Silibinin loaded inhalable solid lipid nanoparticles for lung targeting

Abstract

Aim

In the current study, efforts are being made to prepare Inhalable Silibinin loaded solid lipid nanoparticles (SLNs) with narrow size distribution with improved bioavailability.

Methods

SLNs were formulated by high shear homogenisation method SLNs were characterised, including Differential Scanning Calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR), particle size analysis, entrapment efficiency with Aerodynamic behaviour. The MTT assay was performed against A549 cell line, to measure their anticancer cell activity with In vivo study.

Results

Optimized formulation exhibited spherical surface with a mean particle size of 221 ± 1.251 nm, PI of 0.121 ±  0.081, zeta potential of −4.12 ± 0.744. Aerodynamic behaviour such as Mass median aerodynamic diameter (MMAD) and Geometric size distribution (GSD) were found to be 5.487 ± 0.072 and 2.321 ± 0.141 respectively proved formulation is suitable for inhalation. In vitro cellular efficacy against A549 cells, revealed that the optimised formulations were more effective and potent.

Conclusion

The Inhalable SLNs approach was successfully engineered and administered to the lungs safely without causing any problems.

Keywords:

• Lung cancer
• silibinin
• solid lipid nanoparticle
• inhalation delivery
• A549
• histopathology

Ethical approval

The animal protocol was approved by the Institutional Animal Ethics Committee (IAEC), constituted as per guidelines of the Committee for Purpose of Control and Supervision of Experiments on Animals Government of India (IAEC/DPS/SU/1713; dated 11th November 2017).

Acknowledgements

The authors are thankful to Gattefosse India Pvt. Ltd., Mumbai for providing Dynasan 114 and Glyceryl behenate as a gift sample. The authors also thank GmbH & Co. KG, Germany for providing 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) and dioleoyl-3-trimethylammonium propane (DOTAP) as a gift sample.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

Present research work was funded by Gujarat Council on Science and Technology, Government of Gujarat, Gandhinagar.