Academic Journal

In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations

التفاصيل البيبلوغرافية
العنوان: In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations
المؤلفون: Changzhi Shi, Kewei Guo, Li Zhang, Yi Guo, Yu Feng, Sandra Cvijić, Dongmei Cun, Mingshi Yang
المصدر: Pharmaceutics, Vol 15, Iss 9, p 2287 (2023)
بيانات النشر: MDPI AG, 2023.
سنة النشر: 2023
المجموعة: LCC:Pharmacy and materia medica
مصطلحات موضوعية: respiratory infections, ciprofloxacin, sustained drug release, dry powder for inhalation, pulmonary drug exposure, Pharmacy and materia medica, RS1-441
الوصف: Respiratory antibiotics delivery has been appreciated for its high local concentration at the infection sites. Certain formulation strategies are required to improve pulmonary drug exposure and to achieve effective antimicrobial activity, especially for highly permeable antibiotics. This study aimed to investigate lung exposure to various inhalable ciprofloxacin (CIP) formulations with different drug release rates in a rat model. Four formulations were prepared, i.e., CIP-loaded PLGA micro-particles (CHPM), CIP microcrystalline dry powder (CMDP), CIP nanocrystalline dry powder (CNDP), and CIP spray-dried powder (CHDP), which served as a reference. The physicochemical properties, drug dissolution rate, and aerosolization performance of these powders were characterized in vitro. Pharmacokinetic profiles were evaluated in rats. All formulations were suitable for inhalation (mass median aerodynamic diameter < 5 µm). CIP in CHPM and CHDP was amorphous, whereas the drug in CMDP and CNDP remained predominantly crystalline. CHDP exhibited the fastest drug release rate, while CMDP and CNDP exhibited much slower drug release. In addition, CMDP and CNDP exhibited significantly higher in vivo lung exposure to CIP compared with CHDP and CHPM. This study suggests that lung exposure to inhaled drugs with high permeability is governed by drug release rate, implying that lung exposure of inhaled antibiotics could be improved by a sustained-release formulation strategy.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1999-4923
Relation: https://www.mdpi.com/1999-4923/15/9/2287; https://doaj.org/toc/1999-4923
DOI: 10.3390/pharmaceutics15092287
URL الوصول: https://doaj.org/article/6042943fe3f44a09ac4b1c99ed9c8255
رقم الانضمام: edsdoj.6042943fe3f44a09ac4b1c99ed9c8255
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:19994923
DOI:10.3390/pharmaceutics15092287