Unlocking the Potential of Natural Products—Advances in Drug Formulation, Delivery, and Biological Activity

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 6294

Special Issue Editors


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Guest Editor
Department of Clinical Pharmacy, Faculty of Pharmacy, Lithuanian University of Health Sciences, Sukileliai Avenue 13, LT-50161 Kaunas, Lithuania
Interests: natural compounds; plant extract; analytical chemistry; pharmaceutical development; drug delivery

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Guest Editor
11 Laboratory of Biochemistry, Neuroscience Institute, Lithuanian University of Health Sciences, Eiveniu Str. 4, LT-50162 Kaunas, Lithuania
2. Department of Drug Technology and Social Pharmacy, Lithuanian University of Health Sciences, Sukileliu St. 13, LT-50162 Kaunas, Lithuania
Interests: phenolic compounds; antioxidants; antimicrobial; anticancer; in vitro
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Special Issue Information

Dear Colleagues,

In recent years, there has been an increasing focus on biologically active compounds due to their antimicrobial, anti-inflammatory and antioxidant activity. Products of natural origin are produced and used in various dosage forms depending on the intended use. Natural active compounds often have poor solubility, which can limit their use in the manufacture of pharmaceutical products. The isolation of biologically active compounds from plant material and the improvement of their solubility for efficient application in the production of pharmaceutical forms is one of the important scientific challenges of today. Proper solvent selection and extraction methods can improve the solubility of biologically active compounds. Environment- and human-friendly technologies are increasingly being used to extract biologically active compounds from plant-based raw materials.

This Special Issue aims to obtain up-to-date data on methods for the extraction and quality analysis of biologically active compounds, their biological activity, incorporation into pharmaceutical forms, and in vitro release studies of active compounds.

We invite scientists to submit their original research or review articles for this Special Issue, which will represent a collection of current research on phenolic compounds recovered from plants and their potential application in pharmaceuticals.

We look forward to receiving your contributions.

Prof. Dr. Kristina Ramanauskienė
Prof. Dr. Daiva Majienė
Guest Editors

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Keywords

  • bioactive compounds
  • phenolic compounds
  • pharmaceutical development
  • natural extracts
  • in vitro
  • phytochemical characterization
  • pharmacological activity

Published Papers (4 papers)

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Research

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18 pages, 3723 KiB  
Article
Chemical Composition and Insulin-Resistance Activity of Arginine-Loaded American Cranberry (Vaccinium macrocarpon Aiton, Ericaceae) Leaf Extracts
by Oleh Koshovyi, Inna Vlasova, Heleriin Laur, Ganna Kravchenko, Oksana Krasilnikova, Sebastian Granica, Jakub P. Piwowarski, Jyrki Heinämäki and Ain Raal
Pharmaceutics 2023, 15(11), 2528; https://doi.org/10.3390/pharmaceutics15112528 - 25 Oct 2023
Viewed by 864
Abstract
One of the key pathogenetic links in type 2 diabetes mellitus (T2DM) is the formation of insulin resistance (IR). Besides a wide selection of synthetic antidiabetic drugs, various plant-origin extracts are also available to support the treatment of T2DM. This study aimed to [...] Read more.
One of the key pathogenetic links in type 2 diabetes mellitus (T2DM) is the formation of insulin resistance (IR). Besides a wide selection of synthetic antidiabetic drugs, various plant-origin extracts are also available to support the treatment of T2DM. This study aimed to investigate and gain knowledge of the chemical composition and potential IR correction effect of American cranberry (Vaccinium macrocarpon Aiton) leaf extracts and formulate novel 3D-printed oral dosage forms for such extracts. The bioactivity and IR of L-arginine-loaded cranberry leaf extracts were studied in vivo in rats. The cranberry leaf extracts consisted of quinic, 3-caffeoylquinic (chlorogenic), p-coumaroylquinic acids, quercetin 3-O-galactoside, quercetin-3-O-glucoside, quercetin-3-xyloside, quercetin-3-O-arabino pyranoside, quercetin-3-O-arabinofuranoside, quercetin 3-O-rhamnoside, and quercetin-O-p-coumaroyl hexoside-2 identified by HPLC. In vivo studies with rats showed that the oral administration of the cranberry leaf extracts had a positive effect on insulin sensitivity coefficients under the insulin tolerance test and affected homeostasis model assessment IR levels and liver lipid content with experimental IR. A novel 3D-printed immediate-release dosage form was developed for the oral administration of cranberry leaf extracts using polyethylene oxide as a carrier gel in semi-solid extrusion 3D printing. In conclusion, American cranberry leaf extracts loaded with L-arginine could find uses in preventing health issues associated with IR. Full article
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19 pages, 2045 KiB  
Article
Dermal Delivery of Korean Red Ginseng Extract: Impact on Storage Stability of Different Carrier Systems and Evaluation of Rg1 and Rb1 Skin Permeation Ex Vivo
by Victoria Klang, Eva-Maria Schweiger, Simone Strohmaier, Verena Ina Walter, Zorana Dekic and Ammar Tahir
Pharmaceutics 2023, 15(1), 56; https://doi.org/10.3390/pharmaceutics15010056 - 24 Dec 2022
Cited by 3 | Viewed by 1858
Abstract
The root extract of Panax ginseng C.A. Meyer (Korean red ginseng/KRG extract) is a traditional Asian remedy introduced to dermal products for its antioxidative potential. However, little is known about technological aspects or skin penetration of main ginsenosides. Thus, stable oil-in-water nanoemulsions (NEs) [...] Read more.
The root extract of Panax ginseng C.A. Meyer (Korean red ginseng/KRG extract) is a traditional Asian remedy introduced to dermal products for its antioxidative potential. However, little is known about technological aspects or skin penetration of main ginsenosides. Thus, stable oil-in-water nanoemulsions (NEs) and hydrogels for dermal delivery of KRG extract were developed and characterised using light scattering methods, analysis of flow properties and pH measurements. In addition, Rg1 and Rb1 contents were monitored by UHPLC/MS. Different surfactants (phosphatidylcholine, monoacylphosphatidylcholine and polysorbate 80) and polymers (polyacrylic acid and hydroxyethylcellulose) were tested and compared for their compatibility with KRG extract. The results showed that incorporation of KRG extract led to a significantly reduced formulation pH in hydroxyethylcellulose gels (−22%), NEs (−15%) and carbomer gels (−4–5%). The dynamic viscosity was in the range of 24–28 Pas at 10 s−1 for carbomer gels. The highest storage stability and skin permeation were observed for a hydroalcoholic gel with carbomer 50,000 and TRIS buffer (each of 1% w/w), containing ethanol (20% w/w) and KRG extract (2% w/w). Ex vivo diffusion cell studies confirmed skin permeation of the moderately lipophilic Rg1, but not the more hydrophilic Rb1 with a larger molecular weight. Full article
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15 pages, 3553 KiB  
Article
Comparison of the Formulation, Stability and Biological Effects of Hydrophilic Extracts from Black Elder Flowers (Sambucus nigra L.)
by Aurelijus Laurutis, Julius Liobikas, Monika Stanciauskaite, Mindaugas Marksa, Kristina Ramanauskiene and Daiva Majiene
Pharmaceutics 2022, 14(12), 2831; https://doi.org/10.3390/pharmaceutics14122831 - 16 Dec 2022
Cited by 1 | Viewed by 1177
Abstract
Elderflower preparations have long been used to treat colds and flu, but their use is undeservedly reduced, and only dried flower teas, less often ethanolic extracts, can be purchased in pharmacies. In the case of homemade teas, the medicinal plant material is extracted [...] Read more.
Elderflower preparations have long been used to treat colds and flu, but their use is undeservedly reduced, and only dried flower teas, less often ethanolic extracts, can be purchased in pharmacies. In the case of homemade teas, the medicinal plant material is extracted with hot water for a relatively short time, thus only a small part of the active substances is extracted. The industrially produced ethanolic extract is rich in active substances, but its use is limited since ethanol in many countries is undesirable and unsuitable for children and geriatric patients. Therefore, the aim of this work was to produce extracts from elder flowers using water as extractant and a mixture of water + polyethylene glycol (PEG) 20%, to compare their chemical composition and stability, and to study the ability to neutralize reactive oxygen species (ROS) and to sustain the viability of C6 glial cells under oxidative stress conditions. The ethanolic extract was used as a standard. Thus, the extract with PEG contained more than two times higher amount of total phenolics (PC) than the aqueous one, and the stability at 6–8 °C was comparable to the stability of ethanolic extract. All three extracts showed an antioxidant effect in a concentration-dependent manner in vitro. However, only the PEG containing extract (at 20–40 µg/mL PC) was the most effective in reducing the intracellular level of ROS and sustaining the viability of glial cells. The results suggest that the co-solvent PEG increases the yield of phenolics in the extract, prolongs the stability, and enhances positive biological effects. Full article
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Review

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57 pages, 4701 KiB  
Review
Salvianolic Acid B: A Review of Pharmacological Effects, Safety, Combination Therapy, New Dosage Forms, and Novel Drug Delivery Routes
by Guannan He, Guangfeng Chen, Weidong Liu, Dongxue Ye, Xuehuan Liu, Xiaodong Liang and Jing Song
Pharmaceutics 2023, 15(9), 2235; https://doi.org/10.3390/pharmaceutics15092235 - 29 Aug 2023
Cited by 2 | Viewed by 1619
Abstract
Salvianolic acid B is extracted from the roots and rhizomes of Danshen (Salvia miltiorrhiza Bge., family Labiatae). It is a water-soluble, weakly acidic drug that has demonstrated antitumor and anti-inflammatory effects on various organs and tissues such as the lung, heart, kidney, [...] Read more.
Salvianolic acid B is extracted from the roots and rhizomes of Danshen (Salvia miltiorrhiza Bge., family Labiatae). It is a water-soluble, weakly acidic drug that has demonstrated antitumor and anti-inflammatory effects on various organs and tissues such as the lung, heart, kidney, intestine, bone, liver, and skin and protective effects in diseases such as depression and spinal cord injury. The mechanisms underlying the protective effects of salvianolic acid B are mainly related to its anti-inflammatory, antioxidant, anti- or pro-apoptotic, anti- or pro-autophagy, anti-fibrotic, and metabolism-regulating functions. Salvianolic acid B can regulate various signaling pathways, cells, and molecules to achieve maximum therapeutic effects. This review summarizes the safety profile, combination therapy potential, and new dosage forms and delivery routes of salvianolic acid B. Although significant research progress has been made, more in-depth pharmacological studies are warranted to identify the mechanism of action, related signaling pathways, more suitable combination drugs, more effective dosage forms, and novel routes of administration of salvianolic acid B. Full article
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