Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System

Abstract

Zerumbone extracted from the volatile oil of rhizomes available from the Zinigiber zerumbet has promising pharmacological activity. However, it has poor aqueous solubility and dissolution characteristics. To improve this, a nanosuspension formulation of zerumbone was developed. Nanosuspensions were formulated using high-pressure homogenization (HPH) with sodium dodecyl sulphate (SDS) and hydroxypropylmethylcellulose (HPMC) as stabilizers; the formulation was optimized and freeze dried. The optimized nanosuspension product was evaluated using an optical light microscope, photon correlation spectroscopy (PCS), polydispersity index, zeta potential, SEM, differential scanning calorimetry (DSC) and FT-IR. The physical stability of the nanosuspensions was evaluated for 30 days at 4 • C, 25 • C, and 37 • C. To validate the theoretical benefit of the increased surface area, we determined an in vitro saturation solubility and dissolution profile. The mean particle size, polydispersity index and zeta potential of the zerumbone nanosuspensions stabilized by SDS versus HPMC were found to be 211 ± 27 nm vs. 398 ± 3.5 nm, 0.39 ± 0.06 vs. 0.55 ± 0.004, and −30.86 ± 2.3 mV vs. −3.37 ± 0.002 mV, respectively. The in vitro saturation solubility and dissolution revealed improved solubility for the zerumbone nanosuspension. These results suggested that the nanosuspensionlization improves the saturation solubility and dissolution profile of zerumbone, which may facilitate its use as a therapeutic agent in the future.

Development of Polymer and Surfactant Based Naringenin Nanosuspension for Improvement of Stability, Antioxidant, and Antitumour Activity

“…HPMC-based nanosuspensions showed steric stabilization by getting adsorbed into the surface of the dispersed nanoparticles providing a steric hindrance [21]. e obtained zeta potential was reasonably good for a stable nanosuspension, and this matched with some reported values for HPMC-stabilized nanoparticles [22][23][24]. For the optimized SDS-stabilized nanosuspension, the value of the zeta potential was −40.75 ± 2.76 mV (Figure 1(d)).…”

Nanosuspension-Based Dissolving Microneedle Arrays for Intradermal Delivery of Curcumin

“…In previous studies, it has been shown that the incorporation of SLS yields smaller particle sizes compared to other stabilisers. For instance, SLS was used previously to prepare zerumbone nanosuspensions, which showed a particle size distribution significantly lower than those obtained using hydroxypropyl methylcellulose (HPMC) as stabiliser [23]. Additionally, Elham et al [24] prepared glipizide formulations using HPMC, Tween 80, poloxamer and SLS as stabilisers.…”

Formulation and Nanotechnology-Based Approaches for Solubility and Bioavailability Enhancement of Zerumbone

“…It is completely soluble in dimethyl sulfoxide (DMSO) and ethanol but has extremely poor solubility in water (~1–1.5 mg/L at 25 °C) [ 34 , 58 ]. Zerumbone is highly lipophilic and the poor water solubility contributes to poor absorption, low oral bioavailability, and limited targeting to tissues and organs of interest [ 28 , 35 , 36 , 37 , 47 , 48 ]. The chemical structure and other physicochemical characteristics of zerumbone are presented in Figure 1 and Table 1 , respectively.…”

“…The authors report an increase in solubility, stability, and dissolution profile of zerumbone nanosuspension as compared to zerumbone alone. The results from this study provide evidence of the potential of nanosuspension technology to enhance the therapeutic potential of zerumbone in the future and warrant further in-vivo evaluation [ 48 ].…”

“…However, despite promising in-vitro and in-vivo studies demonstrating the therapeutic utility of zerumbone, its preclinical and clinical development has been limited due to its poor water solubility, poor absorption, or low bioavailability, limiting its targeting into various tissues and organs of interest. Hence, to advance the therapeutic potential in various diseases and overcome the biopharmaceutical challenges of zerumbone, it is essential to develop advanced formulation and nanotechnology-based approaches [ 28 , 35 , 36 , 37 , 47 , 48 ].…”