TY - JOUR

T1 - Encapsulation and release of doxycycline from electrospray-generated PLGA microspheres

T2 - Effect of polymer end groups

AU - Wang, Jiamian

AU - Helder, Leonie

AU - Shao, Jinlong

AU - Jansen, John A.

AU - Yang, Mingshi

AU - Yang, Fang

PY - 2019/6/10

Y1 - 2019/6/10

N2 - The aim of this study was to investigate the influence of end group of poly(lactic-co-glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To this end, doxycycline hyclate (DOX) was selected as a model drug, and PLGA (molecular weight: 17 and 44 kDa) with either an acid or ester end group were electrosprayed with DOX. The processing parameters were optimized to obtain microspheres comparable in size. Drug loading efficiency and release profile were determined by the high-performance liquid chromatography-ultraviolet detection (HPLC-UV) method. PLGA polymers or drug-loaded microspheres were characterized before and after exposure to phosphate buffer saline at 37 °C regarding the wettability of polymers, pH changes of the buffer, molecular weight of PLGA and morphology of the microspheres. The acid end group of PLGA microspheres brought about lower encapsulation efficiency and faster DOX release rate in our study, indicating that different hydrophilicity of polymer and degradation speed were the main reasons causing a difference in encapsulation efficiency and release profile. In addition, DOX released from the PLGA microspheres was active by showing antibacterial effects against Porphyromonas gingivalis as measured using a zone of inhibition test, and varying the end groups showed no impact on the antibacterial efficacy. This study demonstrated that the end group of PLGA can be used as a new tool to regulate drug encapsulation efficiency and release rate to meet different clinical drug delivery requirements.

AB - The aim of this study was to investigate the influence of end group of poly(lactic-co-glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To this end, doxycycline hyclate (DOX) was selected as a model drug, and PLGA (molecular weight: 17 and 44 kDa) with either an acid or ester end group were electrosprayed with DOX. The processing parameters were optimized to obtain microspheres comparable in size. Drug loading efficiency and release profile were determined by the high-performance liquid chromatography-ultraviolet detection (HPLC-UV) method. PLGA polymers or drug-loaded microspheres were characterized before and after exposure to phosphate buffer saline at 37 °C regarding the wettability of polymers, pH changes of the buffer, molecular weight of PLGA and morphology of the microspheres. The acid end group of PLGA microspheres brought about lower encapsulation efficiency and faster DOX release rate in our study, indicating that different hydrophilicity of polymer and degradation speed were the main reasons causing a difference in encapsulation efficiency and release profile. In addition, DOX released from the PLGA microspheres was active by showing antibacterial effects against Porphyromonas gingivalis as measured using a zone of inhibition test, and varying the end groups showed no impact on the antibacterial efficacy. This study demonstrated that the end group of PLGA can be used as a new tool to regulate drug encapsulation efficiency and release rate to meet different clinical drug delivery requirements.

KW - Drug release profile

KW - Electrospraying

KW - Encapsulation efficiency

KW - PLGA microspheres

KW - Polymer end group

U2 - 10.1016/j.ijpharm.2019.04.023

DO - 10.1016/j.ijpharm.2019.04.023

M3 - Journal article

C2 - 30978487

AN - SCOPUS:85064152288

VL - 564

SP - 1

EP - 9

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

ER -