P3.02c-002 Mannosylated Poly (Propylene Imine) Dendrimer Mediated Lung Delivery of Anticancer Bioactive

Abstract

on day 1 of a 21-day cycle. The primary end point is the percentage of patients who experience doselimiting toxicity (DLT) between administration of the first dose of SASP (day 1) and day 21. Results: From April 2015 to January 2016, 15 patients were enrolled in the study (mean age, 64 years; age range, 42e74 years; male/female ratio, 10/5; ECOG performance status 0/1 ratio, 6/9). Immunohistochemical staining of tumor biopsy specimens revealed that the proportion of CD44v-positive cells was >10% in 9 patients before SASP treatment. No DLT was observed in the first three patients treated at SASP dose level 1 (500 mg TID) or those treated at dose level 2 (1000 mg TID). At dose level 3 (1500 mg TID), two of three patients experienced a DLT (anorexia of grade 3). We enrolled additional patients at dose level 2 and two of the total of five patients treated at this dose level experienced DLTs (hypotension or pneumonitis, each of grade 3). To confirm the safety of dose level 1, we enrolled additional patients at this dose level and one of the total of six patients treated at this dose level experienced DLTs (AST and ALT elevation, each of grade 3). Exposure of SASP following oral administration varied markedly among individuals according to ABCG2 and NAT2 genotypes as previously reported. Conclusion: SASP 500 mg TID was the recommended dose when administered with CDDP plus PEM.

Application of Dendrimers in Anticancer Diagnostics and Therapy

“…The potential of using poly (propylene-imine) dendrimers (PPI) as a vehicle for the docetaxel (DTX) targeting of MCF-7 breast cancer was assessed by Thakur [ 61 ]. The synthesis of PPI dendrimers with the drug gemcitabine has also been used in the targeted therapy of A549 lung cancer cells [ 62 ]. PPI dendrimers have been used to increase paclitaxel (PTX) delivery to the brain [ 63 ].…”