Abstract

Paeonol exhibits a wide range of pharmacological activities, such as anti-inflammatory, antidiabetic as well as pain-relieving activities. However, its intrinsic properties, such as low water solubility, poor stability and low oral bioavailability, restrict its clinical application. The current study aimed to optimize paeonol-loaded ethosomal formulation and characterize it in terms of encapsulation efficiency (EE), vesicle size (VS), zeta potential (ZP) and polydispersity index (PDI), in addition to differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) studies. Here, paeonol-loaded ethosomes were prepared by the injection method and optimized by the single-factor test and central composite design-response surface methodology. The optimized paeonol-loaded ethosomes had an EE of 84.33 ± 1.34%, VS of 120.2 ± 1.3 nm, negative charge of −16.8 ± 0.36 mV, and PDI of 0.131 ± 0.006. Ethosomes showed a spherical morphology under the transmission electron microscope (TEM). DSC, XRD and FT-IR results indicated that paeonol was successfully incorporated into the ethosomes. In-vitro transdermal absorption and skin retention of paeonol from paeonol-loaded ethosomes were 138.58 ± 9.60 µg/cm2 and 52.60 ± 7.90 µg/cm2, respectively. With reasonable skin tolerance, ethosomes could be a promising vehicle for transdermal delivery of paeonol.

Highlights

  • Paeonol (20 -hydroxy-40 -methoxyacetophenone) is the main active component found in peonies such as Paeonia moutan and Radix Cynanchi Paniculati [1]

  • Results of differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) experiments showed that the peaks in optimized formulations were diminished or suppressed, indicating successful incorporation of paeonol into the lipid matrix of ethosomes in amorphous or disordered states

  • The PAE ethosomes were prepared by the injection method, and optimized by the single-factor test and central composite design-response surface methodology

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Summary

Introduction

Paeonol (20 -hydroxy-40 -methoxyacetophenone) is the main active component found in peonies such as Paeonia moutan and Radix Cynanchi Paniculati [1]. Studies on the pharmacological activities of paeonol have proven their anti-inflammatory [2], antidiabetic [3], antiallergic [4] and antitumor [5]. Paeonol is a valuable drug with promising prospects. Oral administration of paeonol is limited by its low bioavailability, low water solubility [7] and poor stability [8]. In order to address these limitations, transdermal drug delivery systems (TDDSs) of paeonol were designed and prepared. With the development of medical technology, ethosomes have been shown to play an important role in TDDSs. Unlike conventional liposomes, ethosomes could effectively

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