Assessing the Synergistic Activity of Clarithromycin and Therapeutic Oils Encapsulated in Sodium Alginate Based Floating Microbeads

Abstract

We developed alginate-based floating microbeads of clarithromycin with therapeutic oils for the possible eradication of Helicobacter pylori (H. pylori) infections by enhancing the residence time of the carrier at the site of infection. In pursuit of this endeavor, the alginate was blended with hydroxy propyl methyl cellulose (HPMC) as an interpenetrating polymer to develop beads by ionotropic gelation using calcium carbonate as a gas generating agent. The developed microbeads remained buoyant under gastric conditions for 24 h. These microbeads initially swelled and afterwards decreased in size, possibly due to the erosion of the polymer. Furthermore, swelling was also affected by the type of encapsulated oil, i.e., swelling decreased with increasing concentrations of eucalyptus oil and increased with increasing concentrations of oleic acid. Antibacterial assays of the formulations showed significant antibacterial activity against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli); these assays also showed synergistic activity between clarithromycin and therapeutic oils as evident from the higher zone of inhibition of the microbeads as compared to the pure drug and oils. Scanning electron microscopy (SEM) images revealed a smoother surface for oleic acid containing the formulation as compared to eucalyptus oil containing the formulation. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) revealed the development of a stable formulation, while Fourier transform infrared spectrophotometry (FTIR) studies did not reveal any interaction between the polymers and the active ingredients. Optimized formulations (CLM3 and CLM6) were designed to release the drug in a controlled manner in gastric media by Fickian diffusion. Conclusively, the developed microbeads are a promising carrier to overcome the narrow therapeutic index and low bioavailability of clarithromycin, while the presence of therapeutic oils will produce synergistic effects with the drug to eradicate infection effectively.

Green fabrication of ZnO nanoparticles via spirulina platensis and its efficiency against biofilm forming pathogens

“…The search for innovative antibiofilm agents could lead to new approaches for controlling infections and provide solutions to biofilm-related problems [ 66 ]. According to earlier studies, nanoparticles may have an impact on the life cycles of bacteria, which in turn can alter their activities such as cell-cell communication [ 65 ], many biogenic nanoparticles have been shown to successfully eradicate bacterial biofilms [ 26 ]. In the present study we investigate the antibiofilm potentiality of ZnO NPs on the challenging biofilm-forming bacterial strains, from the results represented in Fig.…”

“…Another previous report revealed the bioefficiency of ZnO NPs synthesized using plantain peel extract against Staphylococcus aureus 26,923, Bacillus cereus MTCC 430, Salmonella enterica , and Klebsiella pneumoniae with minimum inhibitory concentration (MIC) of 100 µg/mL against the tested strains [ 25 ]. Biofilm creation is a public health issue as it is the major cause of multidrug resistance Khan et al [ 26 ] reported that ZnO NPs suppress the growth and biofilm formation of a wide range of bacterial isolates. Therefore, it was of considerable importance to scrutinize the role of ZnO NPs underlining their antimicrobial toxicity against well-known human pathogens including both Gram-negative and Gram-positive pathogenic bacterial isolates.…”

The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole

“…At a low pH, carboxylate groups are partially unionized, which results in polymer shrinkage and decreased swelling ability at pH 1.2. The addition of HPMC, which interpenetrates ALG within the microparticles structure, provides improved swelling capacity [ 37 ]. HPMC in contact with a moisture environment is characterized by rapid water uptake.…”

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

“…IR spectroscopy was used to investigate the probability of drug interaction with other substances in the manufactured TEL-loaded oil-entrapped beads [ 41 ]. Infrared spectroscopy was used to characterize the drug, sodium alginate, and the optimized formulation.…”