Table 2. Synthesis, Macromolecular Characteristics and Biological Evaluation of Drug–Polyester Prodrug Nanoparticles.
| drug | catalyst | polymer (Mn, kg·mol–1)a | drug loading (wt %)b | biological evaluation(s) | ref |
|---|---|---|---|---|---|
| paclitaxel (Ptx) | (BDI-II)ZnN(TMS)2 | PLA (6.9–27.2)c | 3.0–10.9c | in vitro (targeting) | (51) |
| PLA (2.2–14.4)d | 5.6–28.3d | in vitro (cytotoxicity) | (52) | ||
| PVL (14.2–30.4)c | 2.7–5.7c | (53) | |||
| PCL (19.4)c | 4.2c | (53) | |||
| PTMC (13.8)c | 5.8c | (53) | |||
| (BDI-EI)ZnN(TMS)2 | P(Phe-OCA) (3.7–14.8)d | 5.4–18.7c | (54) | ||
| camptothecin (CPT) | (BDI-EI)ZnN(TMS)2 | PLA (1.4–14.2)d | 2.4–19.5d | in vitro (cytotoxicity) | (56) |
| (BDI-II)ZnN(TMS)2 | PLA (1.4)d | 19.5d | in vitro (cytotoxicity) | (52) | |
| PLA (3.6–14.4)d | 2.4–8.8d | (55) | |||
| (BDI-EI)ZnN(TMS)2 | P(Phe-OCA) (4.0–15.1)c | 2.3–8.1c | in vitro (cytotoxicity), in vivo (biodistribution, pharmacokinetics, toxicity) | (54) | |
| docetaxel (Dtx) | (BDI-II)ZnN(TMS)2 | PLA (1.4)d | 35.9d | in vitro (cytotoxicity) | (52) |
| PLA (1.4–3.6)d | 18.3–35.9d | (55) | |||
| PCL (10.4)c | 7.2c | (53) | |||
| (BDI-EI)ZnN(TMS)2 | P(Phe-OCA) (3.7)d | 16.1c | (54) | ||
| doxorubicin (Dox) | (BDI-II)ZnN(TMS)2 | PLA (1.7–18.3)c | 3.6–27.4d | in vitro (cytotoxicity) | (55) |
| (BDI-EI)ZnN(TMS)2 | P(Phe-OCA) (3.7)d | 10.3c | (54) | ||
| cyclosporin (CsA) | (BDI-II)ZnN(TMS)2 | PLA (15.7)c | 7.1c | in vitro (suppression of T cell proliferation and production of inflammatory cytokines); in vivo (targeting lymph nodes, suppression of T cell proliferation) | (57) |
| cyclopamine (Cpa) | (BDI-II)ZnN(TMS)2 | PLA (7.2–14.4)d | 2.8–5.4d | (55) | |
| goserelin (Gos) | (BDI-II)ZnN(TMS)2 | PLA (1.4–14.4)d | 8.1–46.8d | (55) |
a
Mn of the polymer alone (i.e., without drug).
b
Drug loading of the polymer prodrug conjugate alone (that is before poststabilization, if any).
c
Determined experimentally.
d
Calculated from [monomer]0/[initiator]0. PLA = polylactide, PVL = poly(δ-valerolactone), PCL = poly(ε-caprolactone), PTMC = poly(trimethylene carbonate), P(Phe-OCA) = phenyl O-carboxyanhydride.