Novel Lipid and Preservative-free Propofol Formulation: Properties and Pharmacodynamics

Ravenelle, François; Gori, Sandra; Garrec, Dorothée Le; Lessard, D.; Luo, Lan; Palusova, Dana; Sneyd, J. R.; Smith, Daniel

doi:10.1007/s11095-007-9471-5

Cited by 20 publications

(15 citation statements)

References 30 publications

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“…The model hydrophobic drugs propofol and griseofulvin will be used to determine optimal drug solubilisation parameters. Propofol is the most commonly used intravenous anaesthetic agent in the world owing to its rapid onset, short half-life and minimal side-effect profile [30]. The highly lipophilic nature of the compound (logP 4.16) hinders its formulation as an aqueous-based injection.…”

Section: Introductionmentioning

confidence: 99%

Poly(allylamine) Magnetomicelles for Image Guided Drug Delivery

Barnett¹,

Lees²,

Curtis³

et al. 2013

PNT

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Section: Introductionmentioning

confidence: 99%

Poly(allylamine) Magnetomicelles for Image Guided Drug Delivery

Barnett¹,

Lees²,

Curtis³

et al. 2013

PNT

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“…Therefore, propofol was initially formulated as a 1% solution in 16% Cremophor EL, which has been reported to induce undesirable side effects, such as the high occurrence of pain on injection and the risk of anaphylactic reactions associated to Cremophor EL. In view of the clinical importance of propofol, the alternative formulations such as oil/water emulsion consisting of soya bean oil, glycerol, and egg phosphatide (Diprivan ® , Zeneca, UK) [5], microemulsions [6], inclusion complex [1], and polymeric micelles [7,8], have been developed to improve its solubility. Unfortunately, lipid-based emulsions suffer from other limitations including poor physical stability and the potential for embolism.…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of novel mixed micelles as nanocarriers for intravenous delivery of propofol

Zhang

Fan

et al. 2011

Nanoscale Res Lett

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Novel mixed polymeric micelles formed from biocompatible polymers, poly(ethylene glycol)-poly(lactide) (mPEG-PLA) and polyoxyethylene-660-12-hydroxy stearate (Solutol HS15), were fabricated and used as a nanocarrier for solubilizing poorly soluble anesthetic drug propofol. The solubilization of propofol by the mixed micelles was more efficient than those made of mPEG-PLA alone. Micelles with the optimized composition of mPEG-PLA/Solutol HS15/propofol = 10/1/5 by weight had particle size of about 101 nm with narrow distribution (polydispersity index of about 0.12). Stability analysis of the mixed micelles in bovine serum albumin (BSA) solution indicated that the diblock copolymer mPEG efficiently protected the BSA adsorption on the mixed micelles because the hydrophobic groups of the copolymer were efficiently screened by mPEG, and propofol-loaded mixed micelles were stable upon storage for at least 6 months. The content of free propofol in the aqueous phase for mixed micelles was lower by 74% than that for the commercial lipid emulsion. No significant differences in times to unconsciousness and recovery of righting reflex were observed between mixed micelles and commercial lipid formulation. The pharmacological effect may serve as pharmaceutical nanocarriers with improved solubilization capacity for poorly soluble drugs.

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“…It has been recommended that drug wastage should be included in the total cost [57]. If this was the case, propofol may cost even more, in part, because it is packaged as a preservative-free, single-patient-use agent [58]. Therefore, any opened propofol remaining at the end of surgery would have been wasted.…”

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confidence: 99%

A comparison of total intravenous anaesthesia using propofol with sevoflurane or desflurane in ambulatory surgery: systematic review and meta‐analysis

et al. 2014

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SummaryWith the popularity of ambulatory surgery ever increasing, we carried out a systematic review and meta-analysis to determine whether the type of anaesthesia used had any bearing on patient outcomes. Total intravenous propofol anaesthesia was compared with two of the newer inhalational agents, sevoflurane and desflurane. In total, 18 trials were identified; only trials where nitrous oxide was administered to, or omitted from, both groups were included. A total of 1621 patients were randomly assigned to either propofol (685 patients) or inhalational anaesthesia (936 patients). If surgical causes of unplanned admissions were excluded, there was no difference in unplanned admission to hospital between propofol and inhalational anaesthesia (1.0% vs 2.9%, respectively; p = 0.13). The incidence of postoperative nausea and vomiting was lower with propofol than with inhalational agents (13.8% vs 29.2%, respectively; p < 0.001). However, no difference was noted in post-discharge nausea and vomiting (23.9% vs 20.8%, respectively; p = 0.26). Length of hospital stay was shorter with propofol, but the difference was only 14 min on average. The use of propofol was also more expensive, with a mean (95% CI) difference of £6.72 (£5.13-£8.31 (€8.16 (€6.23À€10.09); $11.29 ($8.62-$13.96))) per patient-anaesthetic episode (p < 0.001). Therefore, based on the published evidence to date, maintenance of anaesthesia using propofol appeared to have no bearing on the incidence of unplanned admission to hospital and was more expensive, but was associated with a decreased incidence of early postoperative nausea and vomiting compared with sevoflurane or desflurane in patients undergoing ambulatory surgery.

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Novel Lipid and Preservative-free Propofol Formulation: Properties and Pharmacodynamics

Abstract: Propofol loaded in PVP-PLA micelles (Propofol-PM) is not significantly different in terms of pharmacodynamic but demonstrates no microorganism growth support and improved stability that opens up the door to pain on injection reduction strategy.

Cited by 20 publications

References 30 publications

Poly(allylamine) Magnetomicelles for Image Guided Drug Delivery

Poly(allylamine) Magnetomicelles for Image Guided Drug Delivery

Preparation and evaluation of novel mixed micelles as nanocarriers for intravenous delivery of propofol

A comparison of total intravenous anaesthesia using propofol with sevoflurane or desflurane in ambulatory surgery: systematic review and meta‐analysis

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