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Pharmaceutics
Special Issues
Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines
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Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines

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

Deadline for manuscript submissions: 20 May 2024 | Viewed by 8920

Special Issue Editor

Prof. Dr. Omar Mertins

E-Mail Website
Guest Editor
Laboratory of Nano Bio Materials, Department of Biophysics, Paulista Medical School, Federal University of Sao Paulo, São Paulo 04023-062, Brazil
Interests: nanoparticles; liposomes; cubosomes; biopolymers; drug delivery; giant vesicles; lipid membranes

Special Issue Information

Dear Colleagues,

Today’s nanomedicine benefits largely from the use of a variety of drug delivery systems based on polymeric nanoparticles. Despite the consensus of advantageous high compliance, flexibility in dosage design and reduced costs, the oral route of administration still represents a challenge, especially due to the resulting poor bioavailability. Currently, research on oral drug delivery systems focuses on improved and functional nanoparticles designed to overcome gastrointestinal challenges and provide effective drug targeting.

This Special Issue aims to provide an update on current and recent progress in polymer-based micro- and nanoparticles for oral delivery of drugs, vaccines and bioactives, which can be, for instance, nutraceuticals, antioxidants, anticancer, and antimicrobials.

Polymer-based micro- and nanoparticles are those that have at least one component in their structure that is a polymer, which can be synthetic or of natural origin, as well as biopolymers, polyelectrolytes, and polypeptides. Hence, particles can be hybrids and contain, for instance, lipids or metals.

The design of micro- and nanoparticles for encapsulation, delivery, their characterization, toxicity studies, in vitro and in vivo interaction with the biological milieu, human and veterinary applications, and controlled release and targeting, all focused on oral administration will be considered. Experimental, theoretical, and review articles are welcome.

Prof. Dr. Omar Mertins
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. Pharmaceutics is an international peer-reviewed open access monthly 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 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

  • oral drug delivery
  • nanotechnology
  • bioparticles
  • nanoparticles
  • biopolymers
  • gastrointestinal tract
  • functionalization
  • pH-responsive
  • mucoadhesive
  • microvilli
  • vaccine
  • antioxidant
  • antimicrobial
  • polymers
  • polypeptides
  • flavonoids
  • essential oils
  • immunostimulant

Published Papers (4 papers)

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Research

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16 pages, 2357 KiB  
Article
Flavonoid-Labeled Biopolymer in the Structure of Lipid Membranes to Improve the Applicability of Antioxidant Nanovesicles
by Patrick D. Mathews, Gabriella S. Gama, Hector M. Megiati, Rafael R. M. Madrid, Bianca B. M. Garcia, Sang W. Han, Rosangela Itri and Omar Mertins
Pharmaceutics 2024, 16(1), 141; https://doi.org/10.3390/pharmaceutics16010141 - 20 Jan 2024
Viewed by 1106
Abstract
Nanovesicles produced with lipids and polymers are promising devices for drug and bioactive delivery and are of great interest in pharmaceutical applications. These nanovesicles can be engineered for improvement in bioavailability, patient compliance or to provide modified release or enhanced delivery. However, their [...] Read more.
Nanovesicles produced with lipids and polymers are promising devices for drug and bioactive delivery and are of great interest in pharmaceutical applications. These nanovesicles can be engineered for improvement in bioavailability, patient compliance or to provide modified release or enhanced delivery. However, their applicability strongly depends on the safety and low immunogenicity of the components. Despite this, the use of unsaturated lipids in nanovesicles, which degrade following oxidation processes during storage and especially during the proper routes of administration in the human body, may yield toxic degradation products. In this study, we used a biopolymer (chitosan) labeled with flavonoid (catechin) as a component over a lipid bilayer for micro- and nanovesicles and characterized the structure of these vesicles in oxidation media. The purpose of this was to evaluate the in situ effect of the antioxidant in three different vesicular systems of medium, low and high membrane curvature. Liposomes and giant vesicles were produced with the phospholipids DOPC and POPC, and crystalline cubic phase with monoolein/DOPC. Concentrations of chitosan–catechin (CHCa) were included in all the vesicles and they were challenged in oxidant media. The cytotoxicity analysis using the MTT assay (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) revealed that concentrations of CHCa below 6.67 µM are non-toxic to HeLa cells. The size and zeta potential of the liposomes evidenced the degradation of their structures, which was minimized by CHCa. Similarly, the membrane of the giant vesicle, which rapidly deteriorated in oxidative solution, was protected in the presence of CHCa. The production of a lipid/CHCa composite cubic phase revealed a specific cubic topology in small-angle X-ray scattering, which was preserved in strong oxidative media. This study demonstrates the specific physicochemical characteristics introduced in the vesicular systems related to the antioxidant CHCa biopolymer, representing a platform for the improvement of composite nanovesicle applicability. Full article
(This article belongs to the Special Issue Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines)
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25 pages, 4844 KiB  
Article
pH-Responsive and Mucoadhesive Nanoparticles for Enhanced Oral Insulin Delivery: The Effect of Hyaluronic Acid with Different Molecular Weights
by Shuangqing Wang, Saige Meng, Xinlei Zhou, Zhonggao Gao and Ming Guan Piao
Pharmaceutics 2023, 15(3), 820; https://doi.org/10.3390/pharmaceutics15030820 - 02 Mar 2023
Cited by 11 | Viewed by 1779
Abstract
Drug degradation at low pH and rapid clearance from intestinal absorption sites are the main factors limiting the development of oral macromolecular delivery systems. Based on the pH responsiveness and mucosal adhesion of hyaluronic acid (HA) and poly[2-(dimethylamino)ethyl methacrylate] (PDM), we prepared three [...] Read more.
Drug degradation at low pH and rapid clearance from intestinal absorption sites are the main factors limiting the development of oral macromolecular delivery systems. Based on the pH responsiveness and mucosal adhesion of hyaluronic acid (HA) and poly[2-(dimethylamino)ethyl methacrylate] (PDM), we prepared three HA–PDM nano-delivery systems loaded with insulin (INS) using three different molecular weights (MW) of HA (L, M, H), respectively. The three types of nanoparticles (L/H/M-HA–PDM–INS) had uniform particle sizes and negatively charged surfaces. The optimal drug loadings of the L-HA–PDM–INS, M-HA–PDM–INS, H-HA–PDM–INS were 8.69 ± 0.94%, 9.11 ± 1.03%, and 10.61 ± 1.16% (w/w), respectively. The structural characteristics of HA–PDM–INS were determined using FT-IR, and the effect of the MW of HA on the properties of HA–PDM–INS was investigated. The release of INS from H-HA–PDM–INS was 22.01 ± 3.84% at pH 1.2 and 63.23 ± 4.10% at pH 7.4. The protective ability of HA–PDM–INS with different MW against INS was verified by circular dichroism spectroscopy and protease resistance experiments. H-HA–PDM–INS retained 45.67 ± 5.03% INS at pH 1.2 at 2 h. The biocompatibility of HA–PDM–INS, regardless of the MW of HA, was demonstrated using CCK-8 and live–dead cell staining. Compared with the INS solution, the transport efficiencies of L-HA–PDM–INS, M-HA–PDM–INS, and H-HA–PDM–INS increased 4.16, 3.81, and 3.10 times, respectively. In vivo pharmacodynamic and pharmacokinetic studies were performed in diabetic rats following oral administration. H-HA–PDM–INS exhibited an effective hypoglycemic effect over a long period, with relative bioavailability of 14.62%. In conclusion, these simple, environmentally friendly, pH-responsive, and mucoadhesive nanoparticles have the potential for industrial development. This study provides preliminary data support for oral INS delivery. Full article
(This article belongs to the Special Issue Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines)
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22 pages, 7668 KiB  
Article
Chitosan Surface-Modified PLGA Nanoparticles Loaded with Cranberry Powder Extract as a Potential Oral Delivery Platform for Targeting Colon Cancer Cells
by Mona M. Mostafa, Maha M. Amin, Mohamed Y. Zakaria, Mohammed Abdalla Hussein, Marium M. Shamaa and Shady M. Abd El-Halim
Pharmaceutics 2023, 15(2), 606; https://doi.org/10.3390/pharmaceutics15020606 - 10 Feb 2023
Cited by 16 | Viewed by 2511
Abstract
Nutraceutical cranberry powder extract (CBPE) has distinct polyphenols inhibiting colon cancer growth and proliferation. However, its oral therapeutic efficacy is hindered because of its low permeability. This study aims to formulate chitosan surface-modified PLGA nanoparticles (CS-PLGA NPs) for encapsulating CBPE and modulating its [...] Read more.
Nutraceutical cranberry powder extract (CBPE) has distinct polyphenols inhibiting colon cancer growth and proliferation. However, its oral therapeutic efficacy is hindered because of its low permeability. This study aims to formulate chitosan surface-modified PLGA nanoparticles (CS-PLGA NPs) for encapsulating CBPE and modulating its release rate, permeation, cell targeting, and, therefore, its cytotoxicity. A full 23 factorial design is employed to scrutinize the effect of lactide/glycolide ratio, PLGA weight, and stabilizer concentrations on entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). The optimum formula (F4) shows spherical particles with a relatively high EE% (72.30 ± 2.86%), an appropriate size of 370.10 ± 10.31 nm, PDI; 0.398 ± 0.001, and ZP; −5.40 ± 0.21 mV. Alongside the ATR-FTIR outcomes, the chitosan surface-modified formula (CS-F4) demonstrates a significant increase in particle size (417.67 ± 6.77 nm) and a shift from negative to positive zeta potential (+21.63 ± 2.46 mV), confirming the efficiency of surface modification with chitosan. The intestinal permeability of F4 and CS-F4 is significantly increased by 2.19- and 3.10-fold, respectively, compared to the CBPE solution, with the permeability coefficient (Papp) being 2.05 × 10−4 cm/min and 2.91 × 10−4 cm/min, for F4 and CS-F4, respectively, compared to the CBPE solution, 9.36 × 10−5 cm/min. Moreover, CS-F4 evidences significant caspase-3 protein level expression stimulation and significant inhibition of vascular endothelial growth factor (VEGF) and signal transducer and activator of transcription-3 (STAT-3) protein expression levels, confirming the superiority of CS-F4 for targeting HT-29 cells. Briefly, CS-PLGA NPs could be regarded as a prosperous delivery system of CBPE with enhanced permeation, cell targeting, and antitumor efficacy. Full article
(This article belongs to the Special Issue Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines)
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Review

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23 pages, 3806 KiB  
Review
Chitosan in Oral Drug Delivery Formulations: A Review
by Tanikan Sangnim, Divya Dheer, Nitin Jangra, Kampanart Huanbutta, Vivek Puri and Ameya Sharma
Pharmaceutics 2023, 15(9), 2361; https://doi.org/10.3390/pharmaceutics15092361 - 21 Sep 2023
Cited by 5 | Viewed by 2549
Abstract
Nanoformulations have become increasingly useful as drug delivery technologies in recent decades. As therapeutics, oral administration is the most common delivery method, although it is not always the most effective route because of challenges with swallowing, gastrointestinal discomfort, low solubility, and poor absorption. [...] Read more.
Nanoformulations have become increasingly useful as drug delivery technologies in recent decades. As therapeutics, oral administration is the most common delivery method, although it is not always the most effective route because of challenges with swallowing, gastrointestinal discomfort, low solubility, and poor absorption. One of the most significant barriers that medications must overcome to exert a therapeutic effect is the impact of the first hepatic transit. Studies have shown that controlled-release systems using nanoparticles composed of biodegradable natural polymers significantly improve oral administration, which is why these materials have attracted significant attention. Chitosan possesses a wide variety of properties and functions in the pharmaceutical as well as healthcare industries. Drug encapsulation and transport within the body are two of its most important features. Moreover, chitosan can enhance drug efficacy by facilitating drug interaction with target cells. Based on its physicochemical properties, chitosan can potentially be synthesized into nanoparticles, and this review summarizes recent advances and applications of orally delivered chitosan nanoparticle interventions. Full article
(This article belongs to the Special Issue Polymer-Based Nanoparticles for Oral Delivery of Drugs, Bioactives and Vaccines)
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