Investigation of cutaneous penetration properties of stearic acid loaded to dendritic core-multi-shell (CMS) nanocarriers

• Published in: International journal of pharmaceutics 2016-03, Vol.501 (1-2), p.271-277
• Main Authors: Lohan, S.B., Icken, N., Teutloff, C., Saeidpour, S., Bittl, R., Lademann, J., Fleige, E., Haag, R., Haag, S.F., Meinke, M.C.
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Carbocyanines - administration & dosage; Carbocyanines - chemistry; Dendrimers - administration & dosage; Dendrimers - chemistry; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Electron paramagnetic resonance spectroscopy (EPR; Electron Spin Resonance Spectroscopy; Fluorescence spectroscopy; Fluorescent Dyes - administration & dosage; Fluorescent Dyes - chemistry; Glycerol - administration & dosage; Glycerol - chemistry; Hair follicle; Hair Follicle - metabolism; In Vitro Techniques; Microscopy, Fluorescence; Nanostructures - administration & dosage; Nanostructures - chemistry; Nanotransport system (NTS); Polyethylene Glycols - administration & dosage; Polyethylene Glycols - chemistry; Polymers - administration & dosage; Polymers - chemistry; Skin - metabolism; Skin Absorption; Skin penetration; Stearic Acids - administration & dosage; Stearic Acids - chemistry; Swine
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2016.02.004

[Display omitted] Dendritic core-multi shell (CMS) particles are polymer based systems consisting of a dendritic polar polyglycerol polymer core surrounded by a two-layer shell of nonpolar C18 alkyl chains and hydrophilic polyethylene glycol. Belonging to nanotransport systems (NTS) they allow the transport and storage of molecules with different chemical characters. Their amphipihilic character CMS-NTS permits good solubility in aqueous and organic solutions. We showed by multifrequency electron paramagnetic resonance (EPR) spectroscopy that spin-labeled 5-doxyl stearic acid (5DSA) can be loaded into the CMS-NTS. Furthermore, the release of 5DSA from the carrier into the stratum corneum of porcine skin was monitored ex vivo by EPR spectroscopy. Additionally, the penetration of the CMS-NTS into the skin was analyzed by fluorescence microscopy using indocarbocyanine (ICC) covalently bound to the nanocarrier. Thereby, no transport into the viable skin was observed, whereas the CMS-NTS had penetrated into the hair follicles down to a depth of 340μm±82μm. Thus, it could be shown that the combined application of fluorescence microscopy and multi-frequency EPR spectroscopy can be an efficient tool for investigating the loading of spin labeled drugs to nanocarrier systems, drug release and penetration into the skin as well as the localization of the NTS in the skin.