title: Utilization of microfluidic V-junction device to prepare surface itraconazole adsorbed nanospheres.
abstract: Itraconazole is widely used as an anti-fungal drug to treat infections. However, its poor aqueous solubility results in low bioavailability. The aim of the present study was to improve the drug release profile by preparing surface itraconazole adsorbed polymethylsilsesquioxane (PMSQ) nanospheres using a V-junction microfluidic (VJM) device. In order to generate nanospheres with rough surface, the process flow rate of perfluorohexane (PFH) was set between 50 and 300 μl min(-1) while the flow rate of PMSQ and itraconazole solution were constant at 300 μl min(-1). Variations in the PFH flow rate enable the controlled size generation of nanospheres. PMSQ nanospheres adsorbing itraconazole were characterized by SEM, FTIR and Zetasizer. The release of itraconazole from PMSQ nanosphere surface was measured using UV spectroscopy. Nanosphere formulations with a range of sphere size (120, 320 and 800 nm diameter) were generated and drug release was studied. 120 nm itraconazole coated PMSQ nanospheres were found to present highest drug encapsulation efficiency and 13% drug loading in a more reproducible manner compared to 320 nm and 800 nm sized nanosphere formulations. Moreover, 120 nm itraconazole coated PMSQ nanospheres (encapsulation efficiency: 88%) showed higher encapsulation efficiency compared to 320 nm (encapsulation efficiency: 74%) and 800 nm (encapsulation efficiency: 62%) sized nanosphere formulations. The itraconazole coated PMSQ nanospheres were prepared continuously at the rate of 2.6 × 10(6) per minute via VJM device. Overall the VJM device enabled the preparation of monodisperse surface itraconazole adsorbed nanospheres with controlled in vitro drug release profile.
authors.affiliation: University College London, Department of Mechanical Engineering, Torrington Place, London WC1E 7JE, UK; Firat University, Faculty of Engineering, Department of Metallurgical and Materials Engineering, Elazig 23279, Turkey. Electronic address: israfil.kucuk.11@ucl.ac.uk.
authors.forename: Israfil
authors.initials: I
authors.lastname: Kucuk
authors.affiliation: De Montfort University, Leicester School of Pharmacy, Leicester LE1 9BH, UK. Electronic address: zahmad@dmu.ac.uk.
authors.forename: Zeeshan
authors.initials: Z
authors.lastname: Ahmad
authors.affiliation: University College London, Department of Mechanical Engineering, Torrington Place, London WC1E 7JE, UK. Electronic address: m.edirisinghe@ucl.ac.uk.
authors.forename: Mohan
authors.initials: M
authors.lastname: Edirisinghe
authors.affiliation: University College London, School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UK. Electronic address: m.gul@ucl.ac.uk.
authors.forename: Mine
authors.initials: M
authors.lastname: Orlu-Gul
mesh_terms: D000327:Adsorption; D000935:Antifungal Agents / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D065546:Drug Liberation; D005466:Fluorocarbons / Q000737:chemistry; D017964:Itraconazole / Q000737:chemistry*; D046210:Microfluidic Analytical Techniques; D054118:Nanospheres / Q000737:chemistry*; D017646:Organosilicon Compounds / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D013499:Surface Properties
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D005466:Fluorocarbons; D017646:Organosilicon Compounds; D011108:Polymers; D017964:Itraconazole; C532869:polymethylsilsesquioxane; C078626:perflexane
keywords: Drug delivery; Itraconazole; Nanospheres; Surface drug adsorbed; V-junction microfluidic device