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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.


Changes in particle size and encapsulation efficiency (EE) of propofol-loaded mixed micelles in 0.2% BSA solution at 37 °C at different dilution extent (n = 3).
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Figure 4: Changes in particle size and encapsulation efficiency (EE) of propofol-loaded mixed micelles in 0.2% BSA solution at 37 °C at different dilution extent (n = 3).

Mentions: A basic evaluation of pharmacokinetic modeling and efficacy data for micelles or drug loaded micelles in animal models was conducted, testing the stability of drug loaded micelles in the presence of serum or serum albumins [41]. As shown in Figure 4, the ratio (di/d0) of mixed micelles did not change significantly at different dilution extent within 24 h, indicating that mPEG efficiently protected the BSA adsorption, which resulted from the hydrophobical interaction of the hydrophobic groups with BSA, on the mixed micelles because the hydrophobic groups of the copolymer were efficiently screened by mPEG [42].


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)

Changes in particle size and encapsulation efficiency (EE) of propofol-loaded mixed micelles in 0.2% BSA solution at 37 °C at different dilution extent (n = 3).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 4: Changes in particle size and encapsulation efficiency (EE) of propofol-loaded mixed micelles in 0.2% BSA solution at 37 °C at different dilution extent (n = 3).
Mentions: A basic evaluation of pharmacokinetic modeling and efficacy data for micelles or drug loaded micelles in animal models was conducted, testing the stability of drug loaded micelles in the presence of serum or serum albumins [41]. As shown in Figure 4, the ratio (di/d0) of mixed micelles did not change significantly at different dilution extent within 24 h, indicating that mPEG efficiently protected the BSA adsorption, which resulted from the hydrophobical interaction of the hydrophobic groups with BSA, on the mixed micelles because the hydrophobic groups of the copolymer were efficiently screened by mPEG [42].

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.