Citation: Qiyue Wang, Liang Ge, Lu Wang, Ying Xu, Si Miao, Guiping Yu, Yan Shen. Formulation optimization and in vitro antibacterial ability investigation of azithromycin loaded FDKP microspheres dry powder inhalation[J]. Chinese Chemical Letters, ;2021, 32(3): 1071-1076. doi: 10.1016/j.cclet.2020.03.062 shu

Formulation optimization and in vitro antibacterial ability investigation of azithromycin loaded FDKP microspheres dry powder inhalation

Qiyue Wang ^{a, 1} ,
Liang Ge ^{a, 1} ,
Lu Wang ^a ,
Ying Xu ^b ,
Si Miao ^a ,
Guiping Yu ^{c, *,} ,
Yan Shen ^{a, *,}

a.
Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
b.
College of Pharmacy, Jiangsu University, Zhenjiang 212013, China
c.
Department of Cardiothoracic Surgery, The Affiliated Jiangyin Hospital of Southeast University Medical College, Jiangyin 214400, China

Received Date: 5 February 2020
Revised Date: 20 March 2020
Accepted Date: 23 March 2020
Available Online: 2 April 2020

Figures(6)

Azithromycin loaded fumaryl diketopiperazine (FDKP) dry powder inhalationwas designed and prepared for the treatment of community-acquired pneumonia. The solubility of FDKP and stability of azithromycin solution was investigated. Formulation of azithromycin loaded FDKP microparticle was investigated and optimized by the single factor experiment. High-pressure homogenization and spray drying conditions were also optimized to prepare the particles by spray drying azithromycin dissolved FDKP microparticle suspension at pH 4.5. The in vitro antibacterial efficiency and in vitro dispersion performance was also investigated to confirm the antibacterial efficiency, dispersion and deposition behavers. FDKP/azithromycin mass ratio (3:2) was the optimized formulation of azithromycin loaded FDKP microparticle with the maximal drug loading efficiency. High-pressure homogenization and spray drying conditions were also optimized. The in vitro antibacterial results indicated that only with the antibiotic concentration higher than mutant prevention concentration could totally inhibit the reproduction of bacteria. In vitro dispersion performance of azithromycin loaded FDKP microparticles (AZM@FDKP-MPs) also shows remarkable improvement of dispersion and deposition behavers of AZM. AZM@FDKP-MPs dry powder inhalation as a targeting delivery route has better potential for lung infection treatment.
- Azithromycin,
- FDKP,
- Formulation optimization,
- In vitro antibacterial efficiency,
- Streptococcus pneumoniae
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