PMID- 26608536 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20151215 LR - 20200930 IS - 1931-7573 (Print) IS - 1556-276X (Electronic) IS - 1556-276X (Linking) VI - 10 IP - 1 DP - 2015 Dec TI - Enhanced Antiproliferative Effect of Carboplatin in Cervical Cancer Cells Utilizing Folate-Grafted Polymeric Nanoparticles. PG - 453 LID - 10.1186/s11671-015-1162-2 [doi] LID - 453 AB - Carboplatin (CRB) possesses superior anticancer effect in cervical cancer cells with lower incidence of side effects compared to that of cisplatin. However, CRB suffers from severe side effects due to undesirable tissue distributions which contribute to the low therapeutic efficacy. Here, we report a unique folic acid-conjugated chitosan-coated poly(D-L-lactideco-glycolide) (PLGA) nanoparticles (FPCC) prepared for the selective delivery of carboplatin to the cervical cancer cells. The particles were nanosized and spherical shaped with size less than <200 nm. The presence of protective chitosan layer controlled the overall release rate of CRB from chitosan-coated PLGA nanoparticles (PCC) and FPCC. FPCC displayed a higher cellular uptake capacity in HeLa cells than compared to non-targeted nanoparticles. Selective uptake of FPCC was due to an interaction of folic acid (FA) with the folate receptors alpha (FRs-alpha) which is overexpressed on the HeLa and promoted active targeting. These results indicated that FPCC had a specific affinity for the cancerous, HeLa cells owing to ligand-receptor (FA-FR-alpha) recognition. Consistently, FPCC showed superior cytotoxic effect than any other formulations. The IC50 (concentration of the drug required to kill 50 % of the cells) value of FPCC was 0.65 mug/ml while it was 1.08, 1.56, and 2.35 mug/ml for PCC, PLGA NP, and free CRB, respectively. Consistent with the cytotoxicity assay, FPCC induced higher fraction of early as well as late apoptosis cells. Especially, FPCC induced nearly 45 % of early apoptosis cells and more than 35 % in late apoptosis. Therefore, we propose that folate-conjugated nanoparticles might have potential applications in cervical cancer therapy. FAU - Ji, Jing AU - Ji J AD - Department of Gynecology & Obstetrics, The First Affiliated Hospital of Xi'An, Jiaotong University, No. 277, Yanta Xi Road, Xian, Shanxi, 710061, China. FAU - Zuo, Ping AU - Zuo P AD - Department of Gynecology & Obstetrics, The First Affiliated Hospital of Xi'An, Jiaotong University, No. 277, Yanta Xi Road, Xian, Shanxi, 710061, China. FAU - Wang, Yue-Ling AU - Wang YL AD - Department of Gynecology & Obstetrics, The First Affiliated Hospital of Xi'An, Jiaotong University, No. 277, Yanta Xi Road, Xian, Shanxi, 710061, China. wangyuelingwyl@hotmail.com. LA - eng PT - Journal Article DEP - 20151125 PL - United States TA - Nanoscale Res Lett JT - Nanoscale research letters JID - 101279750 PMC - PMC4659799 OTO - NOTNLM OT - Apoptosis OT - Cervical cancers OT - Chitosan OT - Folate OT - PLGA nanoparticles OT - Targeting EDAT- 2015/11/27 06:00 MHDA- 2015/11/27 06:01 PMCR- 2015/11/25 CRDT- 2015/11/27 06:00 PHST- 2015/07/29 00:00 [received] PHST- 2015/11/15 00:00 [accepted] PHST- 2015/11/27 06:00 [entrez] PHST- 2015/11/27 06:00 [pubmed] PHST- 2015/11/27 06:01 [medline] PHST- 2015/11/25 00:00 [pmc-release] AID - 10.1186/s11671-015-1162-2 [pii] AID - 1162 [pii] AID - 10.1186/s11671-015-1162-2 [doi] PST - ppublish SO - Nanoscale Res Lett. 2015 Dec;10(1):453. doi: 10.1186/s11671-015-1162-2. Epub 2015 Nov 25.