Encapsulation and Characterization of Nanoemulsions Based on an Anti-oxidative Polymeric Amphiphile for Topical Apigenin Delivery.

Tzung-Han Chou,Yu-Shen Cheng,Ming-Jay Deng,Chia-Hua Liang,Jia-Yaw Chang,Daniel Setiyo Nugroho

doi:10.3390/polym13071016

Abstract

Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials. Nevertheless, its poor water solubility and low storage stability have limited its application feasibility on the pharmaceutical field. To address this issue, this study developed nanoemulsions (NEs) using an anti-oxidative polymeric amphiphile, d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydrogenated soy lecithin (HL), black soldier fly larvae (BSFL) oil, and avocado (AV) oil through pre-homogenization and ultrasonication method. Addition of TPGS (weight ratios 100 and 50% as compared to HL) into NEs effectively reduced particle size and phase transition region area of NEs with pure HL. Incorporation of Apig into NEs made particle size increase and provided a disorder effect on intraparticle molecular packing. Nevertheless, the encapsulation efficiency of NEs for Apig approached to about 99%. The chemical stability of Apig was significantly improved and its antioxidant ability was elevated by incorporation with BSFL oil and AV oil NEs, especially for NEs with single TPGS. NEs with single TPGS also exhibited the best Apig skin deposition. For future application of topical Apig delivery, NEs-gel was formed by the addition of hyaluronic acid (HA) into NEs. Their rheological characteristics were dominated by the surfactant ratios of HL to TPGS.

Highlights

Apigenin (Apig) is one of the natural dietary flavonoid compounds originating from the Apiaceae family [1], and it can be found in fruits, vegetables, and herbs [2]
The comparations of average particle size determined from the Transmission Electron Microscopy (TEM) images and DLS measurement showed no significant difference
The droplets ware distributed moderately homogeneous throughout the formulations with slight aggregation observed in several dispersion systems

Summary

Introduction

Apigenin (Apig) is one of the natural dietary flavonoid compounds originating from the Apiaceae family [1], and it can be found in fruits, vegetables, and herbs [2]. Apig is classified as a BCS (Biopharmaceutical Classification System) II drug with low water solubility that hinders its bioavailability [5]. To overcome the problem of drug solubility, different carriers such as ethosomes [6], nanoparticle [7], liposomes [8], and O/W emulsions [9] have been introduced to encapsulate Apig. Employing liposomes and ethosomes on drugs may induce unexpected side effects in humans [10,11], and their protectional performances on the chemical stability of Apig are still not very clear. Among the delivery systems mentioned above, nanoemulsions (NEs) are a suitable vehicle for Apig because they exhibit high potential to improve the water solubility and bioavailability of several oil-soluble phytochemicals including quercetin [12], catechin [13], β-carotene [14], and emodin [15]. The utilization of nanoemulsions is a good candidate for application of topical Apig delivery

Methods

Results

Conclusion