title: A new drug nanocrystal self-stabilized Pickering emulsion for oral delivery of silybin.
abstract: A new silybin nanocrystal self-stabilized Pickering emulsion (SN-SSPE) has been developed using a high pressure homogenization method to improve the oral bioavailability of silybin. Influences of homogenization pressure and drug content on the formation of SN-SSPE were studied. The morphology, structure and size of Pickering emulsion droplets were characterized using a scanning electron micrograph, confocal laser scanning microscopy and atomic force microscopy. The stability, in vitro release and in vivo oral bioavailability of SN-SSPE were investigated. Results indicated that the particle size of silybin nanocrystals (SN-NC) decreased when homogenization pressure increased until 100MPa. When the content of silybin reached 300mg or above, a stable Pickering emulsion of silybin could be formed by sufficient SN-NC covering surfaces of oil droplets completely and thus self-stabilizing the Pickering emulsion. The emulsion droplet of SN-SSPE with the size of 27.3±3.1μm showed a core-shell structure consisting of a core of oil and a shell of SN-NC. SN-SSPE has shown high stability over 40days. The in vitro release rate of SN-SSPE was faster than silybin coarse powder and similar to silybin nanocrystalline suspension (SN-NCS). The peak concentration of silybin of SN-SSPE following intragastric administration in rats was increased by 2.5-fold and 3.6-fold compared with SN-NCS and silybin coarse powder, respectively. The AUC of SN-SSPE was increased by 1.6-fold and 4.0-fold compared with SN-NCS and silybin coarse powder, respectively. All these results showed that the Pickering emulsion of silybin could be stabilized by nanocrystals of silybin itself and increased the oral bioavailability of silybin. The drug nanocrystalline self-stabilized Pickering emulsion was a promising oral drug delivery system for poorly soluble drugs.
authors: School of Health Sciences, Macao Polytechnic Institute, 00853, Macau.
authors: Tao
authors: T
authors: Yi
authors: Guangan Center for Food and Drug Control, Guangan 638500, China.
authors: Chuan
authors: C
authors: Liu
authors: College of Pharmaceutical Sciences,Southwest University, Chongqing 400716, China.
authors: Jiao
authors: J
authors: Zhang
authors: College of Pharmaceutical Sciences,Southwest University, Chongqing 400716, China.
authors: Fan
authors: F
authors: Wang
authors: College of Pharmaceutical Sciences,Southwest University, Chongqing 400716, China.
authors: Jirui
authors: J
authors: Wang
authors: College of Pharmaceutical Sciences,Southwest University, Chongqing 400716, China. Electronic address: damo-huanghun@163.com.
authors: Jifen
authors: J
authors: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation / Q000187:drug effects* / Q000502:physiology; D004355:Drug Stability; D004655:Emulsions; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000378:metabolism*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D000975:Antioxidants; D004655:Emulsions; D012838:Silymarin; D000077385:Silybin
keywords: Nanocrystals; Oral bioavailability; Pickering emulsion; Self-stabilizing; Silybin