Encapsulation of active pharmaceutical ingredients in lipid micro/nanoparticles for oral administration by spray-cooling

Nanoencapsulation via spray cooling (also known as spray chilling and spray congealing) has been used with the aim to improve the functionality, solubility, and protection of drugs; as well as to reduce hygroscopicity; to modify taste and odor to enable oral administration; and many times to achieve a controlled release profile. It is a relatively simple technology, it does not require the use of low-cost solvents (mostly associated to toxicological risk), and it can be applied for lipid raw materials as excipients of oral pharmaceutical formulations. The objective of this work was to revise and discuss the advances of spray cooling technology, with a greater emphasis on the development of lipid micro/nanoparticles to the load of active pharmaceutical ingredients for oral administration.This research was funded by the Portuguese Science and Technology Foundation (FCT/MCT) and European Funds (PRODER/COMPETE), under the project reference UIDB/04469/2020 (strategic fund), co-financed by FEDER, under the Partnership Agreement PT2020, granted to Eliana B. Souto. This work was also supported by the National Science Centre within the MINIATURA 4 for a single research activity carried out by Aleksandra Zieli ´nska (grant no: 2020/04/X/ST5/00789), and by the Institute of Human Genetics, Polish Academy of Sciences by the internal grant for the implementation of a single scientific activity.info:eu-repo/semantics/publishedVersio

Morphology, Stability, and Application of Lycopene Microcapsules Produced by Complex Coacervation

The interest in lycopene has increased in recent years due to studies that associate it with the reduction in risk of developing cardiovascular diseases and cancer. However, due to its high degree of unsaturation, this carotenoid is inclined to isomerize and oxidize during processing and storage, making it difficult to use in the food industry. Microencapsulation can improve this situation, increasing its stability and making incorporation into food formulations possible. Thus, the aim of this study was to microencapsulate lycopene by complex coacervation using gelatin and gum Arabic as the encapsulating agents. The microcapsules were evaluated based on the encapsulation efficiency and their morphology and then submitted to a stability test and applied in cake making. Most of the systems studied presented spherical microcapsules with defined walls. The encapsulation efficiency values were above 90%, and the average diameter of the capsules ranged from 61 to 144 μm. The stability test showed that microencapsulation offered greater protection to the lycopene as compared to its free form. The application of nonfreeze dried coacervated microcapsules in cake making was satisfactory, but the color transference was low when freezedried coacervated microcapsules were used

Production and properties of casein hydrolysate microencapsulated by spray drying with soybean protein isolate

The aim of this work was to encapsulate casein hydrolysate by spray drying with soybean protein isolate (SPI) as wall material to attenuate the bitter taste of that product. Two treatments were prepared: both with 12 g/100 g solids and containing either two proportions of SPI: hydrolysate (70:30 and 80:20), called M1 and M2, respectively. The samples were evaluated for morphological characteristics (SEM), particle size, hygroscopicity, solubility, hydrophobicity, thermal behavior and bitter taste with a trained sensory panel using a paired-comparison test (non-encapsulated samples vs. encapsulated samples). Microcapsules had a continuous wall, many concavities, and no porosity. Treatments M1 and M2 presented average particle sizes of 11.32 and 9.18 mu m, respectively. The wall material and/or the microencapsulation raised the hygroscopicity of the hydrolysate since the free hydrolysate had hygroscopicity of 53 g of water/100 g of solids and M1 and M2 had 106.99 and 102.19 g of water/100 g of solids, respectively. However, the hydrophobicity decreases, the absence of a peak in encapsulated hydrolysates, and the results of the panel sensory test considering the encapsulated samples less bitter (p < 0.05) than the non-encapsulated, showed that spray drying with SPI was an efficient method for microencapsulation and attenuation of the bitter taste of the casein hydrolysate. (c) 2008 Elsevier Ltd. All rights reserved.Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)[051 56674-3

Encapsulation of an astaxanthin-containing lipid extract from shrimp waste by complex coacervation using a novel gelatin-cashew gum complex

In the present work, the suitability of cashew gum for forming coacervates with gelatin and encapsulating a lipid extract from shrimp waste was studied. Gelatin and cashew gum formed coacervates at pHs ranging from 4 to 4.5. They were spherical in shape and tended to aggregate and form clusters at pH 4-4.2, whereas they were formless at pH 4.3-4.5. The coacervates were able to encapsulate the lipid extract (astaxanthin encapsulation efficiency 59.9 ± 0.01%), forming multinucleated, polymorphic microcapsules with an average size of 32.7 ± 9.7 μm. An accelerated stability study (43 days/36 ± 1 °C/80% relative humidity) revealed an improvement in astaxanthin stability as a result of encapsulation. The microcapsules, which showed a water solubility of 28.6 ± 4.7%, dispersed well in plain yogurt, selected as a food matrix to evaluate their coloring capacity. The color provided to the product by the encapsulated lipid extract was different in hue to that of the non-encapsulated one, showing higher chromaticity at comparable concentrations. A trained sensory panel confirmed the improvement in coloring capacity achieved through encapsulation, although no differences in odor were found.Spanish Ministry of Economy and Competitiveness for financial support through projects AGL2011-27607 and 201370E036, the Spanish Ministry of Education, Culture and Sport (CAS14/00331) ; the São Paulo Research Foundation (FAPESP) for T.A. Comunian’s fellowship (Process 2013/25862-5)Peer Reviewe

Physico-chemical properties, stability, and potential food applications of shrimp lipid extract encapsulated by complex coacervation

Lipid extract from shrimp cephalothorax is a potential food coloring owing to its intense red color. However, it presents some drawbacks, such as its characteristic odor, astaxanthin instability, and difficult dosage and manipulation. The present work is an attempt to overcome these problems by means of complex coacervation encapsulation using gelatin and gum arabic as wall materials. Round molecules in which the lipid extract was efficiently encapsulated in the form of multiple droplets were obtained. The resulting microcapsules stabilized by freeze-drying had good properties with a view to their application as food coloring, owing to their intense red color, improved astaxanthin stability, and low water activity, water solubility, and hygroscopicity. The coloring capacity and sensory properties were evaluated when added to yogurt and a gellified fish product. For yogurt, a trained sensory panel determined that encapsulation effectively reduced the characteristic odor, whereas the coloring capacity was improved, as compared to non-encapsulated lipid extract. For the gellified fish product, no sensory improvement was observed, but the encapsulated lipid extract provided an attractive, uniform color.The authors wish to thank the Spanish Ministry of Economy and Competitiveness for financial support through projects AGL2011-27607 and AGL2014-52825, as well as for J. Gómez-Estaca’s “Juan de la Cierva” fellowship; the Spanish Ministry of Education, Culture and Sport for J. Gómez-Estaca’s “José Castillejo” fellowship; and the São Paulo Research Foundation (FAPESP) for T.A. Comunian’s fellowship (Process 2013/25862-5).Peer reviewe

Extending the use for food applications of a functional lipid extract from shrimp through complex coacervation encapsulation

Póster presentado a la 31st EFFoST International Conference titulada: Food Science and Technology Challenges for the 21st Century - Research to Progress Society, celebrada en Sitges (España) del 13 al 16 de noviembre de 2017.Currently, consumers demand food products with a low amount of additives. This is especially true in the case of synthetic additives, so that research on new alternatives from natural origin is of great interest. The lipid extract from shrimp cephalothorax (LES) is a natural food ingredient with potential applications as food coloring and functional ingredient, due to the presence of polyunsaturated fatty acids (including DHA and EPA), tocopherol and astaxanthin. However, the lipid extract is not easily dispersed in aqueous matrices, present an intense shrimp odor and is unstable to oxidation reactions. In the present work, the LES was encapsulated by complex coacervation using a gelatin-gum arabic complex in order solve these problems and expand its use as food ingredient. Microcapsules round in shape measuring 46.9 ± 12.9 µm in which the lipid extract was efficiently encapsulated (93.5 ± 0.01%) were formed. Once stabilized by freeze-drying, the capsules lost their structure; however, it was fully recovered after reconstitution in water. The microcapsules showed low water solubility (9.6 ± 1.5%), indicating a strong interaction between gelatin and gum arabic. The microcapsules were submitted to an accelerated stability study (43 days, 36 °C, 80% RH), using the free oil as control, revealing an improvement in astaxanthin stability as a result of encapsulation, as well as negligible lipid oxidation by TBARS. Two different food matrices were chosen to evaluate the application of encapsulated LES, namely yogurt and gellified fish product, providing them with an attractive orange color. Furthermore, in the case of yogurt, encapsulation efficiently reduced the characteristic shrimp odor imparted by the lipid extract, as determined by a trained sensory panel. From the results, it is concluded that microencapsulation is an effective way of extending the use of LES for food applications.This work has been financed by the Spanish MINECO projects CRUSTAVAL AGL2011-27607 and HALOFISH AGL2014-52825.Peer Reviewe

Microencapsulation of casein hydrolysate by complex coacervation with SPI/pectin

The aim of this work was to encapsulate casein hydrolysate by complex coacervation with soybean protein isolate (SPI)/pectin. Three treatments were studied with wall material to core ratio of 1:1, 1:2 and 1:3. The samples were evaluated for morphological characteristics, moisture, hygroscopicity, solubility, hydrophobicity, surface tension, encapsulation efficiency and bitter taste with a trained sensory panel using a paired comparison test. The samples were very stable in cold water. The hydrophobicity decreased inversely with the hydrolysate content in the microcapsule. Encapsulated samples had lower hygroscopicity values than free hydrolysate. The encapsulation efficiency varied from 91.62% to 78.8%. Encapsulated samples had similar surface tension, higher values than free hydrolysate. The results of the sensory panel test considering the encapsulated samples less bitter (P < 0.05) than the free hydroly-state, showed that complex coacervation with SPI/pectin as wall material was an efficient method for microencapsulation and attenuation of the bitter taste of the hydrolysate. (C) 2009 Elsevier Ltd. All rights reserved.FAPESP (Fundacao de Amparo a Pesquisa do Estado de Sao Paulo)[05/56674-3

Assessment of production efficiency, physicochemical properties and storage stability of spray-dried chlorophyllide, a natural food colourant, using gum Arabic, maltodextrin and soy protein isolate-based carrier systems

P>The aim of this research was to study spray drying as potential action to protect chlorophyllide from environmental conditions for shelf-life extension and characterisation of the powders. Six formulations were prepared with 7.5 and 10 g of carrier agents [gum Arabic (GA), maltodextrin (MA) and soybean protein isolate (SPI)]/100 mL of chlorophyllide solutions. The powders were evaluated for morphological characteristics (SEM), particle size, water activity, moisture, density, hygroscopicity, cold water solubility, sorption isotherms, colour and stability, during 90 days. All the powders were highly soluble, with solubility values around 97%. A significant lower hygroscopicity was observed for GA powders, whilst the lower X(m) values obtained by GAB equation fitting of the sorption isotherms was observed for the 7.5 g MA/100 mL samples. All formulations, but the 1 (7.5 g SPI/100 mL of chlorophyllide), provided excellent stability to the chlorophyllide during 90 days of storage even at room temperature.FAPESP[07/02981-8

Effect of different polysaccharides and crosslinkers on echium oil microcapsules

Microencapsulation by complex coacervation using gelatin and arabic gum (AG) as wall materials and transglutaminase for crosslinking is commonly used. However, AG is only produced in a few countries and transglutaminase is expensive. This work aimed to evaluate the encapsulation of echium oil by complex coacervation using gelatin and cashew gum (CG) as wall materials and sinapic acid (S) as crosslinker. Treatments were analyzed in relation to morphology, particle size, circularity, accelerated oxidation and submitted to different stress conditions. Rounded microcapsules were obtained for treatments with AG (45.45 μm) and microcapsules of undefined format were obtained for treatments with CG (22.06 μm). The S incorporation for 12 h improved the oil stability by three fold compared to oil encapsulated without crosslinkers. Treatments with CG and S were resistant to different stress conditions similar to treatments with AG and transglutaminase, making this an alternative for delivery/application of compounds in food products.The authors thank Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) for the scholarship for T.A. Comunian (Process 2013/25862-5) and for financial support (Process 2012/08058-5) and De Wit Speciality Oils for the echium oil donation. C.S. Favaro-Trindade thanks Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) for the productivity grant (306708/2015-9)Peer Reviewe