Abstract
Etodolac (ETD), a nonsteroidal anti-inflammatory drug, exhibits antinflammatory, analgesic, and antipyretic activity. The main type of ETD administration is oral route, which is associated with significant systemic side effects. Nanostructured lipid carriers (NLC), a modern lipid formulation, are non-toxic, biocompatible, can improve the solubility and stability of drugs. Nanostructured lipid carriers (NLC) containing etodolac were prepared by a melt-emulsification and ultrasonication technique. Full factorial design (FFD) was applied to optimize the composition of NLC and their properties such as zeta potential, polidyspersity index, and entrapment efficiency. Formulations consisting of Capryol 90, glicerol monostearate, and Tween 20 displayed particle size below 300 nm, encapsulated drug with efficiency of approximately 87% and prolonged drug release up to 24 h. Stable formulations displayed moderately negative surface charge suggesting their limited ability to interact with skin surface but simultaneously presenting their lower risk to cause cell-membrane disruption. In fact, cytotoxicity assessment using human dermal fibroblasts and human epidermal keratinocytes revealed that etodolac-loaded NLC had no important impact on skin cells viability evaluated in vitro, which might evidence that NLC formulations are safe for dermal delivery. The studies developed were relatively fast and simple, requiring no specialized equipment method to prepare NLC as ETD carriers ensuring better solubility and prolonged drug release.
Highlights
Introduction iationsEtodolac (1,8-diethyl-1,3,4,9-tetrahydropyranol(3,4-b)indole-1-acetic acid, ETD) is a nonsteroidal anti-inflammatory drug belonging to the group of selective cyclooxygenase-2 inhibitors
Capryol 90 and Miglyol 812 which ensured the greatest solubility of ETD and miscibility with solid lipids were selected for further analysis
Tween 20 provided the highest solubility of ETD (30.98 mg/g) and was selected for Nanostructured lipid carriers (NLC) preparation
Summary
Etodolac (1,8-diethyl-1,3,4,9-tetrahydropyranol(3,4-b)indole-1-acetic acid, ETD) is a nonsteroidal anti-inflammatory drug belonging to the group of selective cyclooxygenase-2 inhibitors. Apart from anti-inflammatory activity, ETD exerts analgesic and antipyretic activity and is mainly used for osteoarthritis and rheumatoid arthritis. Because of relatively shorter terminal half-life (approximately 7 h), sufficient treatment via oral route requires frequent dosing which may lead to adverse cardiovascular effects, fluid retention, edema, or gastrointestinal problems including bleeding, ulceration, and perforation. Local delivery systems with ETD have gained particular attention with potential to enhance local treatment efficacy and simultaneously reduce systemic adverse effects. ETD is a biopharmaceutical classification system (BCS) class II drug, characterized by poor solubility in water (0.016 mg/mL), but high permeability through a lipophilic barriers.
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