Eprinomectin nanoemulgel for transdermal delivery against endoparasites and ectoparasites: preparation, in vitro and in vivo evaluation

Yujuan Mao,Xiaolan Chen,Bohui Xu,Yan Shen,Zixuan Ye,Birendra Chaurasiya,Li Liu,Yi Li,Xiaoling Xing,Daquan Chen

doi:10.1080/10717544.2019.1682720

Abstract

Nanoemulgels are composed of O/W nanoemulsion and hydrogels and are considered as ideal carriers for the transdermal drug delivery because these have high affinity to load hydrophobic drugs. The stable formulation of eprinomectin (EPR) is very challenging because of it is high hydrophobic nature. In this work, we have prepared EPR loaded nanoemulgel for the treatment of endo- and ectoparasites. The surface morphology of optimized formulations was characterized by scanning electron microscopy. Additionally, skin permeability and irritation tests were conducted for in vitro safety and in vivo skin retention and pearmeation test of EPR nanoemulgel were conducted for efficacy study. Obtained results indicated that the optimized formulation had good shear-thinning behavior, bioadhesiveness properties, and are nanosized droplets with porous internal structure, which are required for topical application. Furthermore, this formulation has showed good skin permeability in comparison to suspension and has no skin irritating property. Overall, the obtained results proved that nanoemulgel is a promising carrier for transdermal drug delivery and EPR nanoemulgel is a promising formulation for the treatment of endo- and ectoparasites.

Highlights

Hydrogels, for its three-dimension cross-linked network structure, are well known as excellent carriers for drug-loading
From Figure 3(A,B), it can be seen that the content of castor oil has no significant effect on viscosity of EPR nanoemulgel but has significant effect on Ke
The Ke values of EPR nanoemulsion which contain 0.40 and 1.19 g castor oil were close to 0, whereas the Ke of 2.00 g castor oil group was 2.174, which implied that the nanoemulsion system would be unstable when the content of non-aqueous agent is over a critical value

Summary

Introduction

For its three-dimension cross-linked network structure, are well known as excellent carriers for drug-loading. The hydrophilicity of hydrogel limits the applications for the delivery of hydrophobic drugs. To overcome this shortfall, a novel transdermal delivery system termed emulgel was developed, where emulsion was thickened by hydrogel. Hydrophobic drugs were loaded in the oil cores and the droplets of emulsion are entrapped into the hydrogel cross-linked network. The drug release pattern and quantity from this emulgels are influenced by the types of gelling agents, concentration of emulsifier and oil base used in emulsion (Mohamed, 2004). By controlling emulsion bases in emulgels, the bioadhesive properties and sustained drug release pattern from emulgels can be controlled for prolonged therapeutic effect at desired site of action (Palcso et al, 2019)

Methods

Results

Conclusion