Preparing method of drug-loaded liposome
A technology of liposomes and blank liposomes, which is applied in the direction of liposome delivery, can solve the problems of high encapsulation efficiency drug loading and low encapsulation efficiency drug loading, so as to improve drug loading and increase The encapsulation efficiency of liposomes for most drugs and the effect of a wide range of drug loading
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Embodiment 1
[0025] Example 1 Negatively charged PEGylated liposomes loaded with non-dissociated drug curcumin
[0026] Use 0.9% NaCl aqueous solution (adjust pH=9 with hydrochloric acid) as the water phase, use SPC / DPPG / DPPE-PEG2000 (12:2:1, molar ratio) as the film-forming material, and adopt film dispersion-hydration-extrusion method Prepare blank liposomes (total lipid concentration is 10%), then add curcumin, drug / phospholipid (1:5, w / w), heat up to 50°C and stir (300rpm) for 5h, cool and control the temperature at 2°C , continue stirring for 3h; repeat the high temperature-low temperature cycle operation 0, 1, 3 times to obtain curcumin liposomes.
[0027] Before and after drug loading, the average particle diameter detected by DLS was 150nm, PDI=0.30, ζ=8mV. Remove free drug with Sephadex G50 chromatographic column, detect content by HLPC, cycle high temperature-low temperature operation 0, 1, 3 times, encapsulation efficiency is respectively 20%, 37%, 53%; drug loading (drug / lipid...
Embodiment 2
[0028] Example 2 Neutral PEGylated liposome-loaded amphoteric drug topotecan hydrochloride
[0029] With pH 7.4 phosphate buffer as the aqueous phase and DSPC / CHO / DPPE-PEG2000 (12:7:1, molar ratio) as the membrane material, blank liposomes were prepared by ethanol injection (the total lipid concentration was 2 %), then add topotecan hydrochloride, drug / phospholipid (1:10, w / w), heat up to 70°C and stir (20rpm) for 0.5h, cool and control the temperature at 4°C, continue stirring for 1h; repeat high temperature- The low-temperature cycle operation was performed 3, 5, and 7 times to obtain topotecan hydrochloride liposomes.
[0030] Before and after drug loading, the average particle diameter detected by DLS was 120 nanometers, PDI=0.21, ζ=2mV. Sephadex G50 chromatographic column was used to remove free drug, HLPC detected the content, cycled high temperature-low temperature operation for 3, 5, and 7 times, the encapsulation efficiency was 52%, 85%, and 97% respectively; the dru...
Embodiment 3
[0031] Example 3 Positively charged PEGylated liposomes loaded with baicalein
[0032] With pH 2.5 phosphate buffer as the aqueous phase and DSPC / DPPE-PEG2000 / DOTAP (15:5:1, moleratio) as the membrane material, blank liposomes (liposomes) were prepared by film dispersion-hydration-ultrasonic The concentration is 5%), then add baicalein, drug / phospholipid (1:20, w / w), heat up to 80°C and stir (80rpm) for 2h, cool and control the temperature at 10°C, continue stirring for 4h; repeat high temperature- Low-temperature cycle operation was performed 5, 7, and 9 times to obtain baicalein liposomes respectively.
[0033] Before and after drug loading, the average particle size detected by DLS was 120 nanometers, PDI was about 0.21, ζ=39mV, free drug was removed by Sephadex G50 chromatographic column, content was detected by HLPC, cycle high temperature-low temperature operation 5, 7, 9 Times, encapsulation efficiency were 41%, 59%, 76%; drug loading were 2.1%, 2.95%, 3.8%. It shows ...
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