Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer

Glycyrrhizic acid and its hydrolyzed metabolite 18β-glycyrrhetinic acid, obtained from the plant <i>Glycyrrhiza glabra</i>, have numerous pharmacological activities, such as anti-inflammatory, anti-ulcerative, antiallergic, immunomodulatory, antiviral, antitumor, hepatoprotective, and an...

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Main Authors: Luciano A. Stecanella, Antonio P. R. Bitencourt, Gustavo Richter Vaz, Eride Quarta, José O. C. Silva Júnior, Alessandra Rossi
Format: Article
Language:English
Published: MDPI AG 2021-10-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/13/11/1792
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author Luciano A. Stecanella
Antonio P. R. Bitencourt
Gustavo Richter Vaz
Eride Quarta
José O. C. Silva Júnior
Alessandra Rossi
author_facet Luciano A. Stecanella
Antonio P. R. Bitencourt
Gustavo Richter Vaz
Eride Quarta
José O. C. Silva Júnior
Alessandra Rossi
author_sort Luciano A. Stecanella
collection DOAJ
description Glycyrrhizic acid and its hydrolyzed metabolite 18β-glycyrrhetinic acid, obtained from the plant <i>Glycyrrhiza glabra</i>, have numerous pharmacological activities, such as anti-inflammatory, anti-ulcerative, antiallergic, immunomodulatory, antiviral, antitumor, hepatoprotective, and antioxidant effects, and others. In addition to the pharmacological activities, in the 1980s, an interaction and uptake of these molecules by the liver was verified, which was later confirmed by other studies through the discovery of specific receptors in the hepatocytes. The presence of these specific receptors in the liver led to vectorization and delivery of drugs, by the introduction of glycyrrhizic acid or glycyrrhetinic acid on the surface of nanosystems, for the treatment of liver diseases. This review describes experimental evidence of vectorization by conjugating glycyrrhizic acid or glycyrrhetinic acid to nanosystems and delivery of antitumor drugs for the treatment of liver cancer and also describes the techniques used to perform this conjugation. We have shown that due to the existence of specific receptors for these molecules, in addition to the targeting of nanosystems to hepatocytes, nanosystems having glycyrrhizic acid or glycyrrhetinic acid on their surface had the same therapeutic effect in a significantly lower dose compared to the free drug and unconjugated nanosystems, with consequent reduction of side effects and toxicity.
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spelling doaj.art-1504cb8602084cd19ea84b4a22e4f8e62023-11-23T00:57:40ZengMDPI AGPharmaceutics1999-49232021-10-011311179210.3390/pharmaceutics13111792Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver CancerLuciano A. Stecanella0Antonio P. R. Bitencourt1Gustavo Richter Vaz2Eride Quarta3José O. C. Silva Júnior4Alessandra Rossi5Laboratory R&D Pharmaceutical and Cosmetic, Federal University of Pará, Street Augusto Correa 01, Belém 66075-110, BrazilLaboratory R&D Pharmaceutical and Cosmetic, Federal University of Pará, Street Augusto Correa 01, Belém 66075-110, BrazilDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyLaboratory R&D Pharmaceutical and Cosmetic, Federal University of Pará, Street Augusto Correa 01, Belém 66075-110, BrazilDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyGlycyrrhizic acid and its hydrolyzed metabolite 18β-glycyrrhetinic acid, obtained from the plant <i>Glycyrrhiza glabra</i>, have numerous pharmacological activities, such as anti-inflammatory, anti-ulcerative, antiallergic, immunomodulatory, antiviral, antitumor, hepatoprotective, and antioxidant effects, and others. In addition to the pharmacological activities, in the 1980s, an interaction and uptake of these molecules by the liver was verified, which was later confirmed by other studies through the discovery of specific receptors in the hepatocytes. The presence of these specific receptors in the liver led to vectorization and delivery of drugs, by the introduction of glycyrrhizic acid or glycyrrhetinic acid on the surface of nanosystems, for the treatment of liver diseases. This review describes experimental evidence of vectorization by conjugating glycyrrhizic acid or glycyrrhetinic acid to nanosystems and delivery of antitumor drugs for the treatment of liver cancer and also describes the techniques used to perform this conjugation. We have shown that due to the existence of specific receptors for these molecules, in addition to the targeting of nanosystems to hepatocytes, nanosystems having glycyrrhizic acid or glycyrrhetinic acid on their surface had the same therapeutic effect in a significantly lower dose compared to the free drug and unconjugated nanosystems, with consequent reduction of side effects and toxicity.https://www.mdpi.com/1999-4923/13/11/1792glycyrrhizic acidglycyrrhetinic acidliver cancernanosystemsdrug targeting
spellingShingle Luciano A. Stecanella
Antonio P. R. Bitencourt
Gustavo Richter Vaz
Eride Quarta
José O. C. Silva Júnior
Alessandra Rossi
Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
Pharmaceutics
glycyrrhizic acid
glycyrrhetinic acid
liver cancer
nanosystems
drug targeting
title Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
title_full Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
title_fullStr Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
title_full_unstemmed Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
title_short Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer
title_sort glycyrrhizic acid and its hydrolyzed metabolite 18β glycyrrhetinic acid as specific ligands for targeting nanosystems in the treatment of liver cancer
topic glycyrrhizic acid
glycyrrhetinic acid
liver cancer
nanosystems
drug targeting
url https://www.mdpi.com/1999-4923/13/11/1792
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