Impact of detergents on the physiochemical behavior of itraconazole loaded nanostructured lipid carriers

• Published in: Colloids and surfaces. A, Physicochemical and engineering aspects Physicochemical and engineering aspects, 2017-03, Vol.516, p.63-71
• Main Authors: Bhadra, A., Karmakar, G., Nahak, P., Chettri, P., Roy, B., Guha, P., Mandal, A.K., Nath, R.K., Panda, A.K.
• Format: Article
• Language: English
• Subjects: Antifungul activity; DLS; Drug release; DSC; ITZ; NLC
• ISSN: 0927-7757; 1873-4359
• DOI: 10.1016/j.colsurfa.2016.12.009

[Display omitted] •NLCs were prepared with triolein, cetyl palmitate and palmitic acid.•Cationic, anionic, zwitterionic and nonionic surfactants were used as stabilizers.•Antifungal drug, itraconazole was loaded into NLC.•Physicochemical characterizations of drug loaded NLCs were done.•Drug loaded NLCs showed superior antifungul activities. Effect of different surfactants (nonionic, anionic, cationic and zwitterionic) as stabilizer on the physicochemical properties of the nanostructured lipid carriers (NLC) comprising cetyl palmitate, triolein and palmitic acid were explored in the absence and presence of a potent antifungal drug, itraconazole. The blank and drug loaded NLC formulations were prepared by way of hot homogenization and ultrasonication technique. Combined dynamic light scattering, electron microscopy, atomic force microscopy, differential scanning calorimetry, UV–vis absorption spectroscopy and method of dialysis were adopted in characterizing the formulations. NLCs were stable up to 100days irrespective of the surfactant. While the ionic surfactant comprising NLCs were electrostatically stable, the nonionic surfactants imparted better steric stabilization as revealed from the decreased size and polydispersity index values. Up shift in the phase transition temperature, changes in enthalpy and heat capacity in case of nonionic surfactant comprising systems substantiated its superior stabilization effect over the ionic surfactants. NLC formulations, stabilized by nonionic surfactants, exhibited superior drug incorporation, loading capacity and sustained release for itraconazole. Itraconazole loaded NLC formulations exhibited substantial antifungal activity against the fungal strain Aspergillusniger MTCC 3323. Such a comprehensive set of studies could assess the NLC formulation as potential drug delivery system for itraconazole.