Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

Abstract

Clarithromycin (CLR), categorized as a Biopharmaceutical Classification System class II drug, has several gastrointestinal tract side effects and an extremely unpalatable bitter taste. The current study aimed to design transdermal patch-embedded CLR niosomes to overcome the aforementioned CLR-related challenges. Various niosomal formulations were successfully fabricated and characterized for their morphology, size, in vitro release, and antimicrobial efficacy. Subsequently, the CLR niosomes were loaded into transdermal patches using the solvent casting method. The polydispersity index of the niosomes ranged from 0.005 to 0.360, indicating the uniformity of the niosomes. The encapsulating efficiency (EE)% varied from 12 to 86%. The optimal Chol: surfactant ratio for drug release was found to be 0.5:1. In addition, the encapsulation of CLR into niosomal nanovesicles did not reduce the antibacterial activity of the CLR. The niosomal patch had a significantly higher permeability coefficient of CLR than the conventional patch. In addition to that, a shear-thinning behavior was observed in the niosomal gels before loading them into a niosomal patch. The flux (Jss) of the niosomal patch was significantly higher than the conventional patch by more than 200 times. In conclusion, niosome-based transdermal patches could be a promising method for the transdermal drug delivery of class II drugs and drugs experiencing GIT side effects.

Kaempferia parviflora Extracellular Vesicle Loaded with Clarithromycin for the Treatment of Helicobacter pylori Infection

“…36 The drug solubility in PBS and SGF buffer is 0.12 mg/mL and 0.5 mg/mL, respectively. 46,47 Therefore, we used a releasing media volume at least 6 times greater than the drug solubility for ensuring sink conditions. The kinetic releases of CLA from KPEVs were similar under neutral and gastric mimic environments.…”

Breaking boundaries: the advancements in transdermal delivery of antibiotics

“…A study was conducted by Zaid Alkilani and colleagues (Zaid Alkilani et al., 2023 ) to develop transdermal patches loaded with CLR niosomes, using the solvent casting technique. The niosomes were spherical in shape with a size ranged between 109.0 and 552.1 nm, based on the ratio of cholesterol:surfactant (Span 60).…”

Niosome as an Effective Nanoscale Solution for the Treatment of Microbial Infections

“…In another study, clarithromycin (CLR) niosomes incorporated in transdermal patches were developed by Alkilani et al to address the problems with CLR stated above. The niosomal patch's flux (Jss) was more than 200 times greater than that of the traditional patch [ 28 ]. For example, studies conducted in 2016 by Sohrabi et al showed that the niosomal formula increased antibacterial activity against P. aeruginosa .…”