Development of Ethyl Cellulose and Lecithin Nanoparticles: Permeability Enhancement for Berberine Topical Application

Berberine chloride (BER), a well-known traditional medicine, was renovated into topical application by using a nanoparticle platform with ethyl cellulose (EC) and lecithin (LEC). BER was prepared into nanoparticles by the solvent evaporation method. The investigated formulation parameters included BER (mg), EC (mg), LEC (mg), PVA concentration (%), and water volume (mL). The obtained nanoparticles were characterized by average particle size (Z, nm), polydispersity index (PDI), and encapsulation efficiency (%EE). Furthermore, the effects of inputs on outputs were analyzed by the JMP artificial neural network software to confirm the effects of inputs on outputs during screening. The structure and permeation mechanism of the nanoparticle system were predicted based on the effects of inputs on particle size, polydispersity index (PDI), and encapsulation efficiency. The optimal sample was analyzed with infrared, DSC spectra, and TEM images. The obtained nanoparticle system was loaded into ionic Sepimax Zen gel or non-ionic hydroxyethyl cellulose (HEC) gel for drug permeation study (in vitro and ex vivo). The average particle size of the obtained nanoparticles was less than 200 nm with a negative zeta potential. While EC proportions affected Z (nm) values, they did not have a significant impact on EE (%), according to JMP analysis. IR, DSC, and TEM results illustrated the structure of nanoparticles with EC as the core, while more hydrophilic ingredients like BER or LEC are more dynamic in nanosuspension. Despite a low EE %, the ex vivo data confirmed that gel containing BER nanoparticles provided a better permeation than raw suspension gels. In addition, two distinct gelling types, pre-neutralized Sepimax ZEN and hydroxyl ethyl cellulose (HEC), were proposed for BER nanoparticles. Sepimax exhibited a better drug retention, whereas HEC gel offered a superior permeability. This BER-EC-LEC nanoparticle provided a potential platform for topical application.