Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances

Abstract

Indomethacin (IND) is a drug which after successful clinical trials became available for general prescription in 1965 and from that time is one of the most widely used anti-inflammatory drug with the highest potencies in the in vitro and in vivo models. However, despite its high therapeutic efficacy in relieving the symptoms of certain arthritis and in treating gout or collagen diseases, administration of IND causes a number of adverse effects, such as gastrointestinal ulceration, frequent central nervous system disorders and renal toxicity. These obstacles significantly limit the practical applications of IND and make that 10–20% of patients discontinue its use. Therefore, during the last three decades many attempts have been made to design novel formulations of IND aimed to increase its therapeutic benefits minimizing its adverse effects. In this review we summarize pharmacological information about IND and analyze its new lipid formulations and lipid bioconjugates as well as discuss their efficacy and potential application.

Highly Porous and Drug-Loaded Amorphous Solid Dispersion Microfiber Scaffolds of Indomethacin Prepared by Melt Electrowriting

“…5 However, at the same time, its short half-life time and the associated repeated oral administration result in toxicity issues in the digestive system and kidneys as well as malaises like nausea, stomach pain, and diarrhea, which could be expected to be reduced by using a sublingual delivery system. 6 Maintaining drugs in their amorphous state improves the dissolution rate and oral bioavailability. 7 However, some limitations including recrystallization due to the physical instability of the amorphous state and residual microcrystallinity of the drug can cause problems such as patientto-patient variability.…”

“…This nonsteroidal anti-inflammatory drug is commonly used as a painkiller by oral administration to reduce fever and swelling, as well as a medication to treat rheumatoid arthritis or osteoarthritis due to its strong action and high therapeutic efficacy . However, at the same time, its short half-life time and the associated repeated oral administration result in toxicity issues in the digestive system and kidneys as well as malaises like nausea, stomach pain, and diarrhea, which could be expected to be reduced by using a sublingual delivery system …”

The Effect of Indomethacin on the Sperm Motility of Adult Wistar Rats

“…Indomethacin is a non-steroidal anti-inflammatory drug (NSAID) that is very effective in the treatment of pain, feverish conditions, and inflammation, like other NSAIDs it reduces pain and inflammation [1]. Generally, non-steroidal anti-inflammatory drugs (NSAIDs) are a diverse group of drugs, frequently unrelated chemically, yet the majority are organic acids and known in the treatment of conditions, such as osteoarthritis, rheumatoid arthritis, different type of inflammation, gout, menstrual cramps, dental pain, and headache [2]. However numerous adverse reactions have been linked to NSAIDs use which include nausea, vomiting, diarrhea, constipation, reduced appetite, rash, dizziness, headaches, sleepiness, and stomach ulcers [1, 3,4].…”

Highly Porous and Drug Loaded Amorphous Solid Dispersions Microfiber Scaffolds of Indomethacin prepared by Melt Electrowriting

“…However, at the same time, its short half-life time and the associated repeated oral administration result in toxicity-issues toward the digestive system and kidneys as well as malaises like nausea, stomach pain, and diarrhoea which could be expected to be reduced by using sublingual delivery system. 6 Maintaining drugs in their amorphous state improves the dissolution rate and oral bioavailability. 7 However, some limitations including recrystallization due to the physical instability of the amorphous state and residual micro-crystallinity of the drug can cause problems such as patient-to-patient variability.…”