Relationships Between the Properties of Self-Emulsifying Pellets and of the Emulsions Used as Massing Liquids for Their Preparation

Journal Title: AAPS PharmSciTech - Year 2015, Vol 16, Issue 1

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 R2 = 0.796 for furosemide and R2 = 0.885 for propranolol and for the shape factor, eRR2 = 0.740 and R2 = 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], R2 = 0.856), which may be useful in formulation work.

Authors and Affiliations

Ioannis Nikolakakis, Athanasia Panagopoulou, Andrea Salis, Stavros Malamataris

Keywords

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  • EP ID EP682204
  • DOI  10.1208/s12249-014-0214-8
  • Views 97
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How To Cite

Ioannis Nikolakakis, Athanasia Panagopoulou, Andrea Salis, Stavros Malamataris (2015). Relationships Between the Properties of Self-Emulsifying Pellets and of the Emulsions Used as Massing Liquids for Their Preparation. AAPS PharmSciTech, 16(1), -. https://europub.co.uk/articles/-A-682204