Abstract
Ibuprofen is one of the non-steroidal anti-inflammatory drugs (NSAIDs) widely used to treat pain conditions. NSAIDs encounter several obstacles to passing across biological membranes. To overcome these constraints, we decided to study the effects of a new pH-sensitive formulation of niosomes containing Polysorbate 20 derivatized by Glycine and loaded with ibuprofen (NioIbu) in several animal models of pain in mice. We performed two tests commonly used to study acute antinociceptive activity, namely the writhing test and the capsaicin test. Our results demonstrated that NioIbu, administered 2 h before testing, reduced nociception, whereas the free form of ibuprofen was ineffective. In a model of inflammatory pain, hyperalgesia induced by zymosan, NioIbu induced a long-lasting reduction in hyperalgesia in treated mice. In a model of neuropathic pain induced by sciatic nerve chronic constriction, NioIbu reduced both neuropathy-induced allodynia and hyperalgesia. The results obtained in our experiments suggest that pH-sensitive niosomes containing Polysorbate 20 derivatized by Glycine is an effective model for NSAIDs delivery, providing durable antinociceptive effects and reducing the incidence of side effects.
Highlights
The non-steroidal anti-inflammatory drug (NSAID) Ibuprofen (α-methyl-4-(2-methylpropyl) benzeneacetic acid, IBU) is commonly used in the treatment of pain, fever, and inflammatory diseases.Ibuprofen was discovered in 1960 for the treatment of some pain conditions and inflammatory autoimmune diseases, such as rheumatoid arthritis [1]
For both the samples, the diameter evaluated by Atomic force microscopy (AFM) is 70% of that evaluated by DLS, probably due to the approximations assumed in the model
Several researchers have focused on alternative drug delivery systems to overcome the Several researchers have focused on alternative drug delivery systems to overcome the difficulties associated with the distribution and effectiveness of analgesic drugs
Summary
The non-steroidal anti-inflammatory drug (NSAID) Ibuprofen (α-methyl-4-(2-methylpropyl) benzeneacetic acid, IBU) is commonly used in the treatment of pain, fever, and inflammatory diseases. Ibuprofen was discovered in 1960 for the treatment of some pain conditions and inflammatory autoimmune diseases, such as rheumatoid arthritis [1]. In 1961, Ibuprofen became available in tablet form, and in 1983 was launched as a topical formulation. Ibuprofen is an analgesic drug that inhibits the production of cyclooxygenase (Cox-2) pathway-derived prostaglandins, which increase in inflamed tissues and control inflammatory disorder [2,3]. As is well-known, prostanoids mediate the sensation of peripheral and central pain, increasing membrane excitability and reducing the threshold of nociceptor stimulation [4].
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