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

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In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations. / Shi, Changzhi; Guo, Kewei; Zhang, Li; Guo, Yi; Feng, Yu; Cvijić, Sandra; Cun, Dongmei; Yang, Mingshi.

In: Pharmaceutics, Vol. 15, No. 9, 2287, 2023.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Shi, C, Guo, K, Zhang, L, Guo, Y, Feng, Y, Cvijić, S, Cun, D & Yang, M 2023, 'In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations', Pharmaceutics, vol. 15, no. 9, 2287. https://doi.org/10.3390/pharmaceutics15092287

APA

Shi, C., Guo, K., Zhang, L., Guo, Y., Feng, Y., Cvijić, S., Cun, D., & Yang, M. (2023). In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations. Pharmaceutics, 15(9), [2287]. https://doi.org/10.3390/pharmaceutics15092287

Vancouver

Shi C, Guo K, Zhang L, Guo Y, Feng Y, Cvijić S et al. In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations. Pharmaceutics. 2023;15(9). 2287. https://doi.org/10.3390/pharmaceutics15092287

Author

Shi, Changzhi ; Guo, Kewei ; Zhang, Li ; Guo, Yi ; Feng, Yu ; Cvijić, Sandra ; Cun, Dongmei ; Yang, Mingshi. / In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations. In: Pharmaceutics. 2023 ; Vol. 15, No. 9.

Bibtex

@article{31f66060fe684d39856bf4873648c574,
title = "In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations",
abstract = "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.",
keywords = "ciprofloxacin, dry powder for inhalation, pulmonary drug exposure, respiratory infections, sustained drug release",
author = "Changzhi Shi and Kewei Guo and Li Zhang and Yi Guo and Yu Feng and Sandra Cviji{\'c} and Dongmei Cun and Mingshi Yang",
note = "Publisher Copyright: {\textcopyright} 2023 by the authors.",
year = "2023",
doi = "10.3390/pharmaceutics15092287",
language = "English",
volume = "15",
journal = "Pharmaceutics",
issn = "1999-4923",
publisher = "MDPI AG",
number = "9",

}

RIS

TY - JOUR

T1 - In Vitro and In Vivo Evaluation of Inhalable Ciprofloxacin Sustained Release Formulations

AU - Shi, Changzhi

AU - Guo, Kewei

AU - Zhang, Li

AU - Guo, Yi

AU - Feng, Yu

AU - Cvijić, Sandra

AU - Cun, Dongmei

AU - Yang, Mingshi

N1 - Publisher Copyright: © 2023 by the authors.

PY - 2023

Y1 - 2023

N2 - 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.

AB - 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.

KW - ciprofloxacin

KW - dry powder for inhalation

KW - pulmonary drug exposure

KW - respiratory infections

KW - sustained drug release

U2 - 10.3390/pharmaceutics15092287

DO - 10.3390/pharmaceutics15092287

M3 - Journal article

C2 - 37765256

AN - SCOPUS:85172475602

VL - 15

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 9

M1 - 2287

ER -

ID: 369859974