(76d) Alginate Encapsulation As Drug Targeting Depot System

Authors: 
Tomas, J., University of Chemistry and Technology
Zadrazil, A., University of Chemistry and Technology
Stepanek, F., University of Chemistry and Technology
Targeted drug delivery systems provide better treatment efficiency, less material consumption and less side effects to patients.Currently there are many approaches which explore possibilities of the drug encapsulation and release on demand. Alginate core-shell microcapsulerepresents the type of thedevice, thatamong the otherappears in applicationsranging fromthe food industry tomolecular gastronomy. It can be also used as depot for Active Pharmaceutical Ingredients (APIs) incorporated in the core.

The main aim of this work is to developedthe system based on the alginate core-shell particles capable of API encapsulation and subsequent release.The core-shell micro-capsules where made by laboratory encapsulator BUCHI B-395 Pro.Microcapsules were fabricatedby external gelation, where the coreconsist of vegetable oilinfused with active pharmaceutical ingredient (API) and the shell fromcalcium alginate.Parametric study covering the flow rateof both phases, vibration frequency and voltage with respect to the efficiency of optimal particles preparation was performed. The most influencing parameter isthe flow rate of bothphases. After acquiring optimal shape of the micro-particle by proper parameterssettings, the ibuprofen as model API was incorporated in the particles core.The effect of ibuprofen size and crystallinity was investigated with impact to the particle dissolution kinetics. Different methods of storing of the fabricated microcapsules: (i) drying were or (ii) storing in the liquid state in order to test the storage conditions of the capsules was investigated.Dehydrated particles were further rehydrated andtheir shape was examined before and after the drying process. Dissolution kinetics of rehydrated particles andthe particles stored in liquid state was evaluated and compared.

The dried particles differs in shell thickness and in the stability when rehydrated. Crystallinity of incorporated ibuprofen influenced the dissolution kinetics as well as the thickness of shell and type of the used alginate. Presented method can produce large quantities of uniform particles with consistent properties, and hence, can be used as targeted drug delivery vesicles.