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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.


Sleep-recovery study results. The dose was 10 mg/kg (onset of sleep was less than 0.5 min). * p > 0.05 vs. the commercial lipid emulsion (CLE).
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Figure 6: Sleep-recovery study results. The dose was 10 mg/kg (onset of sleep was less than 0.5 min). * p > 0.05 vs. the commercial lipid emulsion (CLE).

Mentions: The mean time values to loss and recovery of righting reflex were evaluated for mixed micelles and the CLE. It was found that animals rapidly lost righting reflex (within 0.5 min of dose administration) following administration of both of propofol formulations (data not shown). The results of recovery of righting reflex were presented in Figure 6. Time for righting reflex recovery was 7.17 ± 2.75 and 7.29 ± 1.25 min, for mixed micelles and CLE, respectively. On average, both groups of animals given propofol formulations recover their righting reflex after 7.2 min. It was concluded that the time for the animals to lose and recover righting reflex was essentially the same for both formulations of propofol (p > 0.05). In addition, no animals sustained any observable toxic effects from use of either propofol-loaded mixed micelles or CLE. Results from this pharmacological paradigm in rats suggested that the mixed micelles had very similar pharmacological effects as CLE. Based on these data, it might be inferred that the difference in propofol release from the two formulations did not significantly affect the partition of the drug to the site of action (e.g., the central nervous system) in rats, hence explaining the similarity in the pharmacological effects observed.


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)

Sleep-recovery study results. The dose was 10 mg/kg (onset of sleep was less than 0.5 min). * p > 0.05 vs. the commercial lipid emulsion (CLE).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 6: Sleep-recovery study results. The dose was 10 mg/kg (onset of sleep was less than 0.5 min). * p > 0.05 vs. the commercial lipid emulsion (CLE).
Mentions: The mean time values to loss and recovery of righting reflex were evaluated for mixed micelles and the CLE. It was found that animals rapidly lost righting reflex (within 0.5 min of dose administration) following administration of both of propofol formulations (data not shown). The results of recovery of righting reflex were presented in Figure 6. Time for righting reflex recovery was 7.17 ± 2.75 and 7.29 ± 1.25 min, for mixed micelles and CLE, respectively. On average, both groups of animals given propofol formulations recover their righting reflex after 7.2 min. It was concluded that the time for the animals to lose and recover righting reflex was essentially the same for both formulations of propofol (p > 0.05). In addition, no animals sustained any observable toxic effects from use of either propofol-loaded mixed micelles or CLE. Results from this pharmacological paradigm in rats suggested that the mixed micelles had very similar pharmacological effects as CLE. Based on these data, it might be inferred that the difference in propofol release from the two formulations did not significantly affect the partition of the drug to the site of action (e.g., the central nervous system) in rats, hence explaining the similarity in the pharmacological effects observed.

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.