The influence of surfactant HLB and oil/surfactant ratio on the formation and properties of self-emulsifying pellets and microemulsion reconstitution.
Self-emulsifying oil/surfactant mixtures can be incorporated into pellets that have the advantages of the oral administration of both microemulsions and a multiple-unit dosage form. The purpose of this work was to study the effects of surfactant hydrophilic-lipophilic balance (HLB) and oil/surfactant ratio on the formation and properties of self-emulsifying microcrystalline cellulose (MCC) pellets and microemulsion reconstitution. Triglycerides (C(8)-C(10)) was the oil and Cremophor ELP and RH grades and Solutol the surfactants. Pellets were prepared by extrusion/spheronization using microemulsions with fixed oil/surfactant content but with different water proportions to optimize size and shape parameters. Microemulsion reconstitution from pellets suspended in water was evaluated by turbidimetry and light scattering size analysis, and H-bonding interactions of surfactant with MCC from FT-IR spectra. It was found that water requirements for pelletization increased linearly with increasing HLB. Crushing load decreased and deformability increased with increasing oil/surfactant ratio. Incorporation of higher HLB surfactants enhanced H-bonding and resulted in faster and more extensive disintegration of MCC as fibrils. Reconstitution was greater at high oil/surfactant ratios and the droplet size of the reconstituted microemulsions was similar to that in the wetting microemulsions. The less hydrophilic ELP with a double bond in the fatty acid showed weaker H-bonding and greater microemulsion reconstitution. Purified ELP gave greater reconstitution than the unpurified grade. Thus, the work demonstrates that the choice of type and quantity of the surfactant used in the formulation of microemulsions containing pellets has an important influence on their production and performance.
Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, 54 124, Greece.
Irini
I
Matsaridou
Panagiotis
P
Barmpalexis
Andrea
A
Salis
Ioannis
I
Nikolakakis
D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004343:Drug Implants / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D014280:Triglycerides / Q000737:chemistry; D014867:Water / Q000737:chemistry
D004343:Drug Implants; D004655:Emulsions; D005227:Fatty Acids; D009821:Oils; D013501:Surface-Active Agents; D014280:Triglycerides; D014867:Water; C022131:cremophor; D011092:Polyethylene Glycols; D002482:Cellulose; C109691:microcrystalline cellulose