Title : Oral Delivery of Insulin using Nano-emulsion Approach


Authors : Mohammad Shariare, Dewan Reza, Hadiya Jannat, Meher Nigar, Salma Khan, Marcel de Matas,

Abstract : Purpose Control of hyperglycemia in diabetic patients greatly depend on patient compliance and stability of insulin.The stability and bioavailability of insulin, when formulated in an oral dosage form, has presented to be the greatest drawback in optimal diabetic control owing to several chemical, enzymatic and absorption barriers.The aim of this study was to prepare a suitable drug carrier for (oral insulin delivery system) insulin and to understand the impact of processing conditions on the characteristics of the insulin nanoemulsion. Methods Dextran Sulfate, Sodium Alginate, Span 80, Calcium Carbonate, Paraffin Oil (liquid) and Acetic Acid were used in this study. Human rDNA Insulin (26.31 IU/mg) was used as the core drug. The preparation of nanoemulsion containing the drug core was achieved by ionic gelation process(Figure 1) following a full factorial experimental design where three process parameters (stirring rate, sonication time and emulsification rate) were used at two levels (H= high; L=low). Following successful emulsification, pellets containing insulin nanoparticles were recovered by centrifugation and characterized using Malvern Zetasizer Nano Zs90 to obtain particle size and size distribution data.The entrapment efficiency of nanoemulsion batches was also calculated. Results Results showed that the insulin particles obtained were below 300nm with unimodal size distribution, when characterized using Malvern Zetasizer. It is observed that nanoemulsion batch processed at high stirring rate (800 rpm) generates smaller insulin particles (41 nm ± 1) compared to batches processed at low stirring rate (600 rpm) (63 nm ± 0.5). This is probably due to shear force at high stirring rate breaks up larger particles more compared to low stirring rate. It is also observed that longer sonication time (40 minutes) produces small sized insulin particles (63 ± 1) compared to batches processed at shorter sonication time (30minutes) (72 ± 4). This may be linked to breaking up of particles at high intensity of ultrasound waves. Entrapment efficiency of insulin nanoparticles was influenced by the emulsification rate. Results suggest that high entrapment of insulin was observed for batches processed at low emulsification rate. Conclusion The optimum level of processing conditions was identified for the preparation of insulin nanoemulsion. Results suggest that it is possible to control the particle size and size distribution of insulin nanoparticles by controlling the processing conditions.


Journal : Volume : Year : 2015 Issue :
Pages : City : Orlando, Florida Edition : Editors :
Publisher : AAPS annual meeting and exposition , 2015 ISBN : Book : Chapter :
Proceeding Title : American Association of Pharmaceutical scientists (AAPS) annual Meeting and Exposition, USA. Institution : Issuer : Number :