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Delivery Systems of Bioactive Compounds

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

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 8798

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Prof. Dr. Mirela Kopjar

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Guest Editor

Department of Food Technologies, Faculty of Food Technology Osijek, Josip Juraj Strossmayer University of Osijek, HR 31000 Osijek, Croatia
Interests: phenolics; anthocyanins; antioxidants; flavor compounds of fruits and fruit products
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Anita Pichler

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Guest Editor

Faculty of Food Technology Osijek, Josip Juraj Strossmayer University of Osijek, F. Kuhača 18, 31000 Osijek, Croatia
Interests: wine technology; flavor compounds of fruits and fruit products; membrane processing; stability of phenolic compounds
Special Issues, Collections and Topics in MDPI journals

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Dear Colleagues,

Healthy and naturally functional food products and/or additives which provide both nutritional and health-related benefits are an emerging trend in the food industry. Bioactive components such as polyphenols, proanthocyanidins, anthocyanins, glucosinolates, carotenoids, vitamins and others are components with recognized disease-preventative properties. These properties include anti-carcinogenic functionality, risk reduction and prevention of cardiovascular, neurodegenerative and diabetic diseases, as well as many other serious health issues which are all of the increasing importance throughout the world. Many fruits, vegetables and grains are sources of those bioactive compounds; however, the problem can be their instability or that they are not necessarily at significant, health-relevant concentrations or in highly bioavailable forms. Currently, many studies have been conducted with the aim of formulating different delivery systems in order to achieve higher stability of those bioactive components and their controlled release in foods or in the human organism. On the other hand, those delivery systems can be used to improve the quality of food products, especially the improvement of antioxidant potential, color or stability of the products. Formulation of adequate delivery systems (hydrogels, liposomes or dried forms) depends on the properties of bioactive compounds and polymers that were used for the formulation of delivery systems. Conditions under which those delivery systems were prepared are also of high importance, and so many different factors have to be considered to formulate successful delivery systems of bioactive compounds.

Prof. Dr. Mirela Kopjar
Prof. Dr. Anita Pichler
Guest Editors

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Keywords

bioactive compounds
delivery systems
stability
health benefits
food quality

Published Papers (5 papers)

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Research

27 pages, 4281 KiB

Open AccessArticle

In Vitro Bioaccessibility Assessment of Phenolic Compounds from Encapsulated Grape Pomace Extract by Ionic Gelation

by Josipa Martinović, Jasmina Lukinac, Marko Jukić, Rita Ambrus, Mirela Planinić, Gordana Šelo, Ana-Marija Klarić, Gabriela Perković and Ana Bucić-Kojić

Molecules 2023, 28(13), 5285; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28135285 - 07 Jul 2023

Cited by 1 | Viewed by 1240

Abstract

Grape pomace is a by-product of winemaking characterized by a rich chemical composition from which phenolics stand out. Phenolics are health-promoting agents, and their beneficial effects depend on their bioaccessibility, which is influenced by gastrointestinal digestion. The effect of encapsulating phenol-rich grape pomace extract (PRE) with sodium alginate (SA), a mixture of SA with gelatin (SA-GEL), and SA with chitosan (SA-CHIT) on the bioaccessibility index (BI) of phenolics during simulated digestion in vitro was studied. A total of 27 individual phenolic compounds (IPCs) were quantified by UHPLC. The addition of a second coating to SA improved the encapsulation efficiency (EE), and the highest EE was obtained for SA-CHIT microbeads (56.25%). Encapsulation affected the physicochemical properties (size, shape and texture, morphology, crystallinity) of the produced microbeads, which influenced the delivery of phenolics to the intestine and their BI. Thus, SA-GEL microbeads had the largest size parameters, as confirmed by scanning electron microscopy (SEM), and the highest BI for total phenolic compounds and IPCs (gallic acid, 3,4-dihydroxybenzoic acid and o-coumaric acid, epicatechin, and gallocatechin gallate) ranged from 96.20 to 1011.3%. The results suggest that encapsulated PRE has great potential to be used as a functional ingredient in products for oral administration. Full article

(This article belongs to the Special Issue Delivery Systems of Bioactive Compounds)

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13 pages, 5739 KiB

Open AccessArticle

Dual Drug-Loaded Nanoliposomes Encapsulating Curcumin and 5-Fluorouracil with Advanced Medicinal Applications: Self-Monitoring and Antitumor Therapy

by Yu-Shi Liu, Jia-Wen Song, Wen-Xiao Zhong, Ming-Hao Yuan, Yu-Rou Guo, Cheng Peng, Li Guo and Yi-Ping Guo

Molecules 2023, 28(11), 4353; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28114353 - 25 May 2023

Viewed by 1552

Abstract

Due to the presence of physiological barriers, it is difficult to achieve the desired therapeutic efficacy of drugs; thus, it is necessary to develop an efficient drug delivery system that enables advanced functions such as self-monitoring. Curcumin (CUR) is a naturally functional polyphenol whose effectiveness is limited by poor solubility and low bioavailability, and its natural fluorescent properties are often overlooked. Therefore, we aimed to improve the antitumor activity and drug uptake monitoring by simultaneously delivering CUR and 5-Fluorouracil (5-FU) in the form of liposomes. In this study, dual drug-loaded liposomes (FC–DP–Lip) encapsulating CUR and 5-FU were prepared by the thin-film hydration method; their physicochemical properties were characterized; and their biosafety, drug uptake distribution in vivo, and tumor cell toxicity were evaluated. The results showed that the nanoliposome FC–DP–Lip showed good morphology, stability, and drug encapsulation efficiency. It showed good biocompatibility, with no side effects on zebrafish embryonic development. In vivo uptake in zebrafish showed that FC–DP–Lip has a long circulation time and presents gastrointestinal accumulation. In addition, FC–DP–Lip was cytotoxic against a variety of cancer cells. This work showed that FC–DP–Lip nanoliposomes can enhance the toxicity of 5-FU to cancer cells, demonstrating safety and efficiency, and enabling real-time self-monitoring functions. Full article

(This article belongs to the Special Issue Delivery Systems of Bioactive Compounds)

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10 pages, 2110 KiB

Open AccessCommunication

Dry Nutrition Delivery System Based on Defatted Soybean Particles and Its Application with β-Carotene

by Chunyu Wu, Xuewen Ouyang, Xiaoya Zhou, Xiaofei Li, Hongbo Li, Wenying Li, Cuixiang Wan, Bo Yu, Sobhy El-Sohaimy and Zhihua Wu

Molecules 2023, 28(8), 3429; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28083429 - 13 Apr 2023

Cited by 1 | Viewed by 1104

Abstract

Many nutrition delivery systems (NDSs) have been developed for the encapsulation, protection, and delivery of bioactive compounds, such as β-carotene. Most of those systems were prepared in solution, which is inconvenient for transportation and storage in the food industry. In the present work, we constructed an environmentally friendly dry NDS based on defatted soybean particles (DSPs) by milling a β-carotene-DSP mixture. The loading efficiency of the NDS reached 89.0%, and the cumulative release rate decreased from 15.1% (free β-carotene) to 6.0% within 8 h. The stability of β-carotene in the dry NDS was found to have increased in a thermogravimetric analysis. Stored for 14 days at 55 °C or under UV irradiation, the retaining rates of β-carotene in the NDS increased to 50.7% and 63.6%, respectively, while they were 24.2% and 54.6% for the free samples. The bioavailability of β-carotene was improved by the NDS too. The apparent permeability coefficient of the NDS reached 1.37 × 10⁻⁶ cm/s, which is 12 times that of free β-carotene (0.11 × 10⁻⁶ cm/s). Besides being environmentally friendly, the dry NDS can facilitate carriage, transportation, or storage in the food industry, and similar to other NDSs, it improves the stability and bioavailability of nutrients. Full article

(This article belongs to the Special Issue Delivery Systems of Bioactive Compounds)

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11 pages, 2394 KiB

Open AccessArticle

Analgesic Characteristics of NanoBEO Released by an Airless Dispenser for the Control of Agitation in Severe Dementia

by Damiana Scuteri, Laura Rombolà, Takafumi Hayashi, Chizuko Watanabe, Shinobu Sakurada, Kengo Hamamura, Tsukasa Sakurada, Paolo Tonin, Giacinto Bagetta, Luigi A. Morrone and Maria Tiziana Corasaniti

Molecules 2022, 27(15), 4987; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27154987 - 05 Aug 2022

Cited by 5 | Viewed by 1835

Abstract

Chronic pain is one of the most common causes of the need for clinical evaluation, acquiring more importance in the elderly with cognitive impairment. Reduced self-reporting capabilities cause unrelieved pain contributing to the development of agitation. Safe and effective pain treatment can afford the management of agitation without the serious increase in death risk associated with neuroleptics. To this aim, the essential oil of bergamot (BEO), proven by rigorous evidence to have strong preclinical anti-nociceptive and anti-allodynic properties, has been engineered (NanoBEO, patent EP 4003294) to allow randomized, double-blind, placebo-controlled trials (BRAINAID, NCT04321889). The present study: (1) assesses the analgesic effects of a single therapeutic dose of NanoBEO, as supplied by an airless dispenser for clinical translation, in models of inflammatory, neuropathic, and sensitization types of pain relevant to clinic; (2) provides a dose–response analysis of the efficacy of NanoBEO on scratching behavior, a typical behavioral disturbance occurring in dementia. A single therapeutic dose of NanoBEO confirms efficacy following thirty minutes pre-treatment with capsaicin and on the central sensitization phase induced by formalin. Moreover, it has an ID50 of 0.6312 mg and it is efficacious on static and dynamic mechanical allodynia. Altogether, the gathered results strengthen the potential of NanoBEO for clinical management of pain and agitation. Full article

(This article belongs to the Special Issue Delivery Systems of Bioactive Compounds)

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16 pages, 1696 KiB

Open AccessArticle

Apple Fibers as Carriers of Blackberry Juice Polyphenols: Development of Natural Functional Food Additives

by Ivana Buljeta, Mario Nosić, Anita Pichler, Ivana Ivić, Josip Šimunović and Mirela Kopjar

Molecules 2022, 27(9), 3029; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27093029 - 08 May 2022

Cited by 9 | Viewed by 2297

Abstract

Blackberry polyphenols possess various health-promoting properties. Since they are very sensitive to environmental conditions such as the presence of light, oxygen and high temperatures, the application of such compounds is restricted. Fibers are recognized as efficient carriers of polyphenols and are often used in polyphenols encapsulation. In the present study, the ability of apple fiber to adsorb blackberry juice polyphenols was examined. Freeze-dried apple fiber/blackberry juice complexes were prepared with different amounts of fibers (1%, 2%, 4%, 6%, 8% and 10%) and a constant amount of blackberry juice. Polyphenol profile, antioxidant activity, inhibition of the α-amylase, color parameters, as well as the IR spectra, of the obtained complexes were assessed. The results showed a negative effect of higher amounts of fiber (more than 2%) on the adsorption of polyphenols and the antioxidant activity of complexes. With the proper formulation, apple fibers can serve as polyphenol carriers, and thus the application as novel food additives can be considered. Full article

(This article belongs to the Special Issue Delivery Systems of Bioactive Compounds)

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