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.
Highlights
An estimated 80% of the world population relies on traditional therapies, mostly involving the use of natural compounds
The high-pressure homogenization (HPH) technique was used in the preparation of the zerumbone nanosuspensions
Stabilisers were added to nanosuspension formulations to diminish the free energy of the system by diminishing the interfacial tension as well as to prevent the nanoparticle aggregation through the electrostatic/steric stabilisation [15]
Summary
An estimated 80% of the world population relies on traditional therapies, mostly involving the use of natural compounds. Zerumbone has been shown to possess strong in vitro antitumor activity in cell lines. Nanosuspension is one one strategy strategy used used to to improve bioavailability of poorly soluble drugs [8]. The size of a nanosuspensions improves the saturation solubility saturation solubility and and dissolution dissolution rate rate of of the the drug, drug, leading leading to to an an increase increase in in oral oral bioavailability. Apart from improved bioavailability, nanosuspensions offer enhanced stability, reduced. Apart from improved bioavailability, nanosuspensions offer enhanced stability, reduced systemic systemic toxicity and increased pharmacodynamic action [12].
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