preparation and characterization of stable nanoliposomal formulation of fluoxetine as a potential adjuvant therapy for drug-resistant tumors

Authors

azadeh haeri school of pharmacy, shahid beheshti university of medical sciences

behdokht alinaghian school of pharmacy, shahid beheshti university of medical sciences

marjan daeihamed school of pharmacy, shahid beheshti university of medical sciences

simin dadashzadeh shahid beheshti university of medical sciences

abstract

chemotherapy research highly prioritizes overcoming the multidrug resistance (mdr) in human tumors. liposomal formulation of fluoxetine, as a fourth generation chemosensitizer, was constructed and characterized for percent entrapment, release profile, morphology, particle size, zeta potential and stability. liposomes were prepared using different active loading techniques. the influence of different formulation variables such as loading methodology, type of main lipid, addition of pegylated lipid and cholesterol percentage was evaluated to achieve required entrapment efficiency, in vitro release behavior and stability. the studied parameters had significant effect on physicochemical characteristics of the nanocarriers. high fluoxetine encapsulation efficiency (83% ± 3%) and appropriate particle size (101 ± 12 nm) and zeta potential (-9 ± 2 mv) were achieved for pegylation liposomes composed of dspe-peg, dspc and cholesterol at respective molar ratio of 5:70:25. an in vitro fluoxetine release of about 20% in 48 h was observed from optimum formulation. atomic force microscopy (afm) studies confirmed homogeneous distribution of particles and spherical shape with smooth surface. the optimum formulation was stable for 9 days when incubated at 37°c. the results of this study are very encouraging for application of the developed fluoxetine liposomal formulation in drug-resistant tumor models.

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Journal title:

iranian journal of pharmaceutical research

جلد ۱۳، شماره Supplement، صفحات ۳-۱۴

Keywords

fluoxetine nanoliposomes formulation parameters pegylation drug resistant tumors

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