PLGA公司
药品
化学
车辆段
剂型
体内
体外
药理学
溶解度
肌肉组织
利多卡因
色谱法
生物化学
医学
外科
有机化学
生物技术
考古
解剖
生物
历史
作者
Jan Kožák,Miloslava Rabišková,Alf Lamprecht
出处
期刊:Aaps Pharmscitech
[Springer Nature]
日期:2021-03-29
卷期号:22 (3)
被引量:6
标识
DOI:10.1208/s12249-021-01965-4
摘要
Despite the importance of drug release testing of parenteral depot formulations, the current in vitro methods still require ameliorations in biorelevance. We have investigated here the use of muscle tissue components to better mimic the intramuscular administration. For convenient handling, muscle tissue was used in form of a freeze-dried powder, and a reproducible process of incorporation of tested microspheres to an assembly of muscle tissue of standardized dimensions was successfully developed. Microspheres were prepared from various grades of poly(lactic-co-glycolic acid) (PLGA) or ethyl cellulose, entrapping flurbiprofen, lidocaine, or risperidone. The deposition of microspheres in the muscle tissue or addition of only isolated lipids into the medium accelerated the release rate of all model drugs from microspheres prepared from ester-terminated PLGA grades and ethyl cellulose, however, not from the acid-terminated PLGA grades. The addition of lipids into the release medium increased the solubility of all model drugs; nonetheless, also interactions of the lipids with the polymer matrix (ad- and absorption) might be responsible for the faster drug release. As the in vivo drug release from implants is also often faster than in simple buffers in vitro, these findings suggest that interactions with the tissue lipids may play an important role in these still unexplained observations.
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