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Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0
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Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 July 2024) | Viewed by 12960

Special Issue Editor

Dr. Jolanta Sereikaitė

E-Mail Website
Guest Editor
Department of Chemistry and Bioengineering, Faculty of Fundamental Sciences, Vilnius Gediminas Technical University, Vilnius, Lithuania
Interests: delivery of bioactive compounds; carotenoids; antimicrobial peptides; hydrocolloids; nano/microencapsulation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In the past few decades, bioactive compounds (polyphenols, flavonoids, carotenoids, essential oils, and other compounds) have been extensively studied due to a growing interest concerning their biological and pharmacological properties. However, many bioactive compounds have very low water solubility and are light-, air-, and temperature-sensitive. Micro/nanoencapsulation is an effective approach that can increase the stability, solubility, and bioavailability of bioactive compounds for their application in the food, cosmetic, and pharmaceutical industries. Many materials and encapsulation techniques can be used for the delivery of bioactive compounds. Presently, a variety of novel carrier agents and techniques have been proposed for the development of encapsulated systems. New emerging technologies improve the protection of bioactive compounds against environmental conditions and offer better characteristics of encapsulated products. 

I would like to invite you to submit original research papers or review articles to this Special Issue that address any research topic related to the micro/nanoencapsulation of bioactive compounds.

Dr. Jolanta Sereikaitė
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • micro/nanoencapsulation
  • bioactive compounds
  • encapsulation materials
  • encapsulation techniques
  • controlled release

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Published Papers (7 papers)

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Research

17 pages, 3206 KiB  
Article
Sphaeropsidin A Loaded in Liposomes to Reduce Its Cytotoxicity and Preserve Antifungal Activity Against Candida auris
by Annalisa Buonanno, Maria Michela Salvatore, Antonia Feola, Antonietta Siciliano, Rosa Bellavita, Lorenzo Emiliano Imbò, Marco Guida, Anna Andolfi, Rosario Nicoletti, Angela Maione, Annarita Falanga and Emilia Galdiero
Molecules 2024, 29(24), 5949; https://doi.org/10.3390/molecules29245949 - 17 Dec 2024
Viewed by 803
Abstract
Candida species constitute the most common cause of fungal infections in humans; the emergence of resistance and biofilm formation by Candida species further threaten the limited availability of antifungal agents. Over the past decade, C. auris has caused significant outbreaks worldwide and [...] Read more.
Candida species constitute the most common cause of fungal infections in humans; the emergence of resistance and biofilm formation by Candida species further threaten the limited availability of antifungal agents. Over the past decade, C. auris has caused significant outbreaks worldwide and has emerged as a human pathogenic fungus that causes diseases ranging from superficial to life-threatening disseminated infections. Despite the recent advances in antifungal research, the mechanisms of drug resistance in C. auris remain poorly understood even as its ability to form biofilms poses a significant therapeutic challenge. The purpose of this research was to elucidate the fungal properties of Sphaeropsidin A (SphA), a secondary metabolite derived from Diplodia fungi, with a specific focus on its efficacy against C. auris. This study revealed that SphA and its liposomal encapsulated (SphA-L) form are fungistatic with time-kill kinetics highlighting their efficacy and significantly inhibited the formation of C. auris biofilms. Our investigation into the antifungal mechanism of this drug revealed notable alterations in ROS production and the disruption of the Candida cell cycle. Our findings show that SphA-L impairs key pathogenic traits of C. auris, such as its ability to adhere to human epithelial cell lines, while exhibiting no harmful effects on human cells, highlighting its potential as a future therapeutic agent. In Caenorhabditis elegans infection models, both ShpA and SphA-L displayed effective antifungal activity, significantly reducing the C. auris fungal load and improving nematode survival rates, underscoring their promise as antifungal candidates. Overall, the potent antifungal effects of SphA and SphA-L against C. auris encourage further research. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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11 pages, 2752 KiB  
Article
Encapsulation of ɣ-Aminobutyric Acid Compounds Extracted from Germinated Brown Rice by Freeze-Drying Technique
by Tarinee Nilkamheang, Chanikarn Thanaseelangkoon, Rawinan Sangsue, Sarunya Parisaka, Le Ke Nghiep, Pitchaporn Wanyo, Nitchara Toontom and Kukiat Tudpor
Molecules 2024, 29(21), 5119; https://doi.org/10.3390/molecules29215119 - 30 Oct 2024
Cited by 2 | Viewed by 931
Abstract
Gamma-aminobutyric acid (GABA) from plants has several bioactivities, such as neurotransmission, anti-cancer cell proliferation, and blood pressure control. Its bioactivities vary when exposed to pH, heat, and ultraviolet. This study analyzed the protective effect of the GABA encapsulation technique using gum arabic (GA) [...] Read more.
Gamma-aminobutyric acid (GABA) from plants has several bioactivities, such as neurotransmission, anti-cancer cell proliferation, and blood pressure control. Its bioactivities vary when exposed to pH, heat, and ultraviolet. This study analyzed the protective effect of the GABA encapsulation technique using gum arabic (GA) and maltodextrin (MD) and the freeze-drying method. The impact of different ratios of the wall material GA and MD on morphology, GABA content, antioxidant activity, encapsulation efficiency, process yield, and physical properties were analyzed. Results showed that the structure of encapsulated GABA powder was similar to broken glass pieces of various sizes and irregular shapes. The highest GABA content and encapsulation efficiency were, respectively, 90.77 mg/g and 84.36% when using the wall material GA:MD ratio of 2:2. The encapsulated powder’s antioxidant activity was 1.09–1.80 g of encapsulation powder for each formula, which showed no significant difference. GA and MD as the wall material in a 2:2 (w/w) ratio showed the lowest bulk density. The high amount of MD showed the highest Hausner ratio (HR), and Carr’s index (CI) showed high encapsulation efficiency and process yield. The stability of encapsulated GABA powder can be kept in clear glass with a screw cap at 35 °C for 42 days compared to the non-encapsulated one, which can be preserved for only 18 days under the same condition. In conclusion, this study demonstrated that the freeze-drying process for GABA encapsulation preserved GABA component extracts from brown rice while increasing its potential beneficial properties. Using a wall material GA:MD ratio of 2:2 resulted in the maximum GABA content, solubility, and encapsulation efficiency while having the lowest bulk density. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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19 pages, 658 KiB  
Article
Isolation of Bioactive Compounds (Carotenoids, Tocopherols, and Tocotrienols) from Calendula Officinalis L., and Their Interaction with Proteins and Oils in Nanoemulsion Formulation
by Kamil Haładyn, Aneta Wojdyło and Paulina Nowicka
Molecules 2024, 29(17), 4184; https://doi.org/10.3390/molecules29174184 - 4 Sep 2024
Cited by 2 | Viewed by 1305
Abstract
Calendula officinalis L. has numerous health-promoting properties due to the presence of a large number of lipophilic compounds. Their effective delivery to the body requires the use of an appropriate technique such as emulsification. So, the main purpose of this study was to [...] Read more.
Calendula officinalis L. has numerous health-promoting properties due to the presence of a large number of lipophilic compounds. Their effective delivery to the body requires the use of an appropriate technique such as emulsification. So, the main purpose of this study was to understand how the profile of lipophilic compounds from pot marigold and the pro-health potential are shaped by different types of protein, oil, and drying techniques in o/w nanoemulsion. To obtain this, the profiles of carotenoid compounds and tocols were measured. Additionally, antioxidant potential and the ability to inhibit α-amylase and α-glucosidase were measured. Pea protein emulsion exhibited a higher final content of carotenoid compounds (23.72–39.74 mg/100 g), whereas those with whey protein had stronger α-amylase inhibition (487.70 mg/mL). The predominant compounds in the studied nanoemulsions were β-carotene (between 19% and 40%), followed by α-tocopherol/γ-tocopherol. The type of proteins shaped the health-promoting properties and determined the content of health-promoting compounds. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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22 pages, 5523 KiB  
Article
Elevating Skincare Science: Grape Seed Extract Encapsulation for Dermatological Care
by Maria Leonor Castro, João Azevedo-Silva, Diana Valente, Adriana Machado, Tânia Ribeiro, João Paulo Ferreira, Manuela Pintado, Oscar L. Ramos, Sandra Borges and Sara Baptista-Silva
Molecules 2024, 29(16), 3717; https://doi.org/10.3390/molecules29163717 - 6 Aug 2024
Cited by 7 | Viewed by 4603
Abstract
The skin is the largest organ in the human body and serves multiple functions such as barrier protection and thermoregulation. The maintenance of its integrity and healthy structure is of paramount importance. Accordingly, technological advances in cosmetic sciences have been directed towards optimizing [...] Read more.
The skin is the largest organ in the human body and serves multiple functions such as barrier protection and thermoregulation. The maintenance of its integrity and healthy structure is of paramount importance. Accordingly, technological advances in cosmetic sciences have been directed towards optimizing these factors. Plant-derived ingredients have been explored for their bioactivity profiles and sustainable sources. Grape by-products contain a group of bioactive molecules that display important biological activities. Nonetheless, many of these molecules (e.g., phenolic compounds) are unstable and susceptible to degradation. So, their encapsulation using nano/microsystems (i.e., microdispersions) has been explored as a promising solution. In this work, two grape seed extracts were obtained, one from a single grape variety (GSE-Ov) and another from a mix of five grape varieties (GSE-Sv). These extracts were analysed for their antioxidant and antimicrobial activities, as well as their chemical composition and molecular structure. The extract that showed the most promising properties was GSE-Ov with a DPPH IC50 of 0.079 mg mL−1. This extract was encapsulated in soy lecithin microdispersions coated with pectin, with an encapsulation efficiency of 88.8%. They showed an in vitro release of polyphenols of 59.4% during 24 h. The particles displayed a zeta potential of −20.3 mV and an average diameter of 13.6 µm. Microdispersions proved to be safe under 5 and 2.5 mg mL−1 in HaCaT and HDF cell models, respectively. Additionally, they demonstrated anti-inflammatory activity against IL-1α when tested at 2 mg mL−1. This work enabled the valorisation of a by-product from the wine industry by using natural extracts in skincare products. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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23 pages, 5947 KiB  
Article
Influence of Novel Microcapsulates of Bee Products on Gut Microbiota Modulation and Their Prebiotic and Pro-Adhesive Properties
by Gabriela Kowalska, Justyna Rosicka-Kaczmarek, Karolina Miśkiewicz, Adriana Nowak, Ilona Motyl, Joanna Oracz, Anna Brzozowska, Aleksandra Grzegorczyk and Zuzanna Świniarska
Molecules 2024, 29(12), 2751; https://doi.org/10.3390/molecules29122751 - 9 Jun 2024
Cited by 1 | Viewed by 1348
Abstract
With the aim to obtain controlled-release systems and to preserve the antioxidant, immunomodulatory, and prebiotic activity of the bioactive compounds, microencapsulation of both honeydew honey and royal jelly into biopolymeric microparticles based on rye bran heteropolysaccharides (HPS) was successfully performed. Honeydew honey and [...] Read more.
With the aim to obtain controlled-release systems and to preserve the antioxidant, immunomodulatory, and prebiotic activity of the bioactive compounds, microencapsulation of both honeydew honey and royal jelly into biopolymeric microparticles based on rye bran heteropolysaccharides (HPS) was successfully performed. Honeydew honey and royal jelly microcapsules were prepared by spray-drying method and were characterized in terms of morphology and biological properties. Due to the resistance of the obtained encapsulates to the acidic pH in the stomach and digestive enzymes, the microcapsules showed prebiotic properties positively influencing both the growth, retardation of the dying phase, and the pro-adhesive properties of probiotic bacteria, i.e., Bifidobacterium spp. and lactic acid bacteria. Moreover, as a result of fermentation of the microcapsules of bee products in the lumen of the large intestine, an increased synthesis of short-chain fatty acids, i.e., butyric acid, was found on average by 39.2% in relation to the SCFA concentrations obtained as a result of fermentation of native bee products, thus opening new perspectives for the exploitation of honeydew honey and royal jelly loaded microcapsules for nutraceutical applications. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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23 pages, 8246 KiB  
Article
A Quantitative Re-Assessment of Microencapsulation in (Pre-Treated) Yeast
by Giulia Coradello, Chiara Setti, Roberto Donno, Matilde Ghibaudi, Federico Catalano and Nicola Tirelli
Molecules 2024, 29(2), 539; https://doi.org/10.3390/molecules29020539 - 22 Jan 2024
Viewed by 1871
Abstract
Most hydrophobes easily diffuse into yeast cells, where they experience reduced evaporation and protection from oxidation, thus allowing inherently biocompatible encapsulation processes. Despite a long-standing industrial interest, the effect of parameters such as how is yeast pre-treated (extraction with ethanol, plasmolysis with hypertonic [...] Read more.
Most hydrophobes easily diffuse into yeast cells, where they experience reduced evaporation and protection from oxidation, thus allowing inherently biocompatible encapsulation processes. Despite a long-standing industrial interest, the effect of parameters such as how is yeast pre-treated (extraction with ethanol, plasmolysis with hypertonic NaCl, depletion to cell walls), the polarity of the hydrophobes and the process conditions are still not fully understood. Here, we have developed thorough analytical protocols to assess how the effects of the above on S. cerevisiae’s morphology, permeability, and encapsulation efficiency, using three differently polar hydrophobes (linalool, 1,6-dihydrocarvone, limonene) and three separate processes (hydrophobes as pure ‘oils’, water dispersions, or acetone solutions). The harsher the pre-treatment (depleted > plasmolyzed/extracted > untreated cells), the easier the diffusion into yeast became, and the lower both encapsulation efficiency and protection from evaporation, possibly due to denaturation/removal of lipid-associated (membrane) proteins. More hydrophobic terpenes performed worst in encapsulation as pure ‘oils’ or in water dispersion, but much less of a difference existed in acetone. This indicates the specific advantage of solvents/dispersants for ‘difficult’ compounds, which was confirmed by principal component analysis; furthering this concept, we have used combinations of hydrophobes (e.g., linalool and α-tocopherol), with one acting as solvent/enhancer for the other. Our results thus indicate advantages in using untreated yeast and—if necessary—processes based on solvents/secondary hydrophobes. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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16 pages, 3029 KiB  
Article
Use of Double Gelled Microspheres to Improve Release Control of Cinnamon-Loaded Nanoemulsions
by Esther Santamaría, Alicia Maestro and Carmen González
Molecules 2024, 29(1), 158; https://doi.org/10.3390/molecules29010158 - 27 Dec 2023
Cited by 3 | Viewed by 1316
Abstract
The use of nanoemulsions as encapsulation systems for active ingredients, such as cinnamon oil, has been studied. A surfactant based on polyoxyethylene glycerol esters from coconut/palm kernel oil has been used. The nanoemulsions were obtained by the two most commonly low-energy emulsification methods, [...] Read more.
The use of nanoemulsions as encapsulation systems for active ingredients, such as cinnamon oil, has been studied. A surfactant based on polyoxyethylene glycerol esters from coconut/palm kernel oil has been used. The nanoemulsions were obtained by the two most commonly low-energy emulsification methods, the composition inversion phase (PIC) and the temperature inversion phase (PIT) methods. Nanoemulsions were successfully obtained by both methods, with very small droplet sizes (5–14 nm) in both cases, but a greater stability was observed when the PIT method was used. Nanoemulsions were encapsulated by external gelation using two different polysaccharides, alginate or chitosan, dissolved in the continuous phase of the nanoemulsion. Then, the nanoemulsion was dropped into a bath with a gelling agent. To improve the release control of cinnamon oil and avoid the burst effect, beads prepared with one of the polysaccharides were coated with the second polysaccharide and then gelled again. Double gelled beads were successfully obtained, the core with chitosan and the outer layer (shell) with alginate. SEM images showed the morphology of the single beads presenting high porosity. When the beads were coated, the porosity decreased because the second polysaccharide molecules covered the pre-existing pores. The smoother surface was obtained when this second layer was, in turn, gelled. The release patterns at pH = 2 and pH = 7 were studied. It was observed that the double gelled bead provided a more gradual release, but maintained approximately the same amount of final released oil. The release patterns were fitted to the Korsmeyer-Peppas model. The fitting parameters reflected the effect of the different coating layers, correlating with different diffusion mechanisms according to the bead core and shell materials. Full article
(This article belongs to the Special Issue Recent Advances in Micro- and Nanoencapsulation of Bioactive Compounds 2.0)
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