Nanotechnology-Based Approaches for Enhancing Oral Administration of Drugs

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

Deadline for manuscript submissions: 31 March 2024 | Viewed by 6131

Special Issue Editor

Faculty of Pharmacy, University of Coimbra, 3000-348 Coimbra, Portugal
Interests: biodegradable polymers; biopharmaceuticals; drug bioavailability; modified release; pharmaceutical nanotechnology

Special Issue Information

Dear Colleagues,

Oral administration is the most convenient route for drugs, as it increases patient compliance and reduces the risk of most parenteral-related complications. However, the poor solubility and stability of drugs along the gastrointestinal tract are major limitations, preventing their therapeutic effect. Nanotechnology approaches for drug delivery applications have shown remarkable progress in the field of drug delivery, so there is no doubt about its potential to increase the stability and bioavailability of drugs administered by oral route.

Nanotechnology-based drug products may impart drug physicochemical or biological properties providing nanoformulations with new abilities such as targeting specific body areas and bypassing others. A significant impact on drug therapeutic dose and side effect risks can increase treatment efficacy. Nanocrystals are among the most nanotechnology-based drug products being approved in the treatment of several diseases. Whether the nanotechnology approach meets drug properties remains a question which is not to be neglected. 

This Special Issue focuses on nanotechnology approaches in oral drug administration, their in vitro and in vivo performance analysis, and scale-up potential. Additionally, toxicity issues and regulatory affairs requirements are critically analyzed towards a successful market introduction.

Dr. Antônio J. Ribeiro
Guest Editor

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Keywords

  • bioavailability
  • drug
  • modified release
  • nanotechnology
  • oral delivery
  • pharmacokinetics
  • regulatory affairs
  • stability
  • solubility
  • safety

Published Papers (2 papers)

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Research

14 pages, 5619 KiB  
Article
Dasatinib Nanoemulsion and Nanocrystal for Enhanced Oral Drug Delivery
by Chuanqi Wang, Manting Wang, Peng Chen, Jiexin Wang and Yuan Le
Pharmaceutics 2022, 14(1), 197; https://doi.org/10.3390/pharmaceutics14010197 - 15 Jan 2022
Cited by 9 | Viewed by 2446
Abstract
In this work, dasatinib (DAS) nanoemulsion and nanocrystal are produced by high-gravity technology that approaches to practical mass production. The drug nanoformulations were systematically characterized and evaluated. At a low high-gravity level (β) = 47, nanoemulsion droplets were 16.15 ± 0.42 nm with [...] Read more.
In this work, dasatinib (DAS) nanoemulsion and nanocrystal are produced by high-gravity technology that approaches to practical mass production. The drug nanoformulations were systematically characterized and evaluated. At a low high-gravity level (β) = 47, nanoemulsion droplets were 16.15 ± 0.42 nm with a PDI of 0.122 ± 0.021. The nanoemulsion’s size and active pharmaceutical ingredient (API) content remained stable at long-term (4 months) freeze–thaw and dilution experiments. At a high β = 188, the as-prepared nanocrystal was lamellar with a short diameter of about 200 nm and a long diameter of about 750 nm. In vitro performances demonstrated the nanoemulsion displayed higher cytotoxicity on MDA-MB-231 tumor cells, Caco-2 cell permeability and drug release than that of the nanocrystal, indicating that nanoemulsion should be an ideal alternative for dasatinib oral administration. Full article
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20 pages, 3745 KiB  
Article
Oral Delivery of Nucleic Acids with Passive and Active Targeting to the Intestinal Tissue Using Polymer-Based Nanocarriers
by Sagun Poudel, Prabhat R. Napit, Karen P. Briski and George Mattheolabakis
Pharmaceutics 2021, 13(7), 1075; https://doi.org/10.3390/pharmaceutics13071075 - 13 Jul 2021
Cited by 12 | Viewed by 2878
Abstract
Despite the apparent advantages for long-term treatment and local therapies against intestinal diseases, the oral delivery of nucleic acids has been challenging due to unfavorable physiological conditions for their stability. In this study, a novel nanodelivery system of PEG-PCL nanoparticles with encapsulated nucleic [...] Read more.
Despite the apparent advantages for long-term treatment and local therapies against intestinal diseases, the oral delivery of nucleic acids has been challenging due to unfavorable physiological conditions for their stability. In this study, a novel nanodelivery system of PEG-PCL nanoparticles with encapsulated nucleic acids–mannosylated PEI (Man-PEI) complexes was developed for intestinal delivery. We complexed model nucleic acids with Man-PEI at the optimal N/P ratio of 20:1 for in vitro and in vivo analyses. Cells were transfected in vitro and analyzed for gene expression, receptor-mediated uptake, and PEG-PCL nanoparticles’ toxicity. We also evaluated the nucleic acid’s stability in the nanocarrier during formulation, and under simulated gastrointestinal environments or the presence of nucleases. Finally, we assessed the biodistribution for the PEG-PCL nanoparticles with encapsulated complexes and their ability to transfect intestinal cells in vivo. Nucleic acids complexed with Man-PEI were protected from degradation against nucleases. In comparison to the parent compound PEI, Man-PEI transfected the cells with an overall higher potency. Competition assay indicated receptor-mediated endocytosis promoted by mannose receptors. The PEG-PCL nanoparticles with Man-PEI/plasmid complexes indicated minimal cytotoxicity. The nanocarrier successfully protected the complexes in a simulated gastric fluid environment and released them in a simulated intestinal fluid environment, promoted by the presence of lipases. The oral administration of the PEG-PCL nanoparticles with encapsulated Man-PEI/plasmid complexes transfected intestinal cells with the plasmid in vivo, while presenting a time-dependent progression through the intestines. Conclusively, our carrier system can deliver genetic material to the GI tract and actively target mannose receptor overexpressing cells. Full article
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