchanged. Depending on dose, ibuprofen is at least as effective as acetaminophen, ketoprofen, and aspirin in controlling pain.…”

mentioning

confidence: 99%

A Pharmacokinetic Study of an Ibuprofen Topical Patch in Healthy Male and Female Adult Volunteers

Lewis

Connolly

Bhatt

2018

Clinical Pharm in Drug Dev

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The pharmacokinetics of a novel locally applied ibuprofen topical patch was evaluated. Healthy subjects (n = 28) were administered a 200-mg ibuprofen patch every 24 hours for 5 days, and steady-state pharmacokinetics was determined. The amount of ibuprofen remaining in the patch following each patch removal was also assessed. The maximum steady-state drug concentration and area under the concentration curve from time 0 on day 5 (t = 0) to the 24-hours sample on day 6 were 514 ng/mL (95% CI 439 to 603 ng/mL) and 9.78 kg·h/mL (95% CI 8.43 to 11.4 kg·h/mL), respectively. Maximum ibuprofen concentration on day 5 occurred at 20 hours post-patch application. No evidence of drug accumulation was observed, and steady state was achieved between days 2 and 5. Ibuprofen levels attenuated rapidly to baseline within 24 hours after treatment discontinuation. The amount of ibuprofen remaining in the patch was high (≥80%). Treatment-emergent adverse events were generally mild, with the most prevalent being headache (n = 6; 21.4%). Only 4 TEAEs were considered related to the ibuprofen patch: paresthesia (n = 1), headache (n = 2), and pruritic rash (n = 1). The study found that the systematic absorption of ibuprofen from a 200-mg patch was low and that the levels of ibuprofen leaving the patch over a 24-hour period are consistent with levels required for therapeutic relief as shown in other studies.

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Delivery of ibuprofen to the skin

Cited by 47 publications

References 30 publications

Pharmacokinetic Studies of Gel System Containing Ibuprofen Solid Nanoparticles

Pharmacokinetic Studies of Gel System Containing Ibuprofen Solid Nanoparticles

Development of ibuprofen-loaded nanostructured lipid carrier-based gels: characterization and investigation of in vitro and in vivo penetration through the skin

A Pharmacokinetic Study of an Ibuprofen Topical Patch in Healthy Male and Female Adult Volunteers

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