title: Preparation of tripterine nanostructured lipid carriers and their absorption in rat intestine.
abstract: The purpose of this study was to develop an optimized nanostructured lipid carrier formulation (NLC) for tripterine, and to estimate the potential of NLCs as oral delivery system. Tripterine-loaded NLCs were prepared by the solvent evaporation method. The average drug entrapment efficiency, particle size and zeta potential of the optimized tripterine-loaded NLCs were 78.64 +/- 0.37%, 109.6 +/- 5.8 nm and -29.8 +/- 1.3 mV, respectively. The tripterine-loaded NLCs showed spherical morphology with smooth surface under the transmission electron microscope (TEM). The crystallization of drug in NLC was investigated by differential scanning calorimetry (DSC). The drug was in an amorphous state in the NLC matrix. According to the in vitro release study, the tripterine-loaded NLCs showed a delayed release profile of tripterine. The rat intestinal perfusion model was used to study the absorption of tripterine solution and tripterine-loaded NLCs. The Peff* (effective permeability) of tripterine-loaded NLCs in the duodenum, jejunum, ileum and colon was approximately 2.1, 2.7, 1.1, 1.2-fold higher than that of tripterine solution, respectively. The 10% ABS (percent absorption of 10 cm of intestine) of tripterine-loaded NLCs in the duodenum, jejunum, ileum and colon was approximately 2.2, 2.3, 1.2, 1.3-fold higher than that of tripterine solution, respectively. The intestinal toxicity of tripterine formulated in the NLCs was investigated and compared with the tripterine solution by the MTT assay with Caco-2 cell models. According to the result, the tripterine-loaded NLCs could greatly decrease the cytotoxicity of the drug. In conclusion, the NLC formulation remarkably improved the absorption of tripterine and showed a better biocompatibility.
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, PR China.
authors.forename: Lei
authors.initials: L
authors.lastname: Zhou
authors.forename: Yan
authors.initials: Y
authors.lastname: Chen
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.forename: Junjie
authors.initials: J
authors.lastname: He
authors.forename: Meng
authors.initials: M
authors.lastname: Du
authors.forename: Qingqing
authors.initials: Q
authors.lastname: Wu
mesh_terms: D000465:Algorithms; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004339:Drug Compounding; D004563:Electrochemistry; D066298:In Vitro Techniques; D007408:Intestinal Absorption / Q000502:physiology*; D008055:Lipids; D008297:Male; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000737:chemistry; D010316:Particle Size; D053978:Pentacyclic Triterpenes; D010477:Perfusion; D019999:Pharmaceutical Solutions; D051381:Rats; D017207:Rats, Sprague-Dawley; D014315:Triterpenes / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D008055:Lipids; D053978:Pentacyclic Triterpenes; D019999:Pharmaceutical Solutions; D014315:Triterpenes; C050414:celastrol