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Skin Permeation and Antinociception of Compounded Topical Cyclobenzaprine Hydrochloride Formulations

Author(s):  Bryson Evan, Hartman Rachel, Arnold John, Gorman Greg, Sweitzer Sarah.Asbill Scott

Issue:  Mar/Apr 2015 - Volume 19, Number 2
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Abstract:  Cyclobenzaprine has been commonly compounded by pharmacists into topically applied dosage forms for the treatment of pain disorders. However, the efficacy and transdermal penetration of topically applied compounded cyclobenzaprine is currently unknown. In this study, the transdermal penetration of cyclobenzaprine was studied in Franz diffusion cells using porcine skin. Cyclobenzaprine was compounded in two commercially available bases; Lipobase, Lipoderm, and a standard poloxamer lecithin organogel. In addition, cyclobenzaprine was tested in an in vivo formalin pain model. Cyclobenzaprine 5% compounded into all three bases yielded significant transdermal penetration and results in modest levels of cyclobenzaprine being retained in the skin tissue. Systemically administered cyclobenzaprine (10 mcg/kg), but not topically administered cyclobenzaprine (1% and 5%), attenuated nociception in a rodent formalin pain model.

Related Keywords: Evan Bryson, Rachel Hartman, BSc, John Arnold, PhD, Greg Gorman, PhD, Sarah Sweitzer, PhD, Scott Asbill, PhD, cyclobenzaprine, chronic pain, topical preparation, transdermal delivery, skin permeation, transdermal penetration, vehicle, commercial bases, formalin pain model, pain-related behavior, antinociception, pain control, analgesia, topical analgesics, muscle relaxant, permeability studies


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