Comparative study of kanamycin sulphate microparticles and nanoparticles for intramuscular administration: preparation in vitro release and preliminary in vivo evaluation

Abstract

Kanamycin sulphate (KS) is a Mycobacterium tuberculosis protein synthesis inhibitor. KS is polycationic, a property responsible for KS poor oral absorption half-life (2.5 h) and rapid renal clearance, which results in serious nephrotoxicity/ototoxicity. The current study aimed to develop KS-loaded PLGA vitamin-E-TPGS microparticles (MPs) and nanoparticles (NPs) to reduce the dosing frequency and dose-related adverse effect. In vitro release was sustained up to 10 days for KS PLGA–TPGS MPs and 13 days for KS PLGA–TPGS NPs in phosphate-buffered saline (PBS) pH 7.4. The in vivo pharmacokinetic test in Wistar rats showed that the AUC_0–∞ of KS PLGA–TPGS NPs (280.58 μg/mL*min) was about 1.62-fold higher than that of KS PLGA–TPGS MPs (172.30 μg/mL*min). Further, in vivo protein-binding assay ascribed 1.20-fold increase in the uptake of KS PLGA–TPGS NPs through the alveolar macrophage (AM). The studies, therefore, could provide another useful tool for successful development of KS MPs and NPs.

Keywords:

• Microparticles
• nanoparticles
• PLGA
• pharmacokinetic
• in vivo distribution

Acknowledgements

The authors would like to thank Dr. Shobha Rani R. H, principal of Al-Ameen College of Pharmacy for her advice and support to carry out this research work. The authors are grateful to Karnataka antibiotics, Karnataka, India, for providing the gift sample of kanamycin sulphate.

Disclosure statement

The authors report no declarations of interest. The authors alone are responsible for the content and writing of this article.