title: Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release.
abstract: Amoitone B, a novel compound chemically synthesized as the analogue of cytosporone B, has been proved to own superior affinity with Nur77 than its parent compound and exhibit notable anticancer activity. However, its application is seriously restricted due to the water-insolubility and short biological half-time. The aim of this study was to construct an effective delivery system for Amoitone B to realize sustained release, thus prolong drug circulation time in body and improve the bioavailability. Nanostructured lipid carriers (NLC) act as a new type of colloidal drug delivery system, which offer the advantages of improved drug loading and sustained release. Amoitone B-loaded NLC (AmB-NLC) containing glyceryl monostearate (GMS) and various amounts of medium chain triglycerides (MCT) were successfully prepared by emulsion-evaporation and low temperature-solidification technology with a particle size of about 200 nm and a zeta potential value of about -20 mV. The results of X-ray diffraction and DSC analysis showed amorphous crystalline state of Amoitone B in NLC. Furthermore, the drug entrapment efficacy (EE) was improved compared with solid lipid nanoparticles (SLN). The EE range was from 71.1% to 84.7%, enhanced with the increase of liquid lipid. In vitro drug release studies revealed biphasic drug release patterns with burst release initially and prolonged release afterwards and the release was accelerated with augment of liquid lipid. These results demonstrated that AmB-NLC could be a promising delivery system to control drug release and improve loading capacity, thus prolong drug action time in body and enhance the bioavailability.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University , Jinan , PR China and.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Luan
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.forename: Leilei
authors.initials: L
authors.lastname: Hao
authors.forename: Caiyun
authors.initials: C
authors.lastname: Li
authors.forename: Lisi
authors.initials: L
authors.lastname: Qi
authors.forename: Hejian
authors.initials: H
authors.lastname: Guo
authors.forename: Xinquan
authors.initials: X
authors.lastname: Liu
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D003460:Crystallization; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles; D049329:Nanostructures; D010316:Particle Size; D010648:Phenylacetates / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility; D014280:Triglycerides / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D005989:Glycerides; D008055:Lipids; D010648:Phenylacetates; D014280:Triglycerides; C576231:n-amyl 2-(3,5-dihydroxy-2-(1-nonanoyl)phenyl)acetate; C048159:glyceryl monostearate