Enhanced oromucosal delivery of progesterone via hexosomes.
OBJECTIVE
Formulation and characterization of progesterone loaded hexosomes employing a novel method for oromucosal delivery.


METHODS
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.


CONCLUSIONS
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.
Swarnakar
Nitin K
NK
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar (M.P.), 470003, India.
Jain
Vikas
V
Dubey
Vaibhav
V
Mishra
Dinesh
D
Jain
N K
NK
D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D015194:Diffusion Chambers, Culture; D004339:Drug Compounding; D004355:Drug Stability; D004356:Drug Storage; D000431:Ethanol / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry*; D007700:Kinetics; D008081:Liposomes; D018613:Microscopy, Confocal; D009061:Mouth Mucosa / Q000378:metabolism*; D019301:Oleic Acid / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability; D011374:Progesterone / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D011372:Progestins / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry