title: Amine-functionalized poly(lactic-co-glycolic acid) nanoparticles for improved cellular uptake and tumor penetration.
abstract: Amine-functionalized poly(lactic-co-glycolic acid) (PLGA-NH2) nanoparticles (NPs) were developed for the delivery of phloretin. PLGA-NH2/phloretin NPs with 237nm mean diameter, narrow size distribution, and around -6mV zeta potential were fabricated by a modified emulsification-solvent evaporation method. The results of solid state studies revealed that drug was successfully incorporated into the polymeric NPs. The initial particle size of developed NPs was maintained after 24h incubation in human serum albumin (HSA) solution, fetal bovine serum (FBS), and phosphate buffered saline (PBS). Sustained and higher drug release patterns at acidic pH (pH 5.5), compared with neutral pH (pH 7.4), from PLGA-NH2NPs were observed. The experimental data of flow cytometry and confocal laser scanning microscopy (CLSM) studies suggested that PLGA-NH2NPs may have an improved cellular accumulation efficiency, compared with PLGA NPs, in Hep-2 cells (human laryngeal carcinoma). Also, PLGA-NH2NPs exhibited enhanced growth inhibitory effects rather than PLGA NPs in Hep-2 spheroid model. By introducing a simple strategy based on amine-functionalization of PLGA NPs (without installing complicated functional moieties), improved cellular uptake and antitumor efficacies without severe toxicity, compared with unmodified PLGA NPs, have been accomplished.
authors: College of Pharmacy, Kangwon National University, Chuncheon, Gangwon 24341, Republic of Korea.
authors: Song Yi
authors: SY
authors: Lee
authors: College of Pharmacy, Kangwon National University, Chuncheon, Gangwon 24341, Republic of Korea. Electronic address: hjcho@kangwon.ac.kr.
authors: Hyun-Jong
authors: HJ
authors: Cho
mesh_terms: D002152:Calorimetry, Differential Scanning; D002460:Cell Line; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000378:metabolism*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013816:Thermodynamics
chemical_list: D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: Amine group; Nanoparticle; PLGA; Phloretin; Tumor penetration