Improving the 6-Aminopenicillanic acid release process using vermiculite-alginate biocomposite bead on drug delivery system

Drug Dev Ind Pharm. 2021 Sep;47(9):1489-1501. doi: 10.1080/03639045.2021.2001492. Epub 2021 Dec 3.

Abstract

The present study deals with developing vermiculite (VMT)-alginate (Alg) composites with different cross-linker concentrations (CaCl2) to deliver the controlled 6-aminopenicillin acid (6-APA). The Characterization of synthesized composites was conducted by Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analyses. Optimization attempts were explored via the response surface method (RSM) to best predict the actual amount of compound. The adsorption capacity of 6-APA onto this adsorbent was found to be 208.33 mg/g, which was higher than that for other clays. The equilibrium and Kinetic studies (chemical reaction and diffusion-based models) indicated that drug absorption on VMT-Alg is homogeneous with chemical interaction. An increase in cross-linker (CaCl2) concentration leads to improvement in the drug encapsulation efficiency while having no significant effect on loading efficiency. The in-vitro release of the pure drug shows a rapid burst release followed by 100% cumulative release within 6 h. Whereas, the synthesized drug with Alg substantially showed less release of 43% after 8 h. Release experiments revealed that the presence of the CaCl2 delayed the release of the 6-APA less than 35% after 12 h. The kinetic release of 6-APA is followed by the Korsmeyer-Peppas model based on Fick's law mechanism due to the kinetic exponent (n < 0.5). All studied composites antibacterial activity after 24 h exposure against E. Coli and S. aureus. The antibacterial activities of composites were evaluated by the halo of no growth. The results showed that the VMT-Alg-6APA composite had strong activity against Gram-positive and Gram-negative bacteria.

Keywords: 6-Aminopenicillanic acid; antibacterial activity; drug release; equilibrium and kinetic studies; vermiculite-alginate biocomposite.

MeSH terms

  • Alginates* / chemistry
  • Aluminum Silicates
  • Anti-Bacterial Agents* / chemistry
  • Anti-Bacterial Agents* / pharmacology
  • Calcium Chloride
  • Drug Delivery Systems
  • Escherichia coli
  • Glucuronic Acid / chemistry
  • Gram-Negative Bacteria
  • Gram-Positive Bacteria
  • Kinetics
  • Penicillanic Acid / analogs & derivatives
  • Spectroscopy, Fourier Transform Infrared
  • Staphylococcus aureus

Substances

  • Alginates
  • Aluminum Silicates
  • Anti-Bacterial Agents
  • vermiculite
  • Penicillanic Acid
  • Glucuronic Acid
  • Calcium Chloride
  • aminopenicillanic acid