DEVELOPMENT OF NOVEL MICROSTRUCTURED LIPID CARRIERS FOR DISSOLUTION RATE ENHANCEMENT OF ALBENDAZOLE

Authors

  • CASTRO ALPIZAR J. A. Faculty of Pharmacy, University of Costa Rica, San Jose, Costa Rica
  • PACHECO MOLINA J. Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Costa Rica, San Jose, Costa Rica
  • VARGAS MONGE R. Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Costa Rica, San Jose, Costa Rica
  • MADRIGAL REDONDO G. Laboratory of Biopharmacy and Pharmacokinetics (LABIOFAR), Institute of Pharmaceutical Research (INIFAR), Faculty of Pharmacy, University of Costa Rica, San José, Costa Rica https://orcid.org/0000-0002-9856-4044

DOI:

https://doi.org/10.22159/ijap.2020v12i6.34782

Keywords:

Albendazole, Microstructured lipid carrier, Dissolution, Crystalline structure

Abstract

Objective: This study aimed to develop a microstructured lipid carrier that improves the rate of dissolution of the active pharmaceutical ingredient (API) Albendazole.

Methods: A solvent diffusion method was used for the development of microstructured lipid carriers. The developed carriers were characterized by optical microscopy, infrared spectroscopy, differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and dissolution testing.

Results: The morphology of the carriers was irregular, and their size tends to decrease with the addition of modifiers. Furthermore, the diffractograms and the thermograms indicated a loss of crystallinity. The thermograms and infrared spectra showed that there are not chemical incompatibilities between the API and the excipients. When the lipid carrier particles were modified with Aerosil® 200 (specifically when using this excipient at a level of 6% w/w), dissolution was increased up to 85.96±1.17 % of the drug content as per USP test for Albendazole tablets in comparison with 36.13±0.52 % for a lipid carrier formulation without modifiers.

Conclusion: It was demonstrated that it is possible to develop a modified lipid carrier that improves the dissolution rate of an API with a low solubility, which was related to the amorphization of the API crystalline structure.

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References

Attama A, Igbonekwu C. In vitro properties of surface-modified solid lipid microspheres containing an antimalarial drug: halofantrine. Asian Pac J Trop Med 2011;4:253-8.

Bhoyar PK, Morani DO, Biyani DM, Umekar MJ, Mahure JG, Amgaonkar YM. Encapsulation of naproxen in lipid-based matrix microspheres: characterization and release kinetics. J Young Pharm 2011;3:105–11.

Kalepu S, Manthina M, Padavala V. Oral lipid-based drug delivery systems–an overview. Acta Pharm Sin B 2013;3:361–72.

Jannin V, Musakhanian J, Marchaud D. Approaches for the development of solid and semi-solid lipid-based formulations. Adv Drug Delivery Rev 2008;60:734–46.

Mayet L, Jung Cook H, Mendoza O, Rodriguez J. Estudio comparativo de perfiles de disolución de medicamentos del mercado nacional. Rev Mex Cienc Farm 2008;39:4–8.

Hu FQ, Jiang SP, Du YZ, Yuan H, Ye YQ, Zeng S. Preparation and characteristics of monostearin nanostructured lipid carriers. Int J Pharm 2006;314:83–9.

United States Pharmacopeial Convention. USP 40/NF35. Rockville (MD); 2017.

Albertini B, Passerini N, Gonzalez Rodriguez ML, Perissutti B, Rodriguez L. Effect of Aerosil® on the properties of lipid controlled release microparticles. J Controlled Release 2004;100:233–46.

Rowe R, Sheskey P, Quinn M. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press and American Pharmacists Association; 2009.

Susarla R, Afolabi A, Patel D, Bilgili E, Dave RN. Novel use of superdisintegrants as viscosity enhancing agents in biocompatible polymer films containing griseofulvin nanoparticles. Powder Technol 2015;285:25–33.

Padhye SG, Nagarsenker MS. Simvastatin solid lipid nanoparticles for oral delivery: formulation development and in vivo evaluation. Indian J Pharm Sci 2013;75:591–8.

Albertini B, Passerini N, Gonzalez Rodriguez ML, Perissutti B, Rodriguez L. Effect of Aerosil® on the properties of lipid controlled release microparticles. J Controlled Release 2004;100:233–46.

Alanazi FK, El-Badry M, Ahmed MO, Alsarra IA. Improvement of albendazole dissolution by preparing microparticles using spray-drying technique. Sci Pharm 2007;75:63–79.

Gonzalez N, Castro S, Sanchez B, Allemandi D, Palma S. Albendazole solid dispersions: influence of dissolution medium composition on in vitro drug release. Dissolution Technol 2014;21:42-7.

Yurkanis P. Espectrometria de masas, espectroscopia infrarroja y espectroscopia ultravioleta/visible. In: Cruz L. editor. Quimica Organica. 5th ed. México: Pearson Educacion; 2008. p. 512–55.

Pavia DL, Lampman GM, Kriz GS, Vyvyan JR. Introduction to spectroscopy. 4th ed. United States of America: Cengage Learning; 2008.

Hu FQ, Jiang SP, Du YZ, Yuan H, Ye YQ, Zeng S. Preparation and characterization of stearic acid nanostructured lipid carriers by solvent diffusion method in an aqueous system. Colloids Surfaces B 2005;45:167–73.

Herrmann S, Winter G, Mohl S, Siepmann F, Siepmann J. Mechanisms controlling protein release from lipidic implants: effects of PEG addition. J Controlled Release 2007;118:161–8.

Mani N, Suh HR, Jun HW. Microencapsulation of a hydrophilic drug into a hydrophobic matrix using a salting‐out procedure. II. Effects of adsorbents on microsphere properties. Drug Dev Ind Pharm 2004;30:83–93.

Castro Ruiz JM. Diseno de un sistema bioadhesivo de clorhexidina empleando pullulan como matriz para uso en mucosa oral. Colombia: Universidad Nacional de Colombia; 2014.

Hernandez Torres JE, Melgoza Contreras LM. Principales superdisgregantes sintéticos, mecanismos y factores que influyen en su actividad. Rev Colomb Ciencias Quimico Farmaceuticas 2014;43:234–47.

Mohanachandran PS, Sindhumol PG, Kiran TS. Superdisintegrants: an overview. Int J Pharm Sci Rev Res 2011;6:105–9.

Shihora H, Panda S. Superdisintegrants, utility in dosage forms: a quick review. J Pharm Sci Biosci Res 2011;1:148–53.

Yu LX, Furness MS, Raw A, Woodland Outlaw KP, Nashed NE, Ramos E, et al. Scientific considerations of pharmaceutical solid polymorphism in abbreviated new drug applications. Pharm Res 2003;20:531–6.

Published

07-11-2020

How to Cite

J. A., C. A., J., P. M., R., V. M., & G., M. R. (2020). DEVELOPMENT OF NOVEL MICROSTRUCTURED LIPID CARRIERS FOR DISSOLUTION RATE ENHANCEMENT OF ALBENDAZOLE. International Journal of Applied Pharmaceutics, 12(6), 173–178. https://doi.org/10.22159/ijap.2020v12i6.34782

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Original Article(s)