Homopolymer electrolyte composite vesicle, preparation method thereof, antibacterial vesicle, vesicle entrapped with hydrophobic substance and anti-adhesion vesicle
A technology of hydrophobic substances and polyelectrolytes, which is applied in the direction of active ingredients of nitro compounds, drug combinations, antineoplastic drugs, etc., and can solve the problems of complex synthesis methods and high costs of block copolymers
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[0073] The present invention also provides a method for preparing homopolyelectrolyte complex vesicles described in the above scheme, comprising the following steps:
[0074] Self-assembling the aggregation peptides containing amine groups in the side chains and the aggregation peptides containing carboxyl groups in the side chains in water to obtain the aqueous solution of the homopolyelectrolyte complex vesicles.
[0075] In the present invention, the preparation method of the amine group-containing clustered peptide in the side chain preferably includes the following steps:
[0076] Under the condition of ultraviolet light, poly(N-substituted glycine), mercaptoethylamine and photoinitiator are mixed to carry out click chemical reaction to obtain a side chain-containing amine-containing clustered peptide; the poly(N-substituted glycine) is poly( N-allylglycine) (PNAG) or poly(N-propargylglycine) (PNPG).
[0077] In the present invention, the preparation method of poly(N-sub...
Embodiment 1
[0150] The preparation of the clustering peptide containing amine groups in the side chain, the specific structural formula is as shown in formula I-1:
[0151]
[0152] (1) Add glyoxylic acid aqueous solution (150g, 1mol, mass fraction 50%) in the flask, then add 500mL dichloromethane, in ice bath, add allylamine (44.5mL, 0.5mol) while stirring, react for 24h , remove the solvent dichloromethane with a rotary evaporator, then add 500mL of 2mol / L hydrochloric acid, reflux at 110°C for 20h, remove water with a rotary evaporator, and place in methanol:tetrahydrofuran=1:10 in a refrigerator at -20°C. Crystallized three times, then filtered, and dried in vacuo to give white crystals of N-allyl-substituted glycine hydrochloride.
[0153] (2) Dissolve N-allyl substituted glycine hydrochloride (15.1g, 0.1mol) in 200mL deionized water in a round bottom flask, add Boc 2 O (76.35g, 0.2mol), triethylamine (45.3g, 0.448mol), stirred at room temperature for 24h, and extracted with n-he...
Embodiment 2
[0159] The preparation of the clustering peptide containing amine groups in the side chain, the specific structural formula is as shown in formula I-2:
[0160]
[0161] Steps (1)~(3) are identical with embodiment 1, and step (4) is as follows:
[0162] Weigh 1.41g (10mmol) N-allyl-NCA from the glove box into a polymerization tube, then add 15mL of anhydrous THF to the bottle, preheat in an oil bath at 55°C, and then add the prepared benzylamine initiator (Dissolve benzylamine in anhydrous THF), add 644.67 μL (0.05 mmol, mass fraction: 7.47%) of benzylamine solution to the polymerization tube, react for 48 hours, settle in glacial ether after the reaction, and centrifuge and dry to obtain white solid PNAG , The number average molecular weight measured by gel permeation chromatography is 2900g / L, the molecular weight distribution is 1.29, and the number average degree of polymerization is 32.
[0163] Step (5) is identical with embodiment 1, obtains the polymkeric substance...
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