A kind of paclitaxel liposome and its preparation method and application
A liposome and paclitaxel technology, applied in the field of paclitaxel liposome and its preparation, can solve problems such as uneven particle size distribution of liposomes, improve the problem of unstable storage for a long time, reduce the probability of collision and precipitation, and reduce the distribution of narrow effect
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Embodiment 1
[0084] Example 1 Preparation of very small liposomes of monophospholipid components (the molar ratio of guest molecule to host molecule is 1:5)
[0085] Dissolve 0.01 g of 1-stearoyl-2-oleoyl lecithin (chemical name 1-stearoyl-2-oleoyl-sn-glyceryl-3-phosphocholine, SOPC, molecular weight 788) with 25 ml of chloroform , into a 100 ml round bottom flask, and evaporate the solvent to dryness under reduced pressure. Add 50 mL of phosphate-buffered saline solution containing 1 mmol / L n-dodecyl-β-D-maltoside (nonionic surfactant) to the round bottom flask, pH 7.4. SOPC was completely dissolved in the nonionic surfactant phosphate buffered saline by shaking the round bottom flask. 0.33 g of γ-cyclodextrin (molecular weight 1297) was dissolved in 50 ml of water at room temperature (25° C.) to obtain a 5 mmol / L aqueous solution of γ-cyclodextrin. The SOPC solution was added to the aqueous γ-cyclodextrin solution and mixed under vigorous stirring for 15 minutes. In this way, the SOPC...
Embodiment 2
[0088] Example 2 Preparation of paclitaxel-loaded microliposomes using nonionic surfactants (the molar ratio of guest molecule to host molecule is 1:2)
[0089] Dissolve 0.16 g of 1-stearoyl-2-oleoyl lecithin with 50 ml of chloroform, put it into a 250 ml round-bottomed flask, add 10 ml of methanol-chloroform containing 1 mg of paclitaxel (molecular weight 854) (volume ratio: 1:1) solution, the solvent was evaporated to dryness under reduced pressure. Into the round bottom flask was added 100 ml of pH 7.4 phosphate buffered saline solution containing 8 mmol / L of n-dodecyl-β-D-maltoside (non-ionic surfactant). SOPC and paclitaxel were completely dissolved in the nonionic surfactant phosphate buffered saline by shaking the round bottom flask or applying magnetic stirring. 2.10 g of γ-cyclodextrin were dissolved in 100 ml of room temperature (25° C.) water. The obtained mixed solution of SOPC and paclitaxel was mixed with this 100 ml aqueous saturated solution of γ-cyclodextrin...
Embodiment 3
[0090] Example 3 Preparation of paclitaxel-loaded very small liposomes using amphoteric surfactants
[0091] Dissolve 0.01 gram of 1-stearoyl-2-oleoyl lecithin (SOPC, molecular weight 788) with 25 milliliters of chloroform, put it into a 100 milliliter round bottom flask, add 5 milliliters of methanol-chloroform containing 0.5 milligrams of paclitaxel (vol. The ratio was 1:1), and the solvent was evaporated to dryness under reduced pressure. Add 50 mL of 1 mmol / L to the round bottom flask LO (Lauryl Dimethylamine Oxide) (amphoteric surfactant) in Phosphate Buffered Saline, pH 7.4. SOPC and paclitaxel were completely dissolved by shaking the round bottom flask. 0.10 g of α-cyclodextrin was dissolved in 50 ml of water at room temperature. The resulting mixed solution of SOPC and paclitaxel was added to the aqueous α-cyclodextrin solution, and mixed for 15 minutes under vigorous stirring. Thus, a paclitaxel-loaded liposome solution was prepared. The particle size distributi...
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