Design and evaluation of hyaluronic acid-coated PLGA nanoparticles of raloxifene hydrochloride for treatment of breast cancer

Abstract

Context

In the present study, hyaluronic acid (HA)-coated raloxifene-loaded poly(l-lactic-co-glycolic acid) (PLGA) nanoparticles have been developed to improve the anticancer potential and reduce side effects associated with the drug.

Aim and objectives

The investigation was aimed to formulate and optimize raloxifene hydrochloride (RALH)-loaded PLGA nanoparticles with surface modification using HA as a targeting moiety. To perform physicochemical characterization, in vitro cytotoxicity study (using MCF-7), in vitro drug release study and in vivo pharmacodynamic study of optimized formulation.

Methodology

Raloxifene hydrochloride-loaded PLGA nanoparticles were prepared by nanoprecipitation technique, followed by surface modification with HA. Formulation was optimized by using 23 factorial design and characterized by physicochemical, in vitro drug release, in vitro cytotoxicity studies, and in vivo pharmacokinetics.

Results and discussion

The particle size, PDI, zeta potential, entrapment efficiency, and loading capacity of spherically shaped RALH-loaded nanoparticles were 207.3 ± 4.2 d.nm, 0.218 ± 0.127, −.127 mV, 43.75 ± 1.2%, and 7.55 ± 1.14%, respectively. The in vitro drug release showed sustained release and followed Korsmeyer-Peppas model with non-Fickian release pattern. The in vitro cytotoxicity study of drug-loaded NPs by MTT assay on MCF-7 breast carcinoma cell showed anti-cancer activity after 48 h of treatment.

Conclusion

The results of the present investigation suggested that RALH-loaded HA-modified PLGA nanoparticles showed sustained drug release with anticancer activity and can be a promising approach for treatment of breast cancer.

Keywords:

• Hyaluronic acid
• raloxifene hydrochloride
• PLGA nanoparticles
• sustained release
• breast cancer
• optimization
• factorial design

Acknowledgements

We acknowledge Zydus Cadila Healthcare Ltd., Ahmedabad, India for providing gift sample of raloxifene hydrochloride and Evonic Ltd., India for providing PLGA.

Disclosure statement

Authors have no declaration of interest.

Additional information

Funding

The authors are thankful to All India Council for Technical Education, New Delhi for providing financial support to Kajol Bhatt pn form of Junior Research Fellow.