1 Ocak 2022 Dergi makalesi Açık Erişim

Azizoglu, Erkan; Ozer, Ozgen; Prausnitz, Mark R.

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    <subfield code="a">Prausnitz, Mark R.</subfield>
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    <subfield code="a">Fabrication of pure-drug microneedles for delivery of montelukast sodium</subfield>
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    <subfield code="a">Azizoglu, Erkan</subfield>
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    <subfield code="c">2022-01-01</subfield>
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    <subfield code="a">Dissolving microneedle (MN) patches are usually formulated with a blend of drug and excipients added for mechanical strength and drug stabilization. In this study, we developed MNs made of pure drug to maximize drug loading capacity. MN patches were fabricated for transdermal delivery of montelukast sodium (MS) which is used to treat asthma and allergic rhinitis. We developed three different fabrication methods - solvent casting, melt casting, and solvent washing - and determined that filling molds with MS powder followed by a solvent washing method enabled MS to be loaded selectively to the MNs. Drug localization was confirmed with Raman imaging. MNs were able to penetrate in vitro and ex vivo skin models, and maintained strong mechanical properties during 6 months' storage at 22 degrees C. MS was also stable and compatible with the formulation used for the patch backing layer after 3 months' storage at 40 degrees C. MS delivery efficiency into skin was 55%, which enabled delivery of 3.2 mg MS into porcine skin ex vivo, which is in the range of MS doses in human clinical use. We conclude that the solvent washing method can be used to prepare MNs containing pure drug, such as MS at milligram doses in a similar to 1 -cm(2) MN patch.</subfield>
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