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
DOI: https://doi.org/10.35814/jifi.v17i2.568

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.

References

1. World Health Organization. Global tuberculosis report 2016. 2016

2. Kang PB, Azad AK, Torrelles JB, Kaufman TM, Beharka A, Tibesar E & Schlesinger LS. The human macrophage mannose receptor directs Mycobacterium tuberculosis lipoarabinomannan-mediated phagosome biogenesis. Journal of Experimental Medicine. 2005. 202(7): 987-999.

3. Torrelles JB, & Schlesinger LS. Diversity in Mycobacterium tuberculosis mannosylated cell wall determinants impacts adaptation to the host. Tuberculosis. 2010. 90(2): 84-93

4. World Health Organization. Global tuberculosis report 2015. 2015.

5. Becker C. Preparation of biowaiver recommendations for antituberculosis drugs [dissertation]. Senckenberg: Universitätsbibliothek Johann Christian. 2009.

6. Pardeike J, Hommoss A, & Müller RH. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. International journal of pharmaceutics. 2009. 366(1): 170-184

7. Naseri N, Valizadeh H, & Zakeri-Milani P. Solid lipid nanoparticles and nanostructured lipid carriers: structure, preparation and application. Advanced pharmaceutical bulletin. 2015. 5(3): 305.

8. Yang X, Patel S, Sheng Y, Pal D., & Mitra AK. Statistical design for formulation optimization of hydrocortisone butyrate-loaded PLGA nanoparticles. AAPS PharmSciTech. 2014. 15(3): 569-587.

9. Chaubey P, & Mishra B. Mannose-conjugated chitosan nanoparticles loaded with rifampicin for the treatment of visceral leishmaniasis. Carbohydrate polymers. 2014. 101: 1101-1108.

10. Gribble GW & Ferguson DC. Reactions of sodium borohydride in acidic media. Selective reduction of aldehydes with sodium triacetoxyborohydride. Journal of the Chemical Society, Chemical Communications. 1975. (13): 535-536.

11. Nkuzinna OC, Menkiti MC, Onukwuli OD, Mbah GO, Okolo BI, & Egbujor MC. Application of Factorial Design of Experiment for Optimization of Inhibition Effect of Acid Extract of Gnetum africana on Copper Corrosion. Natural Resources. 2014. 5(07): 299.

12. Trinh TK & Kang LS. Application of response surface method as an experimental design to optimize coagulation tests. Environmental Engineering Research. 2010. 15(2): 63-70.

13. Montgomery DC. Design and Analysis of Experiments. 4th Wiley. New York; 1997. p. 704.

14. McCarron PA, Woolfson AD, & Keating SM. Response surface methodology as a predictive tool for determining the effects of preparation conditions on the physicochemical properties of poly (isobutylcyanoacrylate) nanoparticles. International journal of pharmaceutics. 1999. 193(1): 37-47.

15. Hirota K & Terada H. Endocytosis of particle formulations by macrophages and its application to clinical treatment. In Molecular Regulation of Endocytosis. InTech. 2012.

16. Pinheiro M, Ribeiro R, Vieira A, Andrade F, & Reis S. Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis. Drug design, development and therapy. 2016. 10:2467.
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: 26 apr. 2024. doi: https://doi.org/10.35814/jifi.v17i2.568.
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Vol 17 No 2 (2019): JIFI
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