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Effect of Penetration Enhancers on the Percutaneous Delivery of Pain Management Actives

Author(s):  Trimble John, Light Bob

Issue:  May/Jun 2016 - Volume 20, Number 3
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Abstract:  Transdermal compositions for pain management are comprised of nonsteroidal anti-inflammatory drugs, opioid drugs, and adjuvant drugs acting on: voltage-gated channels, gamma-aminobutyric acid receptors, acute musculoskeletal pain, and as an antidepressant. In this work, baclofen, bupivacaine, cyclobenzaprine, diclofenac, gabapentin, ibuprofen, ketamine, and pentoxifylline were loaded in transdermal compositions, prepared using a mixture of lipids (isopropyl palmitate and mineral oil) and one of two selected penetration enhancer mixtures: alkyl dimethicone, phenyl trimethicone, and polyoxyethylene sorbitan monostearate; and cetostearyl polyoxyethylene ether and ethylene oxide/propylene oxide copolymer. The influence of penetration enhancers on transdermal delivery was evaluated using Franz-type diffusion cells and Normal Human 3D Model of Epidermal Tissue. Results showed that drug delivery is affected by the penetration enhancer used in the transdermal composition.

Related Keywords: John Trimble, BS Chemistry, Bob Light, BS Pharm, penetration enhancers, topical preparation, transdermal permeability, percutaneous drug delivery, skin penetration, pain, analgesia, analgesic, adjuvant pain control, voltage-gated channels, gamma-aminobutyric acid receptors, GABA receptors, acute musculoskeletal pain, muscle relaxants, antidepressants, baclofen, bupivacaine, cyclobenzaprine, diclofenac, gabapentin, ibuprofen, ketamine, pentoxifylline, nonsteroidal anti-inflammatory drug, NSAID, alkyl dimethicone, phenyl trimethicone, polyoxyethylene sorbitan monostearate, cetosteryl polyoxyethylene ether, ethylene oxide, propylene oxide copolymer, emulsifiers, lipids, engineered human skin


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