Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria.
Eur J Pharm Biopharm. 2010 Jun;75(2):148-53. doi: 10.1016/j.ejpb.2010.03.014. Epub 2010 Mar 21.
1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) liposomes were prepared by high-pressure homogeniser and coated with two cationic polymers, chitosan (CS) and for the first time Eudragit EPO (EU), respectively. Compared to the control liposomes, the polymeric liposomes showed greater physicochemical stability in terms of mean particle size and zeta potential at room temperature. In the present study, aciclovir and minoxidil have been used as hydrophilic and hydrophobic candidates. In the presence of the drugs, the polymeric liposomes still showed constant particle size and zeta potential. Influences of polymers and model drugs on thermotropic phase transition of DPPC liposomes were studied by micro-differential scanning calorimetry (microDSC). The influences on configuration of DPPC liposomes were investigated by Fourier transform infrared spectroscopy (FTIR). According to DSC results, cationic polymers had a stabilising effect, whereas aciclovir and minoxidil changed the physical properties of the DPPC bilayers by influencing the main phase transition temperature and erasing the pre-transition. The investigation of CO stretching bands of DPPC at 1736 cm(-1) in FTIR spectra showed that aciclovir has strong hydrogen bonding with CO groups of DPPC, whereas carbonyl groups were free in minoxidil presence. Moreover, the coating of liposomes with CS or EU led to higher skin diffusion for both drugs. This could be explained as an effect of positively charged liposomes to interact stronger with skin negatively charged surface and their possible interactions with structures below the stratum corneum.
1,2-二月桂酰基-sn-甘油-3-磷酸胆碱(DPPC)脂质体通过高压匀质机制备,并分别用两种阳离子聚合物壳聚糖(CS)和Eudragit EPO(EU)进行包被。与对照脂质体相比,聚合物脂质体在室温下的平均粒径和zeta 电位方面表现出更大的物理化学稳定性。在本研究中,阿昔洛韦和米诺地尔被用作亲水性和疏水性候选药物。在存在药物的情况下,聚合物脂质体仍显示出恒定的粒径和zeta 电位。通过微差示扫描量热法(microDSC)研究了聚合物和模型药物对 DPPC 脂质体热致相转变的影响。通过傅立叶变换红外光谱(FTIR)研究了聚合物和模型药物对 DPPC 脂质体结构的影响。根据 DSC 结果,阳离子聚合物具有稳定作用,而阿昔洛韦和米诺地尔通过影响主相变温度和消除预相变来改变 DPPC 双层的物理性质。在 FTIR 光谱中对 DPPC 在 1736 cm(-1)处的 CO 伸缩带的研究表明,阿昔洛韦与 DPPC 的 CO 基团具有强氢键,而在米诺地尔存在下羰基基团是自由的。此外,CS 或 EU 对脂质体的包被导致两种药物的皮肤扩散性更高。这可以解释为带正电荷的脂质体与皮肤带负电荷的表面相互作用更强,以及它们与角质层以下结构的可能相互作用。