PURPOSE: Formulation and characterization of progesterone loaded hexosomes employing a novel method for oromucosal delivery. METHOD: Hexosomes were prepared employing a method in which ethanolic solution of lipid phase (monolein and oleic acid) was vortexed with aqueous phase (surfactant solution) and characterized for particle size, morphology and internal structure. FT-IR and confocal laser scanning microscopy (CLSM) were performed to investigate the possible mechanism and penetration pathway of hexosomes within the mucosa. RESULTS: Hexosomes exhibited anisotropy, hexagonal shape and nanometric size (251.2+/-1.8 nm). Internal structure confirmed by X-ray diffraction peaks with spacing ratio of radical1:radical3:radical4 proved two-dimensional hexagonal arrangements. Entrapment efficiency of system was greater than 95%. In vitro release studies revealed an enhanced transmucosal flux (4.67+/-0.14 microg cm(-2) h(-1)) and decreased lag time (1.54 h) across albino rabbit mucosa. FT-IR and CLSM of treated mucosa shows lipid extraction phenomena as well as structural irregularities within intercellular lipids respectively. These irregularities can function as 'virtual channels' facilitating hexosome's penetration. CONCLUSION: Developed hexosomes formulation exhibited high entrapment efficiency, high permeability and better stability on storage, thus proposing itself a novel carrier for enhanced oromucosal delivery of progesterone.
PURPOSE: Formulation and characterization of progesterone loaded hexosomes employing a novel method for oromucosal delivery. METHOD: Hexosomes were prepared employing a method in which ethanolic solution of lipid phase (monolein and oleic acid) was vortexed with aqueous phase (surfactant solution) and characterized for particle size, morphology and internal structure. FT-IR and confocal laser scanning microscopy (CLSM) were performed to investigate the possible mechanism and penetration pathway of hexosomes within the mucosa. RESULTS: Hexosomes exhibited anisotropy, hexagonal shape and nanometric size (251.2+/-1.8 nm). Internal structure confirmed by X-ray diffraction peaks with spacing ratio of radical1:radical3:radical4 proved two-dimensional hexagonal arrangements. Entrapment efficiency of system was greater than 95%. In vitro release studies revealed an enhanced transmucosal flux (4.67+/-0.14 microg cm(-2) h(-1)) and decreased lag time (1.54 h) across albino rabbit mucosa. FT-IR and CLSM of treated mucosa shows lipid extraction phenomena as well as structural irregularities within intercellular lipids respectively. These irregularities can function as 'virtual channels' facilitating hexosome's penetration. CONCLUSION: Developed hexosomes formulation exhibited high entrapment efficiency, high permeability and better stability on storage, thus proposing itself a novel carrier for enhanced oromucosal delivery of progesterone.
Authors: Nilesh R Rarokar; Suprit D Saoji; Nishikant A Raut; Jayashree B Taksande; Pramod B Khedekar; Vivek S Dave Journal: AAPS PharmSciTech Date: 2015-07-25 Impact factor: 3.246