A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs

• Published in: Advanced science Vol. 8; no. 12; pp. 2100389 - n/a
• Main Authors: Mundaca‐Uribe, Rodolfo, Karshalev, Emil, Esteban‐Fernández de Ávila, Berta, Wei, Xiaoli, Nguyen, Bryan, Litvan, Irene, Fang, Ronnie H., Zhang, Liangfang, Wang, Joseph
• Format: Journal Article
• Language: English
• Published: Germany John Wiley & Sons, Inc 01.06.2021; John Wiley and Sons Inc; Wiley
• Subjects: Acetaminophen - administration & dosage; active drug delivery; Administration, Oral; Animals; Aspirin - administration & dosage; Bioavailability; Biological Availability; Drug delivery systems; Drug Delivery Systems - methods; Drugs; Female; Lactose; Levodopa - administration & dosage; Magnesium - administration & dosage; Male; Mice; microstirring pills; Models, Animal; Nanoparticles; Permeability; Pharmaceuticals; porcine models; Stomach; Swine; translational medicine; active drug delivery; translational medicine; bioavailability; microstirring pills; porcine models
• ISSN: 2198-3844; 2198-3844
• DOI: 10.1002/advs.202100389

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. Microstirring pill platform technology offers a built‐in mixing capability for in vivo oral drug delivery and leads to significantly enhanced drug absorption and bioavailability. In vivo studies using murine and porcine models demonstrate that the localized stirring capability of microstirrers results in enhanced bioavailability of drug payloads. This elegant technology offers considerable promise for oral delivery of therapeutics. ​