Development and optimization of erythromycin-loaded lipid-based gel by Taguchi design: In vitro characterization and antimicrobial evaluation

The foremost aim of the current research was to prolong and sustain the release of erythromycin (ERY) by preparing a solid lipid nanoparticles (SLNs)-based gel formulation for the safe and effective treatment of acne. ERY-loaded SLNs were developed, and various process variables were optimized with respect to particle size, zeta potential, and entrapment efficiency using the Taguchi model. The average particle size, PDI, zeta potential, drug entrapment efficiency, and drug loading of optimized SLN (F4) were found to be 176.2±1.82 nm, 0.275±0.011, -34.0±0.84, 73.56%, and 69.74% respectively. The optimized SLN (F4) was successfully incorporated into the carbopol-based hydrogel. The in vitro release of ERY from the SLN gel and plain gel were compared and found to be 90.94% and 87.94% respectively. In vitro study of ERY-loaded SLN gel showed sustained delivery of drug from formulation thus enhancing the antimicrobial activity after 30 hours when compared to ERY plain gel.

本研究的首要目标为制备基于固体脂质纳米粒（solid lipid nanoparticles, SLNs）的凝胶制剂，以延长并维持红霉素（erythromycin, ERY）的释放，实现痤疮的安全有效治疗。本研究制备了载红霉素固体脂质纳米粒，并采用田口模型（Taguchi model）针对粒径、Zeta电位与包封率对多项工艺变量进行了优化。经优化得到的最优制剂F4型固体脂质纳米粒，其平均粒径、多分散指数（polydispersity index, PDI）、Zeta电位、药物包封率与载药量分别为176.2±1.82 nm、0.275±0.011、-34.0±0.84、73.56%与69.74%。将该最优F4型固体脂质纳米粒成功掺入卡波姆基水凝胶中。对载红霉素固体脂质纳米粒凝胶与普通红霉素凝胶的体外药物释放行为进行对比，结果显示二者的累积释放率分别为90.94%与87.94%。体外研究表明，与普通红霉素凝胶相比，载红霉素固体脂质纳米粒凝胶可实现药物的持续递送，在30小时后仍能增强其抗菌活性。