Co-loading of isoniazid-grafted phthalocyanine-in-cyclodextrin and rifampicin in crude soybean lecithin liposomes: Formulation, spectroscopic and biological characterization

Christian Isalomboto Nkanga, Michael Roth, Roderick Bryan Walker, Xavier Siwe Noundou, Rui Werner MaçEdo Krause*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

An inclusion complex of isoniazid-grafted phthalocyanine with gamma-cyclodextrin (Complex) was co-encapsulated with rifampicin (RIF) in crude soybean lecithin liposomes using a heating method. The encapsulation efficiency (%EE) of the Complex-RIF co-loaded liposomes (Rif-Complex-Lips) was determined using UV-Vis spectrophotometry. Rif-Complex-Lips formulations were evaluated using dynamic light scattering, transmission electron microscopy (TEM), 1H-NMR, absorption and emission spectroscopy. Dialysis was used for drug release study in two different media, pH 6.4 and 7.4. HeLa cells were used to assess potential cytotoxicity, and the uptake by lung fibroblasts and epithelial cells was investigated using fluorescence microscopy. The particle size and Zeta potential of Rif-Complex-Lips were approximately 594 nm and -50 mV. Spectroscopic analyses demonstrated molecular distribution of the cargo within the lipid core, and encapsulation efficiency of 58% for Complex and 86% for RIF. TEM analysis unveiled the existence of spherical nanoparticles in our samples, indicating the presence of liposomes. Rif-Complex-Lips exhibited much higher release rates for both INH and RIF at pH 6.4 compared to those tested at pH 7.4. In addition, there was no cytotoxicity on HeLa cells, but remarkable Rif-Complex-Lips internalization by peripheral lung fibroblasts and epithelial cells. Hence, Rif-Complex-Lips are promising vehicles for intracellular delivery of antimicrobial drugs.

Original languageEnglish
Pages (from-to)14-28
Number of pages15
JournalJournal of Biomedical Nanotechnology
Volume16
Issue number1
DOIs
Publication statusPublished - 2020
Externally publishedYes

Keywords

  • Cyclodextrin
  • Isoniazid
  • Liposomes
  • Phthalocyanines
  • Rifampicin
  • Soybean Lecithin

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