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Open AccessArticle

Characterization and Formulation of Isoniazid for High-Dose Dry Powder Inhalation

Department of Pharmaceutical Technology and Biopharmacy, Faculty of Science and Engineering, University of Groningen, 9700 AB Groningen, The Netherlands
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Pharmaceutics 2019, 11(5), 233; https://doi.org/10.3390/pharmaceutics11050233
Received: 5 April 2019 / Revised: 8 May 2019 / Accepted: 9 May 2019 / Published: 13 May 2019
(This article belongs to the Special Issue Advances in Pulmonary Drug Delivery)
Tuberculosis is a major health problem and remains one of the main causes of mortality. In recent years, there has been an increased interest in the pulmonary delivery of antibiotics to treat tuberculosis. Isoniazid is one of these antibiotics. In this study, we aimed to characterize isoniazid and formulate it into a dry powder for pulmonary administration with little or no excipient, and for use in the disposable Twincer® inhaler. Isoniazid was jet milled and spray dried with and without the excipient l-leucine. Physiochemical characterization showed that isoniazid has a low Tg of −3.99 ± 0.18 °C and starts to sublimate around 80 °C. Milling isoniazid with and without excipients did not result in a suitable formulation, as it resulted in a low and highly variable fine particle fraction. Spray drying pure isoniazid resulted in particles too large for pulmonary administration. The addition of 5% l-leucine resulted in a fraction <5 µm = 89.61% ± 1.77% from spray drying, which dispersed well from the Twincer®. However, storage stability was poor at higher relative humidity, which likely results from dissolution-crystallization. Therefore, follow up research is needed to further optimize this spray dried formulation. View Full-Text
Keywords: high dose pulmonary delivery; dry powder inhaler; drug formulation; inhalation; tuberculosis high dose pulmonary delivery; dry powder inhaler; drug formulation; inhalation; tuberculosis
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MDPI and ACS Style

Sibum, I.; Hagedoorn, P.; Frijlink, H.W.; Grasmeijer, F. Characterization and Formulation of Isoniazid for High-Dose Dry Powder Inhalation. Pharmaceutics 2019, 11, 233.

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