Hesperidin-Loaded Lipid Polymer Hybrid Nanoparticles for Topical Delivery of Bioactive Drugs.

Rajendra Jangde,Gamal Osman Elhassan,Deependra Singh,Ram Kumar Sahu,Manju Singh,Sulekha Khute,Jiyauddin Khan

doi:10.3390/ph15020211

Abstract

Hesperidin is a bioflavonoid constituent that among many other biological activities shows significant wound healing properties. However, the bioavailability of hesperidin when applied topically is limited due to its low solubility and systemic absorption, so novel dosage forms are needed to improve its therapeutic efficacy. The objectives of this study were to develop hesperidin-loaded lipid-polymer hybrid nanoparticles (HLPHNs) to enhance the delivery of hesperidin to endogenous sites in the wound bed and promote the efficacy of hesperidin. HLPHNs were optimized by response surface methodology (RSM) using the Box-Behnken design. HLPHNs were prepared using an emulsion-solvent evaporation method based on a double emulsion of water-in-oil-in-water (w/o/w) followed by freeze-drying to obtain nanoparticles. The prepared formulations were characterized using various evaluation parameters. In addition, the antioxidant activity of HLPHN 4 was investigated in vitro using the DPPH model. Seventeen different HLPHNs were prepared and the HLPHN4 exhibited the best mean particle size distribution, zeta potential, drug release and entrapment efficiency. The values are 91.43 nm, +23 mV, 79.97% and 92.8%, respectively. Transmission electron microscope showed similar spherical morphology as HLPHN4. Differential scanning calorimetry verified the physical stability of the loaded drug in a hybrid system. In vitro release studies showed uniform release of the drug over 24 h. HLPHN4 showed potent antioxidant activity in vitro in the DPPH model. The results of this study suggest that HLPHNs can achieve sustained release of the drug at the wound site and exhibit potent in vitro antioxidant activity.

Highlights

Introduction iationsHesperidin (Figure 1) is a bioflavonoid mainly extracted from various citrus fruits
The use of hesperidinloaded lipid-polymer hybrid nanoparticles (HLPHNs) has demonstrated a wide range of success in the implementation of novel clinical and drug delivery applications, as demonstrated by our recent evaluation of a novel drug delivery system for in vitro antioxidant activity in the DPPH model
The results of the current study suggest that the interaction between the ratio of surfactants and lipids affects particle size or decreases particle size as a function of drug concentration

Summary

Introduction

Hesperidin (Figure 1) is a bioflavonoid mainly extracted from various citrus fruits. Numerous researchers have found that hesperidin has antioxidant properties and possesses antitumor, antimicrobial, anti-inflammatory, antidiabetic and hepatoprotective effects [1,2]. The significant wound-healing effect of hesperidin has been demonstrated in animal models of excision wound healing and in clinical studies. Hesperidin reduces the formation of fibroses and scars after wound healing in experimental animals. Hesperidin is used to treat tropical infections by placing a dressing over them. Several studies have focused on the local delivery of the drug for the healing process of the wound through the dressing. This could avoid adverse effects on non-target tissues

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Conclusion