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

Li X, Zhang Y, Fan Y, Zhou Y, Wang X, Fan C, Liu Y, Zhang Q - Nanoscale Res Lett (2011)

Bottom Line: 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.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Haidian District, Beijing 100191, People's Republic of China. yanliu@bjmu.edu.cn.

ABSTRACT
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.

No MeSH data available.


Release profile of propofol from mixed micelles, the commercial lipid emulsion (CLE) and 30% w/w alcohol solution at 37°C.
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Figure 5: Release profile of propofol from mixed micelles, the commercial lipid emulsion (CLE) and 30% w/w alcohol solution at 37°C.

Mentions: When developing intravenous colloidal delivery systems for highly hydrophobic drugs such as propofol, it is important to adequately control the release rate in order to avoid precipitation upon dilution in blood. The in vitro release of propofol from mixed micelles was, therefore, investigated. Prior to conducting this release assay, it was verified that propofol could freely diffuse through the dialysis membrane (Milipore Co. Ltd, USA) when the molecular weight cut-off of the membrane was 3 kD (Figure 5). Moreover, the sink condition was respected by addition of 30% (v/v) ethanol in the release medium. More importantly, no significant change in micelle size upon incubation of the micelle sample with release medium at 37°C with time from 0 to 24 h was observed (data not shown), indicating that the integrity of propofol-loaded mixed micelles was not affected by the release medium upon 24 h long co-incubation.


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

Li X, Zhang Y, Fan Y, Zhou Y, Wang X, Fan C, Liu Y, Zhang Q - Nanoscale Res Lett (2011)

Release profile of propofol from mixed micelles, the commercial lipid emulsion (CLE) and 30% w/w alcohol solution at 37°C.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3211339&req=5

Figure 5: Release profile of propofol from mixed micelles, the commercial lipid emulsion (CLE) and 30% w/w alcohol solution at 37°C.
Mentions: When developing intravenous colloidal delivery systems for highly hydrophobic drugs such as propofol, it is important to adequately control the release rate in order to avoid precipitation upon dilution in blood. The in vitro release of propofol from mixed micelles was, therefore, investigated. Prior to conducting this release assay, it was verified that propofol could freely diffuse through the dialysis membrane (Milipore Co. Ltd, USA) when the molecular weight cut-off of the membrane was 3 kD (Figure 5). Moreover, the sink condition was respected by addition of 30% (v/v) ethanol in the release medium. More importantly, no significant change in micelle size upon incubation of the micelle sample with release medium at 37°C with time from 0 to 24 h was observed (data not shown), indicating that the integrity of propofol-loaded mixed micelles was not affected by the release medium upon 24 h long co-incubation.

Bottom Line: 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.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Haidian District, Beijing 100191, People's Republic of China. yanliu@bjmu.edu.cn.

ABSTRACT
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.

No MeSH data available.