Puglia Carmelo, Offerta Alessia, Tirendi Giorgia Giusy, Tarico Maria Stella, Curreri Sergio, Bonina Francesco, Perrotta Rosario Emanuele
a Department of Drug Sciences , University of Catania , Catania , Italy and.
b Azienda Ospedaliera per l'Emergenza "Cannizzaro" , Dipartimento di Specialità Medico Chirurgiche - Sezione di Chirurgia Plastica , Catania , Italy.
Drug Deliv. 2016;23(1):36-40. doi: 10.3109/10717544.2014.903011. Epub 2014 Apr 15.
Solid lipid nanoparticles (SLN) are drug carriers possessing numerous features useful for topical application. A copious scientific literature outlined their ability as potential delivery systems for lipophilic drugs, while the entrapment of a hydrophilic drug inside the hydrophobic matrix of SLN is often difficult to obtain.
To develop SLN intended for loading caffeine (SLN-CAF) and to evaluate the permeation profile of this substance through the skin once released from the lipid nanocarriers. Caffeine is an interesting compound showing anticancer and protective effects upon topical administration, although its penetration through the skin is compromised by its hydrophilicity.
SLN-CAF were formulated by using a modification of the quasi-emulsion solvent diffusion technique (QESD) and characterized by PCS and DSC analyses. In vitro percutaneous absorption studies were effected using excised human skin membranes (i.e. Stratum Corneum Epidermis or SCE).
SLN-CAF were in a nanometric range (182.6 ± 8.4 nm) and showed an interesting payload value (75% ± 1.1). DSC studies suggest the presence of a well-defined system and the successful drug incorporation. Furthermore, SLN-CAF generated a significantly faster permeation than a control formulation over 24 h of monitoring.
SLN-CAF were characterized by valid dimensions and a good encapsulation efficiency, although the active to incorporate showed a hydrophilic character. This result confirms the suitability of the formulation strategy employed in the present work. Furthermore, the in vitro evidence outline the key role of lipid nanoparticles in enhancing caffeine permeation through the skin.
固体脂质纳米粒（SLN）是具有多种适用于局部应用特性的药物载体。大量科学文献概述了它们作为亲脂性药物潜在递送系统的能力，而将亲水性药物包封在SLN的疏水性基质中往往难以实现。
开发用于负载咖啡因的SLN（SLN-CAF），并评估该物质从脂质纳米载体释放后通过皮肤的渗透情况。咖啡因是一种有趣的化合物，局部给药时具有抗癌和保护作用，但其亲水性会影响其经皮渗透。
采用改进的准乳液溶剂扩散技术（QESD）制备SLN-CAF，并通过PCS和DSC分析进行表征。使用离体人皮膜（即角质层-表皮或SCE）进行体外经皮吸收研究。
SLN-CAF处于纳米级范围（182.6±8.4nm），并显示出可观的载药量值（75%±1.1）。DSC研究表明存在明确的体系且药物成功包封。此外，在24小时的监测中，SLN-CAF产生的渗透速度明显快于对照制剂。
SLN-CAF具有合适的尺寸和良好的包封效率，尽管要包封的活性成分具有亲水性。这一结果证实了本研究中所采用制剂策略的适用性。此外，体外证据表明脂质纳米粒在增强咖啡因经皮渗透方面起关键作用。
