title: Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design.
abstract: The purpose of the present study was to optimize a solid lipid nanoparticle (SLN) of chloramphenicol by investigating the relationship between design factors and experimental data using response surface methodology. A Box-Behnken design was constructed using solid lipid (X(1)), surfactant (X(2)), and drug/lipid ratio (X(3)) level as independent factors. SLN was successfully prepared by a modified method of melt-emulsion ultrasonication and low temperature-solidification technique using glyceryl monostearate as the solid lipid, and poloxamer 188 as the surfactant. The dependent variables were entrapment efficiency (EE), drug loading (DL), and turbidity. Properties of SLN such as the morphology, particle size, zeta potential, EE, DL, and drug release behavior were investigated, respectively. As a result, the nanoparticle designed showed nearly spherical particles with a mean particle size of 248 nm. The polydispersity index of particle size was 0.277 ± 0.058 and zeta potential was -8.74 mV. The EE (%) and DL (%) could reach up to 83.29% ± 1.23% and 10.11% ± 2.02%, respectively. In vitro release studies showed a burst release at the initial stage followed by a prolonged release of chloramphenicol from SLN up to 48 hours. The release kinetics of the optimized formulation best fitted the Peppas-Korsmeyer model. These results indicated that the chloramphenicol-loaded SLN could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.
authors.affiliation: College of Pharmacy, Taishan Medical University, Taian, PR China.
authors.forename: Jifu
authors.initials: J
authors.lastname: Hao
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Fang
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jianzhu
authors.initials: J
authors.lastname: Wang
authors.forename: Fengguang
authors.initials: F
authors.lastname: Guo
authors.forename: Fei
authors.initials: F
authors.lastname: Li
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Peng
mesh_terms: D000287:Administration, Topical; D000704:Analysis of Variance; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002701:Chloramphenicol / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D017076:Computer-Aided Design; D016503:Drug Delivery Systems / Q000379:methods*; D005989:Glycerides / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008956:Models, Chemical; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009391:Nephelometry and Turbidimetry; D009883:Ophthalmic Solutions / Q000737:chemistry* / Q000493:pharmacokinetics; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D015203:Reproducibility of Results; D013499:Surface Properties
chemical_list: D000900:Anti-Bacterial Agents; D005989:Glycerides; D009883:Ophthalmic Solutions; D020442:Poloxamer; C048159:glyceryl monostearate; D002701:Chloramphenicol