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A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs

Majority of drugs are administered orally, yet their efficient absorption is often difficult to achieve, with a low dose fraction reaching the blood compartment. Here, a microstirring pill technology is reported with built‐in mixing capability for oral drug delivery that greatly enhances bioavailabi...

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Autores principales: Mundaca‐Uribe, Rodolfo, Karshalev, Emil, Esteban‐Fernández de Ávila, Berta, Wei, Xiaoli, Nguyen, Bryan, Litvan, Irene, Fang, Ronnie H., Zhang, Liangfang, Wang, Joseph
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8224427/
https://www.ncbi.nlm.nih.gov/pubmed/34194949
http://dx.doi.org/10.1002/advs.202100389
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author Mundaca‐Uribe, Rodolfo
Karshalev, Emil
Esteban‐Fernández de Ávila, Berta
Wei, Xiaoli
Nguyen, Bryan
Litvan, Irene
Fang, Ronnie H.
Zhang, Liangfang
Wang, Joseph
author_facet Mundaca‐Uribe, Rodolfo
Karshalev, Emil
Esteban‐Fernández de Ávila, Berta
Wei, Xiaoli
Nguyen, Bryan
Litvan, Irene
Fang, Ronnie H.
Zhang, Liangfang
Wang, Joseph
author_sort Mundaca‐Uribe, Rodolfo
collection PubMed
description Majority of drugs are administered orally, yet their efficient absorption is often difficult to achieve, with a low dose fraction reaching the blood compartment. Here, a microstirring pill technology is reported with built‐in mixing capability for oral drug delivery that greatly enhances bioavailability of its therapeutic payload. Embedding microscopic stirrers into a pill matrix enables faster disintegration and dissolution, leading to improved release profiles of three widely used model drugs, aspirin, levodopa, and acetaminophen, without compromising their loading. Unlike recently developed drug‐carrying nanomotors, drug molecules are not associated with the microstirrers, and hence there is no limitation on the loading capacity. These embedded microstirrers are fabricated through the asymmetric coating of titanium dioxide thin film onto magnesium microparticles. In vitro tests illustrate that the embedded microstirrers lead to substantial enhancement of local fluid transport. In vivo studies using murine and porcine models demonstrate that the localized stirring capability of microstirrers leads to enhanced bioavailability of drug payloads. Such improvements are of considerable importance in clinical scenarios where fast absorption and high bioavailability of therapeutics are critical. The encouraging results obtained in porcine model suggest that the microstirring pill technology has translational potential and can be developed toward practical biomedical applications.
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spelling pubmed-82244272021-06-29 A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs Mundaca‐Uribe, Rodolfo Karshalev, Emil Esteban‐Fernández de Ávila, Berta Wei, Xiaoli Nguyen, Bryan Litvan, Irene Fang, Ronnie H. Zhang, Liangfang Wang, Joseph Adv Sci (Weinh) Research Articles Majority of drugs are administered orally, yet their efficient absorption is often difficult to achieve, with a low dose fraction reaching the blood compartment. Here, a microstirring pill technology is reported with built‐in mixing capability for oral drug delivery that greatly enhances bioavailability of its therapeutic payload. Embedding microscopic stirrers into a pill matrix enables faster disintegration and dissolution, leading to improved release profiles of three widely used model drugs, aspirin, levodopa, and acetaminophen, without compromising their loading. Unlike recently developed drug‐carrying nanomotors, drug molecules are not associated with the microstirrers, and hence there is no limitation on the loading capacity. These embedded microstirrers are fabricated through the asymmetric coating of titanium dioxide thin film onto magnesium microparticles. In vitro tests illustrate that the embedded microstirrers lead to substantial enhancement of local fluid transport. In vivo studies using murine and porcine models demonstrate that the localized stirring capability of microstirrers leads to enhanced bioavailability of drug payloads. Such improvements are of considerable importance in clinical scenarios where fast absorption and high bioavailability of therapeutics are critical. The encouraging results obtained in porcine model suggest that the microstirring pill technology has translational potential and can be developed toward practical biomedical applications. John Wiley and Sons Inc. 2021-05-18 /pmc/articles/PMC8224427/ /pubmed/34194949 http://dx.doi.org/10.1002/advs.202100389 Text en © 2021 The Authors. Advanced Science published by Wiley‐VCH GmbH https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Articles
Mundaca‐Uribe, Rodolfo
Karshalev, Emil
Esteban‐Fernández de Ávila, Berta
Wei, Xiaoli
Nguyen, Bryan
Litvan, Irene
Fang, Ronnie H.
Zhang, Liangfang
Wang, Joseph
A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title_full A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title_fullStr A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title_full_unstemmed A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title_short A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
title_sort microstirring pill enhances bioavailability of orally administered drugs
topic Research Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8224427/
https://www.ncbi.nlm.nih.gov/pubmed/34194949
http://dx.doi.org/10.1002/advs.202100389
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