RESUMO
Antibody drug conjugates (ADCs) are an emerging class of targeted therapeutics with the potential to improve therapeutic index over the traditional chemotherapy. However, it is difficult to control the site and stoichiometry of conjugation in mAb, typically resulting in heterogeneous mixtures of ADCs that are difficult to optimize. New methods for site-specific drug attachment allow development of more homogeneous conjugates and control of the site of drug attachment. In this article, the new literature on development of ADCs and site-specific ADCs is reviewed. In addition, we summarized the various strategies in production of site-specific ADCs.
RESUMO
OBJECTIVE:To prepare core-shell nanocapsules loading nicardipine hydrochloride and to investigate its pharmaceutical characteristics. METHODS: Core-shell nanocapsules were prepared using layer-by-layer electrostatic self-assembly technique. The indexes including the shape and particle size and the loaded drug amount of the nanocapsules were evaluated, and its accumulative release rates in artificial gastric juice and intestinal juice were computed and compared with those of its crude drug. RESULTS: The results showed that the nanocapsules were spherical with a mean particle size of 200 nm and a maximum loaded drug amount of 2.512%. The drug release rate within 12 h reached 18.64% in artificial gastric juice and 70% in artificial intestinal juice, whereas within 3 h the drug release rate of its crude drug in artificial intestinal juice reached 87%. CONCLUSIONS: The prepared core-shell nanocapsules containing nicardipine hydrochloride had a good pharmaceutical property.