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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.


Micelle size and size distribution of propofol-loaded mPEG-PLA/Solutol HS15 mixed micelles.
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Figure 2: Micelle size and size distribution of propofol-loaded mPEG-PLA/Solutol HS15 mixed micelles.

Mentions: Thus, our final optimized preparation of propofol-loaded mixed micelles had a composition as mPEG-PLA/Solutol HS15/propofol of 10/1/5 by weight, average micelle size of about 101 nm and PDI of 0.12 as shown in Figure 2. The LC of mixed micelles was about 32.4%, and the content of propofol in the preparation was approximately 0.3%.


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)

Micelle size and size distribution of propofol-loaded mPEG-PLA/Solutol HS15 mixed micelles.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 2: Micelle size and size distribution of propofol-loaded mPEG-PLA/Solutol HS15 mixed micelles.
Mentions: Thus, our final optimized preparation of propofol-loaded mixed micelles had a composition as mPEG-PLA/Solutol HS15/propofol of 10/1/5 by weight, average micelle size of about 101 nm and PDI of 0.12 as shown in Figure 2. The LC of mixed micelles was about 32.4%, and the content of propofol in the preparation was approximately 0.3%.

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.