Polymer microparticle for carrying physiologically active substance and method for preparing same
A technology of physiologically active substances and polymers, which is applied in the field of polymer microparticles loaded with physiologically active substances and its preparation, and can solve the problems of quantitative modification of difficult blocking agents, increased batch-to-batch differences, and cumbersome problems
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Embodiment 1
[0101] "Example 1: Synthesis of emulsifier (amphiphilic block copolymer)"
[0102] In the present embodiment, according to the reaction process formula shown below, the synthetic emulsifier (amphiphilic block polymer: PSt 21 -b-POEGMA 41 -Cl), synthesized by Gabriel primary amine (Gabriel) to synthesize ω-terminally aminated amphiphilic block copolymer PSt 21 -b-POEGMA 41 -NH 2 .
[0103] [chemical formula 4]
[0104]
[0105] Under a nitrogen atmosphere, to 10 g of styrene (Kanto Chemical Co., Inc.) and 1 g of hydroxyethanol bromoisobutyrate (HEBiB) (2-hydroxyethyl-2-bro moisobutyrate) as an initiator, 2 g The 2,2'-bipyridine (bipyridine; bpy) and 0.6g of Cu Br were polymerized at 110°C. In addition, HEBiB synthesized by 2-bromoisobutyryl bromide (2-bromoisobutyryl bromide) and ethylene glycol was used. After the polymerization is complete, use tetrahydrofuran (THF) to dilute and reprecipitate in methanol to obtain PSt 21 -Br.
[0106] 7.0 g of oligo(ethylene glyc...
Embodiment 2
[0110] "Example 2: Synthesis of latex particles using emulsifiers"
[0111] With the PSt of 0.05g obtained in embodiment 1 21 -b-POEGMA 41 -NH 2 It was dissolved in 0.1 g of styrene, and further, 1.2 g of ultrapure water was added. The mixture was heated up to 90° C. and stirred for 10 minutes to obtain a W / O type emulsion.
[0112] Then, stirring was carried out while cooling in an ice bath, and a phase inversion emulsification operation was performed to obtain an O / W type emulsion. 0.03 g of a water-soluble initiator (VA-044: Wako Pure Chemical Industries, Ltd.) was added, and polymerization was performed at 40° C. for 6 hours.
[0113] The particle diameter of the obtained latex particles was measured using a dynamic light scattering device (DLS: ELSZ-1000ZSCK light scattering apparatus tus Otsuka), and it was 52±20 nm.
Embodiment 3
[0114] "Example 3: The influence of the chain length of the hydrophobic segment of the emulsifier on the particle size"
[0115] According to Example 1, the repeating unit (equivalent to n of general formula (1)) having polystyrene 13, 21, 46, 95 on the hydrophobic segment and having 42 in the main chain of the hydrophilic segment , 41, 45, and 36 repeating units (corresponding to m in the general formula (1)) are amphiphilic block polymers shown in Table 1. In addition, OEGMA (polymerization degree: 9) was used for the graft part. By setting the molar ratio (M / I ratio) of the monomer (styrene) / initiator (HEBiB) to the value shown in Table 1, the repeating unit of the hydrophobic segment was controlled. By making the molar ratio of monomer (OEGMA) / initiator (PSt-Br) uniform to 50, control of the repeating unit of the hydrophilic segment was performed.
[0116] Then, according to embodiment 2, synthesize the latex particle of the combination described in table 1, promptly syn...
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