Nanostructured Lipid Carrier of Propofol: a Promising Alternative to Marketed Soybean Oil–Based Nanoemulsion

Abstract

Nanostructured lipid carrier (NLC) of propofol was formulated using hot emulsification-probe sonication method for improvising its parenteral delivery by reducing pain on injection and risk of microbial contamination. The formulated NLC was optimized using central composite design and evaluated for particle size, zeta potential, morphology, free propofol concentration, hemocompatibility, stability, pain on injection, in vivo anesthetic activity, pharmacokinetics, and antimicrobial effectiveness in comparison to the marketed formulation. Optimized NLCs exhibited globule size, less than 200 nm, and zeta potential − 24.1 mV, indicating its stability. TEM images confirmed the spherical shape and nanosize (200 nm) of optimized NLCs. Free propofol concentration was also found to be 40% lesser than marketed formulation. Optimized NLC was found to be non-hemolytic. Rat paw-lick study showed that propofol NLC was significantly less painful compared to the marketed formulation. Anesthetic potential and pharmacokinetics of optimized NLCs were found to be similar to that of the marketed formulation. NLC was found stable in long-term storage under room temperature. Antimicrobial effectiveness study showed that propofol NLC suppressed microbial growth to a greater extent as compared to the marketed formulation. Hence, the developed propofol NLCs appeared to be clinically useful as a potential carrier for propofol delivery.

Ezetimibe-Loaded Nanostructured Lipid Carrier for Oral Delivery: Response Surface Methodology; In Vitro Characterization and Assessing the Antihyperlipidemic Effect in Rats

“…It was observed that the particle size of EZ-NLC formulations ranged from 160.95 ± 19.31 to 506.7 ± 11.29 nm. Generally, the incorporation of two emulsifiers (tween 80 and poloxamer 188) with different HLB values played an important role in varying the particle size of different EZ-NLC formulations . Tween 80 was chosen from a range of surfactants owing to its regulatory approval and ability to effectively prepare a variety of NLCs.…”

Nanotherapeutics for Alleviating Anesthesia‐Associated Complications

“…[11,90] To tackle these challenges, numerous innovative nano-formulations have been developed to enhance the efficacy and safety of propofol, while avoiding the use of soybean oil and disodium edetate. [11,90,91] For example, Shevalkar et al devised a nanostructured lipid carrier (NLC) of propofol using the hot emulsification-probe sonication method and refined the combinations of solid lipids, oils and surfactants. This optimized NLC formulation not only reduced the content of free propofol in the aqueous phase by 40%, thereby alleviating injection pain compared to Diprivan, but also exhibited other favorable attributes such as non-hemolysis, comparable pharmacokinetics, reduced risk of hyperlipidemia, improved long-term storage stability, and antimicrobial properties.…”

“…To achieve the necessary concentration for effectiveness, current commercially available etomidate formulations utilize either lipid emulsion (e.g., Etomidate-Lipuro) or propylene glycol (e.g., Amidate) as solubilizing agents. [11] However, these solubilizing agents have been associated with various adverse events, including propylene [83] Copyright 2022, Chu et al, open access. b) Selfassembling APK peptides form antibacterial nanofiber that can be used as a safe nano-formulation for etomidate.…”

Relationship and improvement strategies between drug nanocarrier characteristics and hemocompatibility: What can we learn from the literature

“… Propofol Haemolysis The degree of hemolysis is within an acceptable range. [98] Stearic acid Hot melt homogenization method p.o. Simvastatin Haemolysis Treatment of rats with SV preparations will weaken the hemolysis of RBCs, and SV can reverse hyperlipidemia and cause changes in RBCs membrane fluidity.…”