The invention discloses a
drug loading and
controlled release regulation method of PEGMA-b-PCL
polymer drug-loaded micelles, relates to the technical field of
drug carriers, and comprises two parts of drug loading regulation and drug
controlled release regulation. According to
load regulation and control, PEGMA-b-PCL serves as a carrier, parameters such as the block proportion and the number-average molecular weight of the PEGMA-b-PCL are precisely regulated and controlled, an improved
solvent volatilization-ultrasonic synergistic method is adopted,
raw material pretreatment is combined, efficient
medicine loading is achieved, the encapsulation efficiency is larger than or equal to 85%, and the
medicine loading capacity is larger than or equal to 28%. A pH response and
enzymatic degradation double-
synergistic mechanism is constructed through
controlled release regulation, 0.5-2.0 wt% of a pH
response type cross-linking agent and 0.3-1.2 wt% of an
esterase sensitive
regulator are added, cross-linking
reaction conditions are optimized, and it is achieved that within 48 h
drug release in a normal physiological environment is smaller than or equal to 12%, within 48 h
drug release in a
tumor microenvironment is larger than or equal to 80%, and within 72 h, within 72 h, within 48 h
drug release is larger than or equal to 92%. The particle size of the prepared
micelle is 80-150nm, the particle
size change rate is less than or equal to 8% after the
micelle is sealed and stored at 4 DEG C for 6 months, the drug
leakage rate is less than or equal to 5%, the process is controllable, the stability is good, and the
micelle has good industrial amplification and clinical application prospects.