Publish Time: 2021-12-29 Origin: Site
Boc-PEG plays a vital role in our production and life. There are many preparation methods for Boc-PEG, mainly including solvent volatilization, direct dissolution, dialysis, chemical binding, etc. The choice of the Boc-PEG preparation method mainly depends on the water solubility of the polymer. If the water solubility is not good or is not easily soluble in water, consider dissolving in an organic solvent and then using dialysis or solvent volatilization to remove the organic solvent. So what are the preparation methods and characteristics of Boc-PEG? Next, let us take a look.
Here is that the content:
l Solvent volatilization
l Direct dissolution method
l Dialysis
l Chemical conjugation
l Features
Solvent volatilization
This method is simple and effective and is currently the most common method. The principle is to dissolve Boc-PEG in a volatile organic solvent, such as acetone, methanol, tetrahydrofuran, etc., and then add the organic phase to the stirred aqueous phase, and finally volatilize the organic solvent through operating steps such as rotary evaporation. PEG self-assembles to form Boc-PEG micelles due to microphase separation.
Direct dissolution method
The Boc-PEG direct dissolution method is to add Boc-PEG directly to water or neutral buffer to dissolve it. When the solute concentration is higher than CMC, Boc-PEG micelles can be formed, but some copolymers need to be at a higher temperature Dispersion can ensure that the micellization of Boc-PEG is more Hua Ci.
Dialysis
The Boc-PEG dialysis method is to dissolve the copolymer in a water-miscible organic solvent (such as tetrahydrofuran, dimethyl sulfoxide), then put the mixture into a dialysis bag, and gradually form a Boc-PEG micellar solution through the solvent exchange.
Chemical conjugation
The chemical binding method is that under certain conditions, the drug molecule can chemically react with the specific group in the block copolymer to connect the drug to the hydrophobic or hydrophilic segment and then use physical methods to prepare Boc-PEG micelles. This method requires proper conditions to proceed, and the chemical reaction must not affect the activity of the drug itself.
Features
1. Boc-PEG can keep the drug at a high concentration for a long time during the circulation process in the body, and at the same time, it can avoid the recognition and swallowing of macrophages in the body, reduce the loss of the drug, and reduce the toxic side effects of the drug on normal tissues.
2. The self-assembly process of Boc-PEG amphiphilic block copolymer micelles is simple, fast, and easy to manipulate. Generally, micelles can be formed in water for easy storage.
3. Possess good thermodynamic and kinetic stability. The CMC value of Boc-PEG micelles is generally low, and Boc-PEG micelles can still exist stably even if they are diluted by a large number of body fluids in the body.
4. The surface modification of Boc-PEG micelles can be used to achieve active targeting of the lesion. At the same time, the hydrophobic core of Boc-PEG micelles has a good solubilization effect, which increases the loading capacity of hydrophobic drugs, thereby greatly increasing the effect.
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