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Pharmaceutics
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Polysaccharide in Drug Delivery System
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Polysaccharide in Drug Delivery System

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biopharmaceutics".

Deadline for manuscript submissions: closed (31 August 2020) | Viewed by 16988

Special Issue Editors

Dr. Orazio Vittorio

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Guest Editor
Children's Cancer Institute, University of New South Wales, Kensington, NSW 2750, Australia
Interests: cancer; infectious diseases; neurological diseases; nanoparticles; hydrogels; vesicles; hybrid materials; blood–brain barrier; transdermal delivery; nasal delivery
Special Issues, Collections and Topics in MDPI journals
Dr. Giuseppe Cirillo

E-Mail Website
Guest Editor
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy
Interests: nanomaterials; biomaterials; carbon nanostructures; composite and hybrid materials; biomedical applications of functional materials; therapeutic devices; surface chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polysaccharides have been recognized as one of the most interesting classes of biomaterials for the development of highly effective delivery systems for the treatment of a plethora of human disorders, including cancer, infections, inflammations, and degenerative diseases. This interest is related to their superior chemical features, well matched with the ultimate aim of a drug delivery system (DDS). The main objective of DDS, indeed, is to optimize the delivery of a biologically active agent for improving the systemic circulation controlling, at the same time, the pharmacokinetics, pharmacodynamics, non-immunogenicity, and non-specific toxicity.

Furthermore, polysaccharides possess a wide chemical versatility for tailored functionalization processes. The high functional versatility and structural diversity within such classes of biomaterials, together with the abundance of chemical groups (e.g., amine, carboxyl, carbonyl, and hydroxyl groups) offer many options for the development of different delivery vehicles, including hydrogels, micro- and nano- particles, vesicles, polymeric conjugates, hybrid materials, and others.

Within this Special Issue, we aim to cover the recent advances in the field, by a multidisciplinary approach covering the expertise in polymer science, bioconjugate chemistry, pharmaceutics, and molecular biology of the contributing authors.

Dr. Orazio Vittorio
Dr. Giuseppe Cirillo
Guest Editors

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 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

  • nanoparticles
  • hydrogels
  • vesicles
  • hybrid materials
  • bioconjugate chemistry
  • pharmacokinetics

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Published Papers (4 papers)

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Research

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14 pages, 3298 KiB  
Article
RETRACTED: Chitosan-Based Microparticles Enhance Ellagic Acid’s Colon Targeting and Proapoptotic Activity
by Nabil A. Alhakamy, Osama A. A. Ahmed, Mallesh Kurakula, Giuseppe Caruso, Filippo Caraci, Hani Z. Asfour, Anas Alfarsi, Basma G. Eid, Amir I. Mohamed, Nabil K. Alruwaili, Wesam H. Abdulaal, Usama A. Fahmy, Hani A. Alhadrami, Basmah M. Eldakhakhny and Ashraf B. Abdel-Naim
Pharmaceutics 2020, 12(7), 652; https://doi.org/10.3390/pharmaceutics12070652 - 9 Jul 2020
Cited by 26 | Viewed by 3915 | Retraction
Abstract
This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative [...] Read more.
This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative pH values. Maximum release was observed at 24 h and pH 7.4. The cytotoxicity of EA MPs on HCT 116 colon cancer cells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry suggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher cell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic activity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation of the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and total cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the double-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography. In conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting as well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared with the administration of raw EA. Full article
(This article belongs to the Special Issue Polysaccharide in Drug Delivery System)
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11 pages, 2078 KiB  
Article
Development of a Phosphoric Acid-Mediated Hyaluronic Acid Gel Sheet for Efficient Transdermal Delivery of Alendronate for Anti-Osteoporotic Therapy
by Chihiro Naito, Hidemasa Katsumi, Kunio Yoneto, Mao Omura, Mayuko Nishidono, Sachi Kamei, Akiya Mizoguchi, Ayaka Tamba, Akiko Tanaka, Masaki Morishita and Akira Yamamoto
Pharmaceutics 2019, 11(12), 643; https://doi.org/10.3390/pharmaceutics11120643 - 2 Dec 2019
Cited by 7 | Viewed by 3098
Abstract
For efficient transdermal delivery of alendronate (ALN) for anti-osteoporotic therapy, we developed a hyaluronic acid (HA) gel sheet that was prepared simply by enhancing HA noncovalent interactions using phosphoric acid and polyhydric alcohol (propanediol and glycerin). HA solution viscosity increased after addition of [...] Read more.
For efficient transdermal delivery of alendronate (ALN) for anti-osteoporotic therapy, we developed a hyaluronic acid (HA) gel sheet that was prepared simply by enhancing HA noncovalent interactions using phosphoric acid and polyhydric alcohol (propanediol and glycerin). HA solution viscosity increased after addition of phosphoric acid, and the HA gel sheet formed after heated drying. The HA gel sheet could be converted to high viscosity state by addition of water. These results indicate that phosphoric acid enhances the noncovalent interactions of HA molecules. The HA gel sheet elicited no skin irritation over 7 days after a 24-h application. The permeation of ALN across rat and human skin was 109 and 7.17 µg/cm2, respectively, up to 24 h after application of the ALN-loaded HA gel sheet, which is sufficient for clinical treatment of osteoporosis. The bioavailability of ALN in rats was ~20% after application of the ALN-loaded HA gel sheet, and plasma calcium levels were effectively reduced 3 days after sheet application. Furthermore, in a rat osteoporosis model, the reduction in tibial bone density was suppressed by treatment with the ALN-loaded HA gel sheet. These results indicate that our phosphoric acid-mediated HA gel sheet is a promising transdermal formulation for efficient ALN delivery. Full article
(This article belongs to the Special Issue Polysaccharide in Drug Delivery System)
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Review

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26 pages, 3445 KiB  
Review
Natural Polysaccharide Carriers in Brain Delivery: Challenge and Perspective
by Manuela Curcio, Giuseppe Cirillo, Jourdin R. C. Rouaen, Federica Saletta, Fiore Pasquale Nicoletta, Orazio Vittorio and Francesca Iemma
Pharmaceutics 2020, 12(12), 1183; https://doi.org/10.3390/pharmaceutics12121183 - 6 Dec 2020
Cited by 23 | Viewed by 3762
Abstract
Targeted drug delivery systems represent valuable tools to enhance the accumulation of therapeutics in the brain. Here, the presence of the blood brain barrier strongly hinders the passage of foreign substances, often limiting the effectiveness of pharmacological therapies. Among the plethora of materials [...] Read more.
Targeted drug delivery systems represent valuable tools to enhance the accumulation of therapeutics in the brain. Here, the presence of the blood brain barrier strongly hinders the passage of foreign substances, often limiting the effectiveness of pharmacological therapies. Among the plethora of materials used for the development of these systems, natural polysaccharides are attracting growing interest because of their biocompatibility, muco-adhesion, and chemical versatility which allow a wide range of carriers with tailored physico-chemical features to be synthetized. This review describes the state of the art in the field of targeted carriers based on natural polysaccharides over the last five years, focusing on the main targeting strategies, namely passive and active transport, stimuli-responsive materials and the administration route. In addition, in the last section, the efficacy of the reviewed carriers in each specific brain diseases is summarized and commented on in terms of enhancement of either blood brain barrier (BBB) permeation ability or drug bioavailability in the brain. Full article
(This article belongs to the Special Issue Polysaccharide in Drug Delivery System)
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33 pages, 2763 KiB  
Review
Carbohydrate Immune Adjuvants in Subunit Vaccines
by Sahra Bashiri, Prashamsa Koirala, Istvan Toth and Mariusz Skwarczynski
Pharmaceutics 2020, 12(10), 965; https://doi.org/10.3390/pharmaceutics12100965 - 14 Oct 2020
Cited by 36 | Viewed by 5288
Abstract
Modern subunit vaccines are composed of antigens and a delivery system and/or adjuvant (immune stimulator) that triggers the desired immune responses. Adjuvants mimic pathogen-associated molecular patterns (PAMPs) that are typically associated with infections. Carbohydrates displayed on the surface of pathogens are often recognized [...] Read more.
Modern subunit vaccines are composed of antigens and a delivery system and/or adjuvant (immune stimulator) that triggers the desired immune responses. Adjuvants mimic pathogen-associated molecular patterns (PAMPs) that are typically associated with infections. Carbohydrates displayed on the surface of pathogens are often recognized as PAMPs by receptors on antigen-presenting cells (APCs). Consequently, carbohydrates and their analogues have been used as adjuvants and delivery systems to promote antigen transport to APCs. Carbohydrates are biocompatible, usually nontoxic, biodegradable, and some are mucoadhesive. As such, carbohydrates and their derivatives have been intensively explored for the development of new adjuvants. This review assesses the immunological functions of carbohydrate ligands and their ability to enhance systemic and mucosal immune responses against co-administered antigens. The role of carbohydrate-based adjuvants/delivery systems in the development of subunit vaccines is discussed in detail. Full article
(This article belongs to the Special Issue Polysaccharide in Drug Delivery System)
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