IQAC-CSIC, Department of Chemical and Surfactants Technology, Barcelona, Spain.
IQAC-CSIC, Department of Chemical and Surfactants Technology, Barcelona, Spain.
Eur J Pharm Biopharm. 2014 Feb;86(2):212-8. doi: 10.1016/j.ejpb.2013.05.012. Epub 2013 Jun 5.
This study assesses the potential usefulness of bicellar systems to retard the penetration of drugs into damaged skin. The active compound used in this study was diclofenac diethylamine (DDEA). Initially, physicochemical characterisation of the DDEA bicellar systems was performed at different temperatures by small-angle X-ray scattering (SAXS), wide-angle X-ray scattering (WAXS) and differential scanning calorimetry (DSC) techniques. Subsequently, in vitro percutaneous absorption of bicellar systems into in vitro damaged skin was studied. SAXS results indicated a slight decrease in the width of their bilayers with increasing temperature, with no apparent stacking in those systems. WAXS patterns were compatible with an orthorhombic lateral packing of the nanoaggregates. The thermogram obtained by DSC indicated a decrease in gel-to-liquid crystalline transition temperature (Tm) when the drug was included into bicellar systems. A retardation effect for DDEA was detected by in vitro percutaneous absorption studies when DDEA was vehiculised in the bicellar systems with respect to an aqueous solution of the drug. It seems that the use of bicellar systems as a vehicle for topical application of DDEA on skin with an impaired barrier function may inhibit the penetration of DDEA to the systemic level. Such systems may consequently repair stratum corneum barrier function to some extent. The use of these systems could be considered a new alternative strategy to treat topically pathological skin with different drugs.
本研究评估双分子胶束系统在延缓药物渗透进入受损皮肤方面的潜在用途。本研究中使用的活性化合物是双氯芬酸二乙胺（DDEA）。最初，通过小角 X 射线散射（SAXS）、广角 X 射线散射（WAXS）和差示扫描量热法（DSC）技术在不同温度下对 DDEA 双分子胶束系统进行了物理化学特性评估。随后，研究了双分子胶束系统向体外受损皮肤的体外经皮吸收。SAXS 结果表明，随着温度的升高，双分子胶束的双层宽度略有减小，这些系统中没有明显的堆积。WAXS 图谱与纳米聚集体的正交层状堆积相兼容。DSC 获得的热谱表明，当药物被包含在双分子胶束系统中时，凝胶到液晶相转变温度（Tm）降低。与药物的水溶液相比，当 DDEA 被包封在双分子胶束系统中时，通过体外经皮吸收研究检测到 DDEA 的延迟作用。似乎在具有受损屏障功能的皮肤上局部应用 DDEA 时，使用双分子胶束系统作为载体可能会抑制 DDEA 渗透到全身水平。因此，这些系统可能在一定程度上修复角质层屏障功能。可以考虑将这些系统用作治疗不同药物局部病理性皮肤的新替代策略。
