Abstract

Nanosuspensions are widely reported to enhance the solubility of poorly soluble drugs. In addition to enhancement in solubility, improvement of stability and therapeutic efficacy would be an added advantage. In the present study, premilling and subsequent high-pressure homogenization were carried out to produce naringenin nanosuspension. Hydroxypropyl methylcellulose and sodium dodecyl sulfate were evaluated for their performance as stabilizers under various homogenization cycles. The prepared nanosuspensions were studied for average particle size and size distribution, zeta potential, solubility, drug release, antioxidant activity, and in vitro antitumor activity. It was observed that both hydroxypropyl methylcellulose-stabilized nanosuspension and sodium dodecyl sulfate-stabilized nanosuspension produced an enhancement in physical stability, antioxidant potential, and in vitro cytotoxicity compared with naringenin. Furthermore, hydroxypropyl methylcellulose-stabilized nanosuspension was found to be better than sodium dodecyl sulfate-stabilized nanosuspension in terms of particle size and size distribution, storage stability, and drug release. This study showed that nanosuspension formulations could be a potential strategy for improving dissolution and antitumor activity of naringenin.

Highlights

  • Breast cancer has been the major cause of cancer-related deaths in women

  • Hydroxypropyl methylcellulose (HPMC)- and sodium dodecyl sulfate (SDS)-stabilized systems are reported for nanosuspensions [14,15,16]

  • HPMC and SDS were evaluated for their performance as stabilizers under homogenization cycles of 1, 5, 10, 15, and 20. e prepared nanosuspensions were studied for particle size and size distribution, zeta potential, solubility, drug release, antioxidant activity, and in vitro antitumor activity. e particle size and size distribution were determined by Photon Correlation Spectroscopy (PCS). e homogenization cycle was found to affect the average particle size and the polydispersity index (PDI)

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Summary

Introduction

Breast cancer has been the major cause of cancer-related deaths in women. Breast cancer can be treated by chemotherapy and other methods [1]. Ere have been no studies on the anticancer or antioxidant effects of NAR nanosuspensions, other flavonoids, such as apigenin, puerarin, and diosmin, in the nanosuspension were shown, respectively, to have increased antioxidant activity [8], anticancer actions with lower toxicity [10], band-enhanced permeation, and dissolution characteristics for better drug delivery [11]. Erefore, evaluation of NAR nanosuspensions for antioxidant and antitumor activity on the breast cancer cell line was warranted. Antitumor activity of NAR nanosuspensions was examined in a breast cancer cell line (MCF-7 cells), and its in vitro antioxidant potential was determined and compared with free drug solution

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