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| Author(s): |
Lucimara Benelli
Total Authors: 1
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| Document type: | Doctoral Thesis |
| Press: | Ribeirão Preto. |
| Institution: | Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto (PCARP/BC) |
| Defense date: | 2016-02-19 |
| Examining board members: |
Wanderley Pereira de Oliveira;
Gustavo Cesar Dacanal;
Priscyla Daniely Marcato Gaspari;
Luiz Fernando Lopes Guimaraes
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| Advisor: | Wanderley Pereira de Oliveira |
| Abstract | |
This work aimed to investigate coating/agglomeration process of herbal extracts in fluidized bed with top spray atomization in order to improve stability of bioactive compounds and their pharmacotechnical properties. Crystal sugar granules, sugar and microcrystalline cellulose pellets, microcrystalline cellulose, cassava flour and rice granules, were used as seed particles. First, coating/agglomeration processes with cassava flour and sugar pellets as seed particles and feed compositions loaded with herbal extract of Rosmarinus officinalis (rosemary) were investigated. Fluidized bed performance was evaluated based on coating efficiency and agglomeration percentage. Products were characterized by determining the particle sizes, flow properties and retention of bioactive compounds (polyphenols). Herbal compositions were also spray dried to compare the product generated by both processes. Results showed that coating efficiency and percentage of agglomeration depend on seed particles and feed compositions physicochemical properties. The viscosity of the feed formulations and the interaction with seed particles influenced process performance. Fluidized bed granules exhibited higher efficiency of coating/agglomeration, higher retention of bioactive compounds and better flow properties than the powder obtained by spray drying. Microcrystalline cellulose pellets of different sizes were used as seed particles to investigate system dynamic during fluidized bed encapsulation/agglomeration by analysis of pressure fluctuation signals associated with growth kinetics and process performance. Two distinct operating modes were investigated: intermittent (interrupting the composition atomization for a specific period of time in order to reduce the system humidity) and continuous (without interruption of feed atomization). The increase in the agglomeration percentage to a certain value during the processes caused an increase in the standard deviation of the amplitude of the pressure fluctuations signals while the system remained stable, indicative of slight change on solids circulation patterns. However, the standard deviation of the amplitude of the pressure fluctuations signals tended to decrease when agglomeration percentage reached a value able to affect significantly the system stability, in which agglomerates growth tended to cause the system collapse. This behavior was most evident for small size seed particles and continuous operating mode. The changes in the standard deviation of the amplitude of pressure fluctuation signals showed strong evidence that this method would be able to detect changes in system dynamics and can be a useful tool for process control and system monitoring. Different operational variables, feed flow rate and fluidizing air flow rate, were used to analyze fluidized bed performance using intermittent mode and microcrystalline cellulose pellets as seed particles. Operating conditions that promoted higher coating efficiency and lower percentage of agglomeration were selected to be used in processes to evaluated different feed compositions loaded with herbal extract and encapsulating agents of two types, Arabic gum and whey protein, associated with stearic acid and poloxamer 407. Process performance was evaluated by coating efficiency and percentage of agglomeration. Products were evaluated by flow properties and the retention of bioactive compounds: cafeic acid, rosmarinic acid, carnosol and carnosic acid, determined by HPLC-DAD. Both compositions presented high coating efficiency and retention of bioactive compounds. Products were submitted to accelerated and long-term stability tests. Bioactive compounds of all granules suffered degradation during the tests with total loss of carnosol and carnosic acid. In vitro gastrointestinal digestion assays were carried out with the two types of products obtained. The concentrations of caffeic and rosmarinic acids did not change significantly during the digestion process, both in the simulation of gastric as intestinal conditions. The carnosol and carnosic acid have undergone total loss at the end of the intestinal phase in both types of products. The two types of granules with different encapsulating agents, were coated with Opadry® II aiming to provide greater stability against degradation of bioactive compounds. Higher protection of carnosol occurred in the granules containing gum Arabic subjected to long term stability test at 30 ° C, 75% RH, but this protection was not effective for any of the granules subjected to accelerated stability testing at 40 °C. The results provide strong evidence of the feasibility of the fluidised bed as a promising method for production of encapsulated phytopharmaceutical compositions with adequate pharmacotechnical and physicochemical properties. (AU) | |
| FAPESP's process: | 12/00562-6 - Fluidized bed encapsulation of herbal extracts |
| Grantee: | Lucimara Benelli |
| Support Opportunities: | Scholarships in Brazil - Doctorate |