Formula Optimization of NLC with D-Mannose Targeting for Rifampicin Delivery System

  • Tri Suciati School of Pharmacy, Bandung Institut of Technology
  • Nurani Istiqomah School of Pharmacy, Bandung Institut of Technology
  • Benny Permana School of Pharmacy, Bandung Institut of Technology
  • Elin Julianti
  • Marlia Singgih Wibowo
  • Titah Yudistira Industrial Enggineering, Bandung Institute of Technology
  • Yani Triyani Faculty of Medicine, Bandung Islamic University

Abstract

Limited accumulation of anti-tuberculosis drugs in macrophages become a barrier to the success of latent tuberculosis therapy. The purpose of this study is to develop a D-mannose modified nanoparticle formula as a targeting agent to the mannose receptors to increase the internalization of rifampicin into macrophages. D-mannose was conjugated with chitosan using an amine reducing agent. Chitosan-D-mannose conjugate was characterized using FTIR. Subsequently, the conjugate was adsorbed onto the nanostructured lipid carrier (NLC) electrostatically. The NLC formula consisted of an ethyl acetate solution of solid-liquid lipid blend and rifampicin and an aqueous solution of chitosan-D-mannose conjugate, which were emulsified using polysorbate 80. Solidification of the NLC-chitosan-mannose nanoparticles was carried out by ionotropic gelation and solvent evaporation. The nanoparticle formula was optimized using Box-Behnken design. The formation of chitosan-D-mannose conjugate was shown by the change of the amide band wave number and the Schiff base formation of the FTIR spectra. The optimum formula of nanoparticles had a diameter of 766.1 ± 57.56 nm with a polydispersity index of 0.32 ± 0.02, encapsulation efficiency of 91.54 ± 0.18% and drug loading of 36.62 ± 0.07%. Rifampicin was released from the nanoparticles at pH 5.2 or 7.4 with a similar rate. This D-mannose modified NLC formula has the potential to be further developed as an intracellular antibiotic targeting to macrophages.

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Published
2019-10-29
How to Cite
SUCIATI, Tri et al. Formula Optimization of NLC with D-Mannose Targeting for Rifampicin Delivery System. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 17, n. 2, p. 189-198, oct. 2019. ISSN 2614-6495. Available at: <http://jifi.farmasi.univpancasila.ac.id/index.php/jifi/article/view/568>. Date accessed: 18 nov. 2019. doi: https://doi.org/10.35814/jifi.v17i2.568.
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Articles