Self-Assembled Nanoparticles Platform Based on Pectin-Dihydroartemisinin Conjugates for Codelivery of Anticancer Drugs.

Natural pectin is an important carrier for delivering drugs in biomedical research, however, there are only a few reports on the preparation of pectin nanoparticles, especially a particle size of below 100 nm with high yield. Here we design pectin-dihydroartemisinin/hydrooxycampothecin nanoparticles (PDC-H NPs) through a self-assembly method. The prepared PDC-H NPs contained hydrophilic part of pectin and hydrophobic anticancer drugs of dihydroartemisinin and hydroxycamptothecin, which could increase drug loading, improve water solubility, and achieve controlled release of drugs. The results indicated that the particle size of PDC-H NPs was about 70 nm, drug-loaded efficiency of DHA was 20.33 wt %, and encapsulation efficiency of HCPT was 14.11 wt %. PDC-H NPs exhibited a higher cytotoxicity, the blood retention time of PDC-H NPs was 4.8-fold longer than DHA and was 6.8-fold longer than HCPT. In addition, effective cellular uptake exhibited an obvious synergistic effect compared with DHA and HCPT. 4T1 tumor-bearing mice also showed a higher survival rate than free DHA and free HCPT. The result show that the self-assembled PDC-H NPs is a promising anticancer drug for codelivery.