Formulation of chitosan coated nanoliposomes for the oral delivery of colistin sulfate: in vitro characterization, 99m Tc-radiolabeling and in vivo biodistribution studies.

Autor: Aboumanei MH; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo, Egypt., Mahmoud AF; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo, Egypt., Motaleb MA; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo, Egypt.
Jazyk: angličtina
Zdroj: Drug development and industrial pharmacy [Drug Dev Ind Pharm] 2021 Apr; Vol. 47 (4), pp. 626-635. Date of Electronic Publication: 2021 Apr 09.
DOI: 10.1080/03639045.2021.1908334
Abstrakt: Colistin sulfate is a very important antibiotic for the treatment of multidrug-resistant Gram-negative infections. Unfortunately, it has low oral bioavailability and several side effects following parenteral administration. The present study aims to develop chitosan-coated colistin nanoliposomes to improve the stability in the gastrointestinal tract and to enhance the oral delivery of colistin. The chitosan-coated colistin nanoliposomes were obtained via thin-film evaporation and electrostatic deposition methods using either Span 60, Tween 65 or Tween 80 as surfactants with different cholesterol: surfactant: soya lecithin ratios. The influence of systems variables was further characterized by vesicle size analysis, zeta potential (ZP), poly dispersibility index (PDI), and also their entrapment efficiency percentage (EE %) was evaluated. Various systems were formed with vesicle sizes in the nano-range, 155.64 ± 12.53 nm to 315.64 ± 15.90 nm, and EE % of 45.2 ± 2.9% to 81.8 ± 2.9%. Moreover, the ZP value of the prepared nanoliposomes switched from a negative to a positive value after chitosan coating. To track the released colistin in vivo, technetium 99m ( 99m Tc) was incorporated into the optimum system (S-3) system via direct coupling with colistin. Chitosan-coated 99m Tc-colistin nanoliposome, 99m Tc-colistin suspension, and 99m Tc-chitosan-coated nanoliposomes (placebo) were administered orally into bacterial infection ( Escherichia coli ) bearing mice. The biodistribution results showed that chitosan-coated nanoliposome significantly enhanced the bioavailability of colistin compared to colistin suspension (the commercially available). Moreover, the system effectively improved the localization of colistin at the infected muscle. In conclusion, this approach offers a promising tool for enhanced oral delivery of colistin.
Databáze: MEDLINE
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