(DOX-NPtm)的生物物理特性:FTIR和DSC研究

Amal Abdullah Al Mutairi, Mohsen Mahmoud Mady
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摘要

与多柔比星(DOX)相比,多柔比星装载到聚乙二醇(PEG)脂质体中具有更长的循环时间和更低的心脏毒性。本研究旨在研究已上市制剂dox -封装脂质体(DOX-NPTM)的生物物理特性。阿霉素与脂质体之间的相互作用有助于脂质体的发育。用差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)对脂质体和DOX-NPTM进行了表征。测定了脂质体样品的流变特性。药物官能团与脂质体之间可能发生物理相互作用,可能通过弱氢键的形成或偶极-偶极相互作用引起的弱键的形成。在dox包封的脂质体样品中存在的脂质体特征峰之间没有检测到现有峰的移位或新峰的出现。这表明只有药物和脂质之间发生了物理相互作用,而它们之间没有化学相互作用。DSC信息显示,在将DOX加载到脂质体中后,相变温度降低。DSC曲线有较小的展宽。这可能推断在DOX包合后脂质体膜的酰基链之间的协同性略有下降。DOX包封脂质体降低了脂质体的塑性粘度(从1.64 cP降至1.48 cP),表明膜流动性增加。
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Biophysical Characterization of (DOX-NPtm): FTIR and DSC Studies
Doxorubicin loaded into liposomes grafted with polyethylene glycol (PEG) has been demonstrated to have a longer circulation time and lower cardiotoxicity than doxorubicin (DOX). This study aims to investigate the biophysical characterization of a marketed formulation DOX-encapsulated liposome (DOX-NPTM). The interactions between doxorubicin and liposomal lipids can help in liposomal development. The liposome and DOX-NPTM were characterized in terms of differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The rheological properties of liposomal samples were also measured. Physical interactions may be occurred between the drug functional groups and liposomal lipids, probably by weak hydrogen bond formation or weak bond formation due to dipole-dipole interaction. There was no shift of existing peaks or appearance of new peaks was detected between the characteristic peaks of the liposomal lipids were present in the DOX-encapsulated liposome sample. This suggests that there were physical interactions that took place only between the drug and lipids and no chemical interaction between them. DSC information shows that the phase transition temperature shifts to lower temperature degrees after loading of DOX into the liposomes. The DSC curve has a small broadening. This may infer a little cooperativity decrease between acyl chains of liposomal membranes after DOX inclusion. The encapsulation of DOX into liposomes decreases the plastic viscosity of liposomes (from 1.64 to 1.48 cP), which shows that the membrane fluidity was increased.
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