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Article in Press as accepted by the International Journal of Pharmaceutics, Volume 409, Issues 1-2, 16 May 2011, Pages 209-215

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Table of contents

Abstract 72

Keywords 72

List of Abbreviations 72

1. Introduction 72

2. Material and methods 73

2.1 Materials 73

2.2 Preparation of lipid drug carriers 73

2.3 Determination of particle size distribution 73

2.4 Morphological analysis 73

2.5 Determination of entrapment efficacy 73

2.6 Stability testing 74

2.7 Statistical analysis 74

3. Results 74

3.1 Calibration curve for size determination 74

3.2 Characterization of formulations 74

3.3 A 14 day entrapment efficacy study of Pheroid™ vesicle formulations 75

4. Discussion 76

5. Conclusion 77

6. Acknowledgements 77

7. References 77

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List of Figures

Figure 1 Micrographs of Pheroid™ vesicles and liposomes, with and without MQ stained with Nile Red. The initial formulations are compared with micrographs at three months at the different temperatures. Spherical structures of Pheroid™ vesicles are clearly visible in red in the images.

Bilayers of the liposomes without MQ are red surrounding a black aqueous volume with only a slight change in size at month three.

Unilaminer liposomes loaded with MQ can be seen with the initial formulation, but only lipid structures with crystals after stability testing with small oil drops visible at 5°C.

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Figure 2 Entrapment efficacy and span of Pheroid™ vesicles (A) and liposomes (B) loaded with mefloquine. Bars represents entrapment efficacy and lines span. Results are shown as mean ± SEM (n=2). *Highly significant difference in entrapment efficacy compared to the initial values.

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Figure 4 Entrapment efficacy and span of Pheroid™ vesicles loaded with mefloquine. Bars represent entrapment efficacy and lines span.

Results are shown as mean ± SEM (n=2). PF1 – loaded with MQ during manufacturing and PF2 – MQ added to Pheroid™ vesicles after manufacturing.

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List of Tables

Table 1 Size and pH of PheroidTM and liposomes at different temperature over three months. Results are presented as mean ± SEM (n=2) in μm and p-values was determine by Tukey’s post hoc test.

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Table 2 The pH of mefloquine loaded formulation over three months at different temperatures. Results are presented as mean ± SEM (n=2) and p- values were determined by Tukey’s post hoc test. All of the vlues were statistically significant (p≤0.05) when compared with the initial value, except for the values marked.

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