title: Non-aggregated protamine-coated poly(lactide-co-glycolide) nanoparticles of cisplatin crossed blood-brain barrier, enhanced drug delivery and improved therapeutic index in glioblastoma cells: in vitro studies.
abstract: OBJECTIVE
  Non-aggregated protamine impregnated poly(lactide-co-glycolide) nanoparticles of cisplatin (Pt-PLGA NPs) were synthesized to augment brain delivery.
  
  
  RESULTS
  The mean particle size of Pt-PLGA NPs and PLGA NPs were observed to be 173.2 ± 7.9 nm and 140 ± 10.2 nm, respectively. The Pt-PLGA NPs significantly (p < 0.05, one-way analysis of variance; ANOVA) delivered higher amount (172.41 ± 15.04 μg) of cisplatin in comparison to 110.48 ± 4.71 μg by PLGA NPs and 20.83 ± 1.65 μg by cisplatin solution across in vitro bovine brain microvessel endothelial cells. Cisplatin bearing Pt-PLGA NPs was found to be highly cytotoxic to U87 glioblastoma cells with an IC50 of 2.1 μM as compared (one-way ANOVA, p < 0.05) to PLGA NPs (3.9 μM) and cisplatin alone (13.33 μM). Impregnation with Pt enhanced the uptake of PLGA NPs in U87 glioblastoma cells as compared to PLGA NPs by following endocytosis mechanism.
  
  
  CONCLUSIONS
  Cisplatin-loaded Pt-PLGA NPs compel preclinical tumour regression study to further improve its utility against glioblastoma.
authors: Department of Pharmaceutics, Chandigarh College of Pharmacy , Mohali, Punjab , India .
authors: Neel Kamal
authors: NK
authors: Dhami
authors: Ravi Shankar
authors: RS
authors: Pandey
authors: Upendra Kumar
authors: UK
authors: Jain
authors: Ramesh
authors: R
authors: Chandra
authors: Jitender
authors: J
authors: Madan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001812:Blood-Brain Barrier / Q000378:metabolism* / Q000473:pathology; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002417:Cattle; D045744:Cell Line, Tumor; D002945:Cisplatin; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005909:Glioblastoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D011098:Polyglactin 910 / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011479:Protamines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D011479:Protamines; D011098:Polyglactin 910; D002945:Cisplatin
keywords: Blood–brain barrier; cisplatin; glioblastoma; poly(lactide-co-glycolide); protamine