Preparation and release properties of 3-methyladenine mesoporous silica
Objective To prepare polydopamine(PDA)coated mesoporous silica nanoparticles(MSN)nanoparticles modified with zoledronic acid(ZOL),and to determine their characterization and drug release properties.Methods ZOL was connected with amino-pegyl-sulfhydryl group as the bone targeting ligand and modified on PDA-coated MSN surface by addition reaction to obtain MSN@PDA-PEG-ZOL,which was characterized by 1H-NMR,FT-IR,TEM,particle size and Zeta potential.Autophagy inhibitor 3-methyladenine(3-MA)was used as a drug model.Different drug concentrations were designed to calculate the drug loading and encapsulation rate,and screen the optimal prescription.The drug release of in different environments was determined.Results The prepared nanoparticles had uniform spherical structure.The particle size was(229.1±8.8)nm and the Zeta potential was-(30.3±0.6)mV.When the drug loading concentration was 1000 µg·mL-1,the encapsulation rate was(90.87±0.05)%and the drug loading was(37.55±0.02)%.The drug release rate of nanoparticles was(16.99±0.15)%in PBS solution(pH 7.4)and(65.11±1.64)%in PBS solution(pH 5.0)within 48 h,which was more conducive to drug release in tumor microenvironment.Conclusion Nanometer preparations loaded with 3-MA with targeting and pH response are successfully prepared,with good dispersion,high drug loading and encapsulation rate,etc.,laying the foundation for further research.
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