Document Type

Article

Publication Date

2015

Abstract

OBJECTIVE: Niacin, activating G-protein coupled receptor (GPR) 109A, stimulates release of vasodilatory prostaglandins (PGs) such as PGE2 which can elicit niacin-associated flushing side effects. Poly-lactic-co-glycolic acid (PLGA) and poly-lactic acid (PLA) are used in nanoparticle (NP) drug delivery to reduce adverse effects and modulate drug release. Our study evaluated the in vitro effects of niacin-loaded PLGA or PLA-NPs on PGE2 expression in whole human blood as a model for niacin-induced flushing.

MATERIALS AND METHODS: NPs were formulated using a solvent evaporation process and characterized by size, polydispersity, zeta potential, drug entrapment, morphology, and drug release. NP in vitro effects on PGE2 release were measured via ELISA analysis.

RESULTS: PLGA-NPs demonstrated the lowest NP size (66.7 ± 0.21 nm) with the highest zeta potential and percent drug entrapment (42.00 ± 1.62 mV and 69.09 ± 0.29%, respectively) when compared to PLA-NPs (130.4 ± 0.66 nm, 27.96 ± 0.18 mV, 69.63 ± 0.03 %, respectively). In vitro release studies showed that PLGA-NPs underwent significant reductions in cumulative drug release when compared to PLA-NPs (p < 0.05). Furthermore, when compared to plain niacin, PLGA-NPs significantly reduced in vitro PGE2 release (p < 0.05).

CONCLUSIONS: These results support the use of PLGA-NPs as a novel method of delivery for reducing niacin-associated flushing.

Comments

This article was originally published in European Review for Medical and Pharmacological Sciences, volume 19, in 2015.

Copyright

European Review for Medical and Pharmacological Sciences

Creative Commons License

Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.

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