title: Relationships between the properties of self-emulsifying pellets and of the emulsions used as massing liquids for their preparation.
abstract: Self-emulsifying pellets were prepared using microcrystalline cellulose, emulsions of caprylic/capric triglyceride, and three Cremophors (ELP, RH40, and RH60) at 1.5 and 2.3 weight ratios, and two drugs (furosemide and propranolol) of different lipophilicity. Droplet size, zeta potential (ζ) and viscosity of emulsions, and pellet size, shape, friability, tensile strength, disintegration, and drug migration in pellets were determined. Evaluation of reconstituted emulsions was based on droplet size and ζ. Factorial design and 3-way ANOVA was applied to estimate the significance of the effects of the drug, surfactant and oil/surfactant ratio. It was found that droplet size, viscosity and ζ of emulsions, and size, shape, and friability of pellets were affected by the studied factors and were significant interactions between their effects on pellet size and friability. Migration of drug towards the pellet surface was higher for the less lipophilic furosemide and higher oil content. Linear relationships were found between the emulsion viscosity and the shape parameters of the pellets (for the aspect ratio R (2) = 0.796 for furosemide and R (2) = 0.885 for propranolol and for the shape factor, e R R (2) = 0.740 and R (2) = 0.960, respectively). For all the formulations examined, an exponential relationship was found between migration (M%) and the product of viscosity (η) and solubility of drug in oil/surfactant mixture (S) (M% = 98.1e-0.016 [η•S], R (2) = 0.856), which may be useful in formulation work.
authors.affiliation: Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, Thessaloniki, 54 124, Greece, yannikos@pharm.auth.gr.
authors.forename: Ioannis
authors.initials: I
authors.lastname: Nikolakakis
authors.forename: Athanasia
authors.initials: A
authors.lastname: Panagopoulou
authors.forename: Andrea
authors.initials: A
authors.lastname: Salis
authors.forename: Stavros
authors.initials: S
authors.lastname: Malamataris
mesh_terms: D065966:Absorption, Physicochemical; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods; D004343:Drug Implants / Q000138:chemical synthesis*; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry*; D005665:Furosemide / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011433:Propranolol / Q000008:administration & dosage / Q000737:chemistry*; D013718:Tensile Strength; D014783:Viscosity
chemical_list: D004343:Drug Implants; D045703:Emulsifying Agents; D004655:Emulsions; D005665:Furosemide; D011433:Propranolol