Utilizing Laser Activation of Photothermal Plasmonic Nanoparticles to Induce On-Demand Drug Amorphization inside a Tablet
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Utilizing Laser Activation of Photothermal Plasmonic Nanoparticles to Induce On-Demand Drug Amorphization inside a Tablet. / Hempel, Nele Johanna; Merkl, Padryk; Asad, Shno; Knopp, Matthias Manne; Berthelsen, Ragna; Bergström, Christel A.S.; Teleki, Alexandra; Sotiriou, Georgios A.; Löbmann, Korbinian.
In: Molecular Pharmaceutics, Vol. 18, No. 6, 2021, p. 2254–2262.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Utilizing Laser Activation of Photothermal Plasmonic Nanoparticles to Induce On-Demand Drug Amorphization inside a Tablet
AU - Hempel, Nele Johanna
AU - Merkl, Padryk
AU - Asad, Shno
AU - Knopp, Matthias Manne
AU - Berthelsen, Ragna
AU - Bergström, Christel A.S.
AU - Teleki, Alexandra
AU - Sotiriou, Georgios A.
AU - Löbmann, Korbinian
N1 - Publisher Copyright: © 2021 American Chemical Society. All rights reserved.
PY - 2021
Y1 - 2021
N2 - Poor aqueous drug solubility represents a major challenge in oral drug delivery. A novel approach to overcome this challenge is drug amorphization inside a tablet, that is, on-demand drug amorphization. The amorphous form is a thermodynamically instable, disordered solid-state with increased dissolution rate and solubility compared to its crystalline counterpart. During on-demand drug amorphization, the drug molecularly disperses into a polymer to form an amorphous solid at elevated temperatures inside a tablet. This study investigates, for the first time, the utilization of photothermal plasmonic nanoparticles for on-demand drug amorphization as a new pharmaceutical application. For this, near-IR photothermal plasmonic nanoparticles were tableted together with a crystalline drug (celecoxib) and a polymer (polyvinylpyrrolidone). The tablets were subjected to a near-IR laser at different intensities and durations to study the rate of drug amorphization under each condition. During laser irradiation, the plasmonic nanoparticles homogeneously heated the tablet. The temperature was directly related to the rate and degree of amorphization. Exposure times as low as 180 s at 1.12 W cm-2 laser intensity with only 0.25 wt % plasmonic nanoparticles and up to 50 wt % drug load resulted in complete drug amorphization. Therefore, near-IR photothermal plasmonic nanoparticles are promising excipients for on-demand drug amorphization with laser irradiation.
AB - Poor aqueous drug solubility represents a major challenge in oral drug delivery. A novel approach to overcome this challenge is drug amorphization inside a tablet, that is, on-demand drug amorphization. The amorphous form is a thermodynamically instable, disordered solid-state with increased dissolution rate and solubility compared to its crystalline counterpart. During on-demand drug amorphization, the drug molecularly disperses into a polymer to form an amorphous solid at elevated temperatures inside a tablet. This study investigates, for the first time, the utilization of photothermal plasmonic nanoparticles for on-demand drug amorphization as a new pharmaceutical application. For this, near-IR photothermal plasmonic nanoparticles were tableted together with a crystalline drug (celecoxib) and a polymer (polyvinylpyrrolidone). The tablets were subjected to a near-IR laser at different intensities and durations to study the rate of drug amorphization under each condition. During laser irradiation, the plasmonic nanoparticles homogeneously heated the tablet. The temperature was directly related to the rate and degree of amorphization. Exposure times as low as 180 s at 1.12 W cm-2 laser intensity with only 0.25 wt % plasmonic nanoparticles and up to 50 wt % drug load resulted in complete drug amorphization. Therefore, near-IR photothermal plasmonic nanoparticles are promising excipients for on-demand drug amorphization with laser irradiation.
KW - amorphous solid dispersions
KW - in situ drug amorphization
KW - near-IR laser irradiation
KW - plasmonic nanoaggregates
U2 - 10.1021/acs.molpharmaceut.1c00077
DO - 10.1021/acs.molpharmaceut.1c00077
M3 - Journal article
C2 - 33951909
AN - SCOPUS:85106503744
VL - 18
SP - 2254
EP - 2262
JO - Molecular Pharmaceutics
JF - Molecular Pharmaceutics
SN - 1543-8384
IS - 6
ER -
ID: 273634612