Preliminary investigation on coconut oil-based self-emulsifying formulation for the delivery of Metronidazole

Contenu principal de l'article

Zwanden Sule Yahaya
Paul Osereme Yahaya
Boma Blessing Mohammed

Résumé

The aim of this study was to perform a preliminary evaluation of the suitability of natural coconut oil in the formulation of a self-emulsifying drug delivery system (SEDDS) for metronidazole. Different SEDDS mixtures comprising of different proportions of coconut oil, cremophor EL (surfactant) and PEG-400 (co-surfactant) of varying mass ratios were prepared. A pseudo-ternary phase diagram was generated from the phase titration studies between water and the different SEDDS mixtures at room temperature which facilitated the selection of a stable SEDDS. The stable SEDDS was then loaded with the metronidazole powder and characterized with respect to globule size, polydispersity index (PDI), emulsification time, stability, post-dilution drug precipitation and in vitro release studies. It was also converted to powder by adsorption on cabosil® at 1:2 (w/w) ratio and evaluated. The formulation consisted of 20 % coconut oil, 60 % cremophor EL, 20 % PEG-400 and demonstrated stability against phase separation. Also, it exhibited an emulsification time of 15.0 s, a mean globule size of 18.95 nm, a polydispersity index (PDI) of 0.238 and released over 90 % of the drug within 30 min. The powdered formulation demonstrated acceptable flow properties, contains particles that are irregular and free from rough edges. At 20 min, the percentage of drug released from the metronidazole-SEDDS powder during the in vitro release studies was 37 % lower than the liquid metronidazole-SEDDS, indicating that solidification of lipid-based formulations through adsorption onto a carrier may limit drug release. The experimental results from this preliminary investigation were satisfactory, indicating that natural coconut oil can serve as a promising alternative colloidal drug carrier in the field of novel drug delivery systems.

Téléchargements

Les données relatives au téléchargement ne sont pas encore disponibles.

Renseignements sur l'article

Comment citer
Yahaya, Z. S. ., Yahaya, P. O. ., & Mohammed, B. B. . (2020). Preliminary investigation on coconut oil-based self-emulsifying formulation for the delivery of Metronidazole. Nigerian Journal of Pharmaceutical and Applied Science Research, 9(1), 18–24. Consulté à l’adresse https://nijophasr.net/index.php/nijophasr/article/view/326
Rubrique
Articles
Bibliographies de l'auteur-e

Zwanden Sule Yahaya

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna - Nigeria

Paul Osereme Yahaya

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna - Nigeria

Boma Blessing Mohammed

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna - Nigeria

Références

Barakat, N.S. (2010). Self-Emulsifying System for Improving Drug Dissolution and Bioavailability: In Vitro/In Vivo Evaluation. Drug Development Research 71: 149 -158

Dixit, A.R., Rajput, S.J. and Patel, S.G. (2010). Preparation and Bioavailability Assessment of SMEDDS Containing Valsartan. American Association of Pharmaceutical Scientist, 11 (1): 314 - 321.

Gershanik, T. and Benita, S. (2000). Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. European Journal of Pharmaceutics and Biopharmaceutics, 50: 179 - 88.

Gumaste, S. G., Dalrymple, D. M., Serajuddin A. T. M. (2013). Development of Solid SEDDS, V: Compaction and Drug Release Properties of Tablets Prepared by Adsorbing Lipid-Based Formulations onto Neusilin® US2. Pharmaceutical Research, doi:10.1007/s11095-013-1106-4.

Hani U., Bhat R. S., and Shivakumar, H. G. (2011). Formulation Design and Evaluation of Metronidazole Microspheres in a Bioadhesive Gel for Local Therapy of Vaginal Candidiasis. Latin American Journal of Pharmacy, 30 (1): 161-167.

Kim, D.S., Cho, J.H. Park, J.H., Kim, J.S., Song, E.S., Kwon, J., Giri, B.R., Jin, S.G., Kim, K.S., Choi, H.G. and Kim, D.W. (2019). Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate. International Journal of Nanomedicine, 14: 4949 - 4960.

Porter, C.J.H. (2013). Strategies to address low solubility in discovery and development. Pharmacology Review, 65:315 - 499.

Pouton, C. W. (2006). Formulation of water-soluble drugs for oral administration:physicochemical and physiological issues and the lipid formulation classification system. European Journal of Pharmaceutical Sciences, 29: 278-287.

Pouton, C.W., and Porter, CJ.H. (2008). Formulation of lipid-based delivery systems for oral administration: Materials, methods and strategies. Advanced Drug Delivery Reviews, 60: 625 - 637.

Shah, R.B., Tawakkul, M.A., Khan, M.A. (2008). Comparative evaluation of flow for pharmaceutical powders and granules. AAPS PharmSciTech, 9: 250 - 258.

Speybroeck, M. V., Williams, H. D., Nguyen, T., Anby, M. U., Porter, C. J. H., and Augustijns, P. (2012). Incomplete Desorption of Liquid Excipients Reduces the in Vitro and in Vivo Performance of Self-Emulsifying Drug Delivery Systems Solidified by Adsorption onto an Inorganic Mesoporous Carrier. Molecular Pharmaceutics, 9: 2750 – 2760

Tripathi, C. B., Kaur S., B., R., Bandopadhyay, G., S. and Singh, B., S. (2016). Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential. Drug Delivery, 23(9): 3209 - 3223.

United States Pharmacopoeial Convention (1995). United States Pharmacopoeia, 23rd edition, Maryland.

Wu W., Wang, Y., and Que, L. (2006). Enhanced bioavailability of silymarin by self-microemulsifying drug delivery system. European Journal of Pharmaceutics and Biopharmaceutics, 63: 288 – 294.

Yahaya, Z.S., Oyi, A.R., Allagh, T.S., Abdulsamad, A. and Dagogot, N.C. (2019). Piroxicam-loaded self-emulsifying drug delivery system. The Nigerian Journal of Pharmacy, 53(1): 34 - 47.

Zhang, P., Liu, Y., Feng, N. and Xu, J. (2008). Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. International Journal of Pharmaceutics, 355: 269 - 276.