Friday, September 2, 2016

PLGA-NH2 from PolySciTech investigated for improved cellular uptake as chemotherapy delivery system

PolySciTech Division of Akina, Inc. ( provides a wide array of biodegradable copolymers including Amine endcapped PLGA. Recently, researchers at Kangwon National University in Korea utilized PLGA-NH2 (PolyVivo AI062) and unreactive PLGA (PolyVivo AP063) from PolySciTech to develop a nanoparticle system for the delivery of phloretin (a natural dihydrochalcone which induces cancer apoptosis, doi: 10.1002/ijc.24189) to test Hep-2 cells (human laryngeal carcinoma). This research holds promise for improved chemotherapeutic strategies. Read more: Lee, Song Yi, and Hyun-Jong Cho. "Amine-functionalized poly (lactic-co-glycolic acid) nanoparticles for improved cellular uptake and tumor penetration." Colloids and Surfaces B: Biointerfaces (2016).

“Abstract: Amine-functionalized poly(lactic-co-glycolic acid) (PLGA-NH2) nanoparticles (NPs) were developed for the delivery of phloretin. PLGA-NH2/phloretin NPs with 237 nm mean diameter, narrow size distribution, and around −6 mV 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 24 h 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-NH2 NPs were observed. The experimental data of flow cytometry and confocal laser scanning microscopy (CLSM) studies suggested that PLGA-NH2 NPs may have an improved cellular accumulation efficiency, compared with PLGA NPs, in Hep-2 cells (human laryngeal carcinoma). Also, PLGA-NH2 NPs 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. Highlights: Poly(lactic-co-glycolic acid)-amine (PLGA-NH2) nanoparticles (NPs) were fabricated. Phloretin was encapsulated into the PLGA-NH2 NPs for tumor-targeted delivery. PLGA-NH2 NPs exhibited an improved cellular accumulation, compared with PLGA NPs. Enhanced tumor penetration efficiency in spheroids was observed in PLGA-NH2 NPs group.”

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