title: Enhancement in antifungal activity of eugenol in immunosuppressed rats through lipid nanocarriers.
abstract: In the present study eugenol loaded solid lipid nanoparticles (SLN) was prepared and characterized for particle size, polydispersity index, zeta potential, encapsulation efficiency, in vitro release and in vivo antifungal activity. Effect of addition of liquid lipid (caprylic triglyceride) to solid lipid (stearic acid) on crystallinity of lipid matrix of SLN was determined by using Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) techniques. Transmission electron microscopy (TEM) was carried out to determine the morphology of SLN. In vivo antifungal activity of eugenol loaded lipid nanoparticles was evaluated by using a model of oral candidiasis in immunosuppressed rats. Particle size results showed that d(90) of SLN(1) (single lipid matrix) and SLN(2) (binary lipid matrix) was 332±14.2 nm and 87.8±3.8 nm, respectively. Polydispersity index was found to be in the range of 0.27-0.4 which indicate moderate size distribution. Encapsulation efficiency of SLN(2) (98.52%) was found to be more than that of SLN(1) (91.80%) at same lipid concentration (2%, w/v). Increasing of the solid lipid concentration from 2% (w/v) to 4% (w/v) resulted in increase in encapsulation efficiency and the particle size. SLN(2) shows faster release of eugenol than that of SLN(1) due to smaller size and presence of liquid lipid which provide less barriers to the diffusion of drug from matrix. TEM study reveals the spherical shape of SLN. FT-IR, DSC and XRD results indicate less crystallinity of SLN(2) than that of SLN(1). In vivo studies show no significant difference in log cfu value of all the groups at 0 day. At 8th day, log cfu value of group treated with saline (control), standard antifungal agent, eugenol solution, SLN(1) and SLN(2) was found to be 3.89±.032, 2.69, 3.39±.088, 3.19±.028 and 3.08±0.124, respectively. The in vivo study results indicate improvement in the antifungal activity of eugenol when administrated in the form of SLN.
authors.affiliation: Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh, India.
authors.forename: A
authors.initials: A
authors.lastname: Garg
authors.forename: S
authors.initials: S
authors.lastname: Singh
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D002176:Candida albicans / Q000187:drug effects* / Q000254:growth & development; D002180:Candidiasis, Oral / Q000188:drug therapy* / Q000276:immunology / Q000382:microbiology / Q000473:pathology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003460:Crystallization; D003907:Dexamethasone / Q000009:adverse effects / Q000494:pharmacology; D004337:Drug Carriers / Q000032:analysis / Q000138:chemical synthesis*; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D005054:Eugenol / Q000737:chemistry / Q000494:pharmacology*; D007109:Immunity / Q000187:drug effects; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000032:analysis / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D051381:Rats; D011919:Rats, Inbred Strains; D014961:X-Ray Diffraction
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D007166:Immunosuppressive Agents; D008055:Lipids; D005054:Eugenol; D003907:Dexamethasone