Open AccessPharmacokinetics and in vivo distribution of optimized PLGA nanoparticles for pulmonary delivery of levofloxacin
Author(s) -
Shah Sunny R.,
Prajapati Hani R.,
Sheth Devang B.,
Gondaliya Ekta M.,
Vyas Amit J.,
Soniwala Moinuddin M.,
Chavda Jayant R.
Publication year - 2020
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.13275
Subject(s) - pharmacokinetics , in vivo , levofloxacin , cmax , plga , particle size , pharmacology , bronchodilator , chemistry , homogenization (climate) , chromatography , materials science , medicine , in vitro , biochemistry , biology , microbiology and biotechnology , antibiotics , biodiversity , ecology , asthma
Objectives The aim of this study was to develop and optimize levofloxacin loaded PLGA nanoparticles (LN) for pulmonary delivery employing screening and experimental design and evaluate their in‐vitro and in‐vivo performance. The objective was to achieve Mass Median Aerodynamic Diameter (MMAD) of LN of less than 5μm, sustain the drug release up to 120 h and a higher AUC/MIC at the site of action. Methods LN were prepared by modified emulsion solvent evaporation technique employing high speed homogenization, probe sonication and subsequent lyophilization. Key Findings The Pareto chart from Placket Burman screening design revealed that homogenization speed and amount of PLGA were found to be significant ( P < 0.05). Further analysis by 3 full‐factorial design revealed that F‐ratio was found to be far greater than the theoretical value ( P < 0.05) for each regression model. Conclusion The optimized formulation with desirability value 0.9612 showed mean particle size of 146 nm, MMAD of 4.40 μm and sustained the drug release up to 120 h in simulated lung fluid. Augmentation in C max (1.71‐fold), AUC 0‐∞ (5.46‐fold), Mean Residence Time (6.64‐fold) and AUC/MIC (6.21‐fold) of LN through pulmonary route was found to significantly higher ( P < 0.05) than levofloxacin (p. o.).