Development and characterization of itraconazole-loaded solid lipid nanoparticles for ocular delivery.
The purpose of this study was to investigate the feasibility of entrapping water-insoluble drug itraconazole into solid lipid nanoparticles (SLNs) for topical ocular delivery. The drug-loaded SLNs were prepared from stearic acid and palmitic acid using different concentrations of polyvinyl alcohol employed as emulsifier. SLNs were prepared by the melt-emulsion sonication and low temperature-solidification method and characterized for particle size, zeta potential, drug loading and drug entrapment efficiency. The mean particle size of SLNs prepared with stearic acid ranged from 139 to 199 nm, while the SLNs prepared with palmitic acid had particle size in the range of 126-160 nm. The SLNs were spherical in shape. Stearic acid-SLNs showed higher entrapment of drug compared with palmitic acid-SLNs. Differential scanning calorimetry (DSC) and X-ray diffraction measurements showed decrease in crystallinity of drug in the SLN formulations. The modified Franz-diffusion cell and freshly excised goat corneas were used to test drug corneal permeability. Permeation of itraconazole from stearic acid-SLNs was higher than that obtained with palmitic acid-SLNs. The SLNs showed clear zone of inhibition against Aspergillus flavus indicating antimicrobial efficacy of formulations.
Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj , Odisha , India .
Biswaranjan
B
Mohanty
Dipak K
DK
Majumdar
Sagar K
SK
Mishra
Amulya K
AK
Panda
Soma
S
Patnaik
D060433:Administration, Ophthalmic; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001228:Aspergillosis / Q000188:drug therapy; D001231:Aspergillus flavus / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003315:Cornea / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004655:Emulsions / Q000737:chemistry; D006041:Goats; D017964:Itraconazole / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D019308:Palmitic Acid / Q000737:chemistry*; D010316:Particle Size; D013229:Stearic Acids / Q000737:chemistry*; D014961:X-Ray Diffraction
D000935:Antifungal Agents; D004337:Drug Carriers; D004655:Emulsions; D013229:Stearic Acids; D019308:Palmitic Acid; D017964:Itraconazole; C031183:stearic acid
Itraconazole; palmitic acid; permeation; solid lipid nanoparticles; stearic acid