PH sensitivity modified liposome and its preparation method
A liposome and sensitive technology, which is applied in liposome delivery, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of long process time and unfavorable practical application, and achieve high preparation efficiency, save preparation time, and particle size evenly distributed effect
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Embodiment 1
[0047] Accurately weigh 48mg of lecithin and 12mg of cholesterol, and add 2.5ml of ether to fully dissolve. Inject 1 ml of 12 mg / ml cytarabine aqueous solution. Ultrasonic for 2min to form a W / O emulsion. Add modifier—2.5% polyaspartic acid aqueous solution with a mass fraction of pH 8.8, shake well, place in a rotary evaporator (RE-52AA, Shanghai Yarong Biochemical Instrument Factory) at 0.02MPa, 25°C for 30min have to. Use a transmission electron microscope (JEM-3010 high-resolution transmission electron microscope, Japan Electronics Co., Ltd.) to analyze the surface structure of pH-sensitive modified liposome particles. The results are shown in figure 1 . The average particle size of polyaspartic acid modified cytarabine liposomes measured by laser particle size analyzer (Mastersizer2000 type, Malvern, UK) is 183nm, see figure 2 .
Embodiment 2
[0049] Accurately weigh 48mg of lecithin and 12mg of cholesterol, and add 2.5ml of ether to fully dissolve. Inject 1 ml of 12 mg / ml cytarabine aqueous solution. Ultrasonic for 2min to form a W / O emulsion. Add the external water phase—an octylamine-grafted polyaspartic acid aqueous solution with a mass fraction of 2.5% and a grafting rate of 8% at pH 8.8, shake well, place in a rotary evaporator at 0.02 MPa, and rotate at 25°C for 30 minutes under reduced pressure. have to. The average particle diameter of octylamine-grafted polyaspartic acid-modified cytarabine liposomes measured by the same method as in Example 1 was 332 nm.
[0050] Comparing the results of Example 1 and Example 2, it can be found that the modifier-octylamine grafted polyaspartic acid with a hydrophobic fatty segment can be used to obtain liposomes with a larger particle size, because the hydrophobic segment The presence of the modifier increases the affinity of the hydrophobic segment of the phospholipid...
Embodiment 3
[0051] Prepare the cytarabine liposomes modified by the octylamine grafted polyaspartic acid of grafting rate 8% by the method of embodiment 1, and measure pH sensitive modified liposome at pH5.0 and pH7.4 Drug release profile in media. The drug release was determined by reverse dialysis method. The specific process was to prepare phosphate buffer solution with pH5.0 and pH7.4, measure 200ml of buffer solution as the external solution, and place 10ml of the same solution in a dialysis bag with a molecular weight cut-off of 3500 (D6066-25EA, Sigma) as the inner liquid, take 2ml of the newly prepared liposome emulsion in the outer liquid, take 2ml of the inner liquid at regular intervals, place it in a full-wavelength microplate reader to measure the absorbance, and convert it to the concentration according to the standard curve Calculate leakage. The pH-sensitive liposome drug release profile is obtained, such as image 3 shown.
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