Influence of polymeric carrier on the disposition and retention of 20(R)-ginsenoside-rg3-loaded swellable microparticles in the lung.
The objective of this study was to investigate the influence of differently charged biocompatible polymers, including chitosan (CS), hyaluronic acid (HA), and hydroxypropyl cellulose (HPC), on the disposition and retention of 20(R)-ginsenoside-rg3 (Rg3)-loaded swellable microparticles in the lung. A high-pressure homogenization method combined with spray drying was used to prepare Rg3-loaded microparticles. In vitro aerodynamic performance of different microparticles was characterized by the Next Generation Impactor (NGI). Retention of the swellable microparticles in the rat lung was investigated using bronchoalveolar lavage fluid method. Influence of drug loading, polymer molecular weight, and polymer charge on the properties of the swellable microparticles was investigated. It was found that drug loading had no significant influence on experimental mass median aerodynamic diameter (MMADe) and fine particle fraction (FPF). Increasing polymer molecular weight caused no remarkable change in MMADe value, but the FPF value decreased with the increase of polymer molecular weight. At the same molecular weight level, polymer structure and charge had no statistical influence on the in vitro aerodynamic properties of the microparticles and lung disposition, but it influenced the swelling and bioadhesion behavior and therefore lung retention profile. Desirable phagocytosis escapement and inhibition of A549 cell proliferation were achieved for the developed swellable microparticles. In conclusion, the lung retention of swellable microparticles can be adjusted by selecting polymeric carriers with different structure and charge.
['Wang|Xiuhua|X|', 'Zhang|Xiao|X|', 'Fan|Linlin|L|', 'He|Huan|H|', 'Zhang|Xiaofei|X|', 'Zhang|Yuyang|Y|', 'Mao|Shirui|S|http://orcid.org/0000-0002-5036-6559']
D000072283:A549 Cells D000268:Adhesiveness D000818:Animals D001992:Bronchoalveolar Lavage Fluid D002470:Cell Survival D002482:Cellulose D048271:Chitosan D004337:Drug Carriers D065546:Drug Liberation D036145:Ginsenosides D006801:Humans D006820:Hyaluronic Acid D007413:Intestinal Mucosa D007583:Jejunum D008168:Lung D008264:Macrophages D008297:Male D051379:Mice D008970:Molecular Weight D010316:Particle Size D000067996:RAW 264.7 Cells D017207:Rats, Sprague-Dawley D017208:Rats, Wistar
Swellable microparticle Chitosan Hyaluronic acid Hydroxypropyl cellulose 20(R)-ginsenoside-rg3 A549 cells Lung disposition and retention