Nanostructured Lipid Carriers Engineered as Topical Delivery of Etodolac: Optimization and Cytotoxicity Studies

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.

Development of Tea Seed Oil Nanostructured Lipid Carriers and In Vitro Studies on Their Applications in Inducing Human Hair Growth

“…It is found that the EE of tea seed oil in the NLC-C particles is 96.26 ± 2.26%. Lipophilic drugs result in high EE of NLC because they are highly associated with lipid phase [ 62 ]. The result of this study that shows high quantitative encapsulation of tea seed oil is due to the high lipophilicity of the oil in combination with its low aqueous solubility.…”

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

“…LORA-NLCs were prepared by using hot melt emulsification combined with high-speed stirring and ultrasonication methods (Czajkowska-Kośnik et al, 2021 ), where LORA (10 mg) was combined with solid lipid Compitrol 888 ATO ® and liquid lipids whether (Labrasol ® or Labrafil ® ) a clear and homogeneous oil phase was produced when heated to 85 °C with moderate mixing (Kar et al, 2017 ). The overall amount of solid and liquid lipid inside the blend was 1% (w/v).…”

An Innovative Formulation Based on Nanostructured Lipid Carriers for Imatinib Delivery: Pre-Formulation, Cellular Uptake and Cytotoxicity Studies

“…The preparation of NLCS were performed by using emulsification-sonication methods [10][11][12][13]. Oleic acid and compritol, oleic acid and gelucire derivatives (Gelucire 48/16 and Gelucire 43/01 pellets) were used as the lipid phase.…”