University of Athens, School of Pharmacy, Dept of Pharmaceutical Technology, Panepistimioupolis, Zografou, 15771 Athens, Greece.
Colloids Surf B Biointerfaces. 2010 Nov 1;81(1):11-9. doi: 10.1016/j.colsurfb.2010.06.010. Epub 2010 Jun 25.
A new Liposomal-Locked in-Dendrimer (LLD) formed by DPPC-DPPG and PAMAM 3.5 incorporating the anticancer drug DOX was studied by means of spectroscopic and DSC investigations. Multilamellar Lipid Bilayers were also considered for the sake of comparison. The results were in line with a picture of phase separation between DPPC-DPPG lipids and dendrimer that promotes the stability of the liposome membrane and the cooperativity of the relevant gel-to-liquid-crystal transition, which is enhanced in the presence of the dendrimer and the drug. As a result, the inner core of the liposome contained large amounts of dendrimer-DOX complex and was protected by a very stable membrane. This view was given a more general validation through investigations performed with other types of dendrimers, namely PG1 and PG2. The thermodynamic interpretation of the DSC data allowed a better understanding of the physico-chemical factors that justify this behaviour that makes these LLDs very promising as a new class of Modulatory Liposomal Controlled Release System (MLCRS) that could lead to drug formulations with higher safety and efficacy profiles.
一种新型的脂锁定树状聚合物(LLD)由 DPPC-DPPG 和 PAMAM 3.5 形成,其中包含抗癌药物 DOX,通过光谱和 DSC 研究进行了研究。还考虑了多层脂质双层以进行比较。结果与 DPPC-DPPG 脂质与树突状聚合物之间的相分离情况一致,这促进了脂质体膜的稳定性和相关凝胶到液晶的转变的协同性,在存在树突状聚合物和药物的情况下,这种协同性得到增强。结果,脂质体的内核包含大量的树突状聚合物-DOX 复合物,并受到非常稳定的膜的保护。通过对其他类型的树突状聚合物,即 PG1 和 PG2 进行的研究,对 DSC 数据的热力学解释提供了更一般的验证。对 DSC 数据的热力学解释允许更好地理解物理化学因素,这些因素证明了这种行为是合理的,这使得这些 LLD 成为一种很有前途的新型调节型脂质体控释系统(MLCRS),这可能导致具有更高安全性和疗效的药物配方。