Insight into Nanoscale Network of Spray-dried Polymeric Particles: Role of Polymer Molecular Conformation

TY - JOUR

T1 - Insight into Nanoscale Network of Spray-dried Polymeric Particles

T2 - Role of Polymer Molecular Conformation

AU - Wan, Feng

AU - Larsen, Flemming Hofmann

AU - Nunes Bordallo, Heloisa

AU - Foged, Camilla

AU - Rantanen, Jukka

AU - Yang, Mingshi

PY - 2018/10/31

Y1 - 2018/10/31

N2 - Poly(lactic-co-glycolic acid) (PLGA) microparticles represent a promising formulation approach for providing steady pharmacokinetic/pharmacodynamic profiles of therapeutic drugs for a long period. Understanding and controlling the supramolecular structure of PLGA microparticles at a molecular level is a prerequisite for the rational design of well-controlled, reproducible sustained-release profiles. Herein, we reveal the role of PLGA molecular conformation in particle formation and drug release. The nanoscale network of PLGA microparticles spray-dried using the solvents with distinct polarities was investigated by using NMR and neutron scattering. By employing chemometric method, we further demonstrate the evolution of nanoscale networks in spray-dried PLGA microparticles upon water absorption. Our results indicate that PLGA molecules form more chain entanglements during spray drying when using the solvents with low polarity, where PLGA molecule adopts a more flexible, extended conformation, resulting in the network being more resistant to water absorption in spray-dried PLGA microparticles. This work underlines the role of PLGA molecular conformation in controlling formation and evolution of nanoscale network of spray-dried PLGA microparticles and will have important consequences in achieving customized drug release from the PLGA microparticles.

AB - Poly(lactic-co-glycolic acid) (PLGA) microparticles represent a promising formulation approach for providing steady pharmacokinetic/pharmacodynamic profiles of therapeutic drugs for a long period. Understanding and controlling the supramolecular structure of PLGA microparticles at a molecular level is a prerequisite for the rational design of well-controlled, reproducible sustained-release profiles. Herein, we reveal the role of PLGA molecular conformation in particle formation and drug release. The nanoscale network of PLGA microparticles spray-dried using the solvents with distinct polarities was investigated by using NMR and neutron scattering. By employing chemometric method, we further demonstrate the evolution of nanoscale networks in spray-dried PLGA microparticles upon water absorption. Our results indicate that PLGA molecules form more chain entanglements during spray drying when using the solvents with low polarity, where PLGA molecule adopts a more flexible, extended conformation, resulting in the network being more resistant to water absorption in spray-dried PLGA microparticles. This work underlines the role of PLGA molecular conformation in controlling formation and evolution of nanoscale network of spray-dried PLGA microparticles and will have important consequences in achieving customized drug release from the PLGA microparticles.

U2 - 10.1021/acsami.8b12475

DO - 10.1021/acsami.8b12475

M3 - Journal article

C2 - 30211530

SN - 1944-8244

VL - 10

SP - 36686

EP - 36692

JO - A C S Applied Materials and Interfaces

JF - A C S Applied Materials and Interfaces

IS - 43

ER -