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Preparation and property of doxorubicin magnetic thermosensitive liposomes / 中国药学杂志
Chinese Pharmaceutical Journal ; (24): 1294-1298, 2013.
Article in Chinese | WPRIM | ID: wpr-860293
ABSTRACT

OBJECTIVE:

To optimize the formulation of the doxorubicin magnetic thermosensitive liposomes (DOX-MTSLs) was optimized by orthogonal design and evaluated its property.

METHODS:

DOX-MTSLs were prepared by reverse evaporation combined with (NH4)2 SO4-gradient method. The entrapment efficiency was determined by mini-column centrifugation-RP-HPLC method. The transform temperature was determined by differential scanning caliorimetric (DSC). The particle size and Zeta electric potential were measured by transmission electron microscopy (TEM) and the laser scattering particle size distribution analyzer. The in vitro release behavior of DOX-MTSLs at different temperatures and different time points were studied by dialyzer in constant temperature water and simulated the release regression equation at(41 ±0.5)°C. The heating effect of DOX-MTSLs was determined in the high alternation magnetic field(AMF).

RESULTS:

The optimum recipe of DOX-MTSLs was founded as DOX/DPPC of 120(m/m), DPPC/Chol of 41 (mol/mol), the concentration of magnetic fluid 15 mg · mL-1, pH value of 7.4. The average entrapment efficiency of three batches of DOX-MTSLs(100416,100507,100517 self-preparation) were(82.77 ±0.88) %, (83.03 ±1.38)% and (80.68 ±0.42)% (n=3). The average particle size of doxorubicin magnetic thermosensitive liposomes were 177.1 nm, and the polydispersity index(PDI) was 0.700. When the temperature increased from (25 ± 0.5)°C to (37 ± 0.5)°C, the in vitro drug release was very slow and incomplete (15.45% and 19.54%) even up to 10 h. However, at the phase transition temperature(Tm) 41°C, the in vitro drug release significantly reached 90.99% within 2 h and continued to release. The DOX-MTSLs was showed to be temperature dependent and the in vitro release model was fitting the kinetic equation of Higuchi at(41±0.5)°C. The heating temperature and balanceable temperature of DOX-MTSLs(Fe3O2 3.19 mg · mL-1) were respectively raised to 39.9°C in 10 min and to 56.7°C in 40 min in high frequency induction heating equipment of oscillation frequency 80 kHz and current 12A.

CONCLUSION:

The optimized conditions can be obtained with high entrapment efficiency, good thermosensitivity and perfect magnetic susceptibility to reach the expectation.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Pharmaceutical Journal Year: 2013 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Pharmaceutical Journal Year: 2013 Type: Article