Abstract
The importance of interfacial interactions affecting drug release from O/W submicron emulsions has been demonstrated. In this study, the effect of temperature (25-40 ° C) and cosurfactant concentration on the release of lidocaine from 30% sesame oil in water submicron emulsions is evaluated. All emulsions contained three percent of a nonionic surfactant (HLB = 10) and were prepared using the Microfluidizer® device. The cosurfactant, sodium lauryl sulfate (SLS), was added in concentrations ranging from zero to one percent and was used to manipulate the O/W interfacial adsorption of lidocaine. Increased interfacial adsorption of lidocaine is reflected by greater L values and correspondingly lower drug release rates in vitro as measured by free drug release across a semipermeable membrane. Increasing the SLS concentration does increase L and decrease the drug release rate. A linear estimation is developed to quantify this phenomena. The thermal effects are biphasic, exhibiting a peak L value(minimum release rate) at 30 °C. Relevant mechanisms involving temperature dependent hydrogen bonding and mobility changes are proposed to explain these observations.
- Received May 22, 1987.
- Accepted October 14, 1987.
- Copyright © Parenteral Drug Association. All rights reserved.
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