USING A SIMPLEX CENTROID DESIGN AND FATTY ACIDS TO OPTIMIZE FLUCONAZOLE-LOADED SOLID LIPID NANOPARTICLES (SLNs)

PAKORN KRAISIT; NAMON HIRUN; PREMJIT LIMPAMANOCH; SONTAYA LIMMATVAPIRAT

doi:10.22159/ijap.2021v13i6.42789

Authors

PAKORN KRAISIT Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani, 12120, Thailand
NAMON HIRUN Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani, 12120, Thailand
PREMJIT LIMPAMANOCH Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani, 12120, Thailand
SONTAYA LIMMATVAPIRAT Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand

DOI:

https://doi.org/10.22159/ijap.2021v13i6.42789

Keywords:

Simplex centroid design, Solid lipid nanoparticles (SLNs), Fluconazole, Fatty acids, Experimental design

Abstract

Objective: This study aimed to prepare fluconazole (FZ)-loaded solid lipid nanoparticles (SLNs) using a simplex centroid design and fatty acids to optimize the SLNs to get small-sized nanoparticles with a narrow distribution.

Methods: Hot emulsification was used to prepare the FZ-loaded SLNs. Stearic acid (Sa) (X₁), palmitic acid (Pa) (X₂), and myristic acid (Ma) (X₃) were the solid lipids. The effect of various types and amounts of fatty acids on the particle size, polydispersity index, zeta potential, and pH of the SLNs was studied using the simplex centroid design.

Results: The particle size of all formulations ranged between 16.49 nm and 56.65 nm, and the polydispersity index (PDI) ranged between 0.258 and 0.676, indicating a relatively narrow size distribution. The zeta potential ranged from–7.47 to–12.2 mV. The pH was around 4.63–4.77, indicating that the SLN system was a weak acid. Design-Expert^® software was used to design the responses of all model formulations and to select the optimized formulation. The optimal formulation comprised 0.190 g Sa, 0.048 g Pa, and 0.002 g Ma. The experimental values of the particle size and PDI of the optimal formulation did not differ significantly from the predicted values and lay within a 95% confidence interval (CI).

Conclusion: Therefore, the simplex centroid design using fatty acids could efficiently formulate and optimize FZ-loaded SLNs.

Downloads

Download data is not yet available.

References

Kittiwisut S, Kraisit P. Physicochemical characterization of propranolol-loaded chitosan nanoparticles for a buccal drug delivery system. Int J App Pharm. 2020;12:243-7. doi: 10.22159/ijap.2020v12i4.38009.

Kraisit P, Limmatvapirat S, Nunthanid J, Sriamornsak P, Luangtana-anan M. Nanoparticle formation by using shellac and chitosan for a protein delivery system. Pharm Dev Technol. 2013;18(3):686-93. doi: 10.3109/10837450.2012.685657, PMID 22568768.

Kraisit P, Limmatvapirat S, Luangtana-Anan M, Sriamornsak P. Buccal administration of mucoadhesive blend films saturated with propranolol loaded nanoparticles. Asian J Pharm Sci. 2018;13(1):34-43. doi: 10.1016/j.ajps.2017.07.006, PMID 32104376.

Kraisit P, Hirun N, Mahadlek J, Limmatvapirat S. Fluconazole-loaded solid lipid nanoparticles (SLNs) as a potential carrier for buccal drug delivery of oral candidiasis treatment using the Box-Behnken design. J Drug Delivery Sci Technol. 2021;63. PMID 102437.

Lin CH, Chen CH, Lin ZC, Fang JY. Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers. J Food Drug Anal. 2017;25(2):219-34. doi: 10.1016/j.jfda.2017.02.001, PMID 28911663.

Xie S, Zhu L, Dong Z, Wang X, Wang Y, Li X, Zhou W. Preparation, characterization and pharmacokinetics of enrofloxacin-loaded solid lipid nanoparticles: influences of fatty acids. Colloids Surf B Biointerfaces. 2011;83(2):382-7. doi: 10.1016/j.colsurfb.2010.12.014, PMID 21215599.

Kraisit P. Impact of hydroxypropyl methylcellulose (HPMC) type and concentration on the swelling and release properties of propranolol hydrochloride matrix tablets usning a simplex centroid design. Int J App Pharm. 2019;11:143-51. doi: 10.22159/ijap.2019v11i2.31127.

Kraisit P, Limmatvapirat S, Nunthanid J, Sriamornsak P, Luangtana Anan M. Preparation and characterization of hydroxypropyl methylcellulose/polycarbophil mucoadhesive blend films using a mixture design approach. Chem Pharm Bull (Tokyo). 2017;65(3):284-94. doi: 10.1248/cpb.c16-00849, PMID 27980251.

Duangjit S, Kraisit P. Optimization of orodispersible and conventional tablets using simplex lattice design: the relationship among excipients and banana extract. Carbohydr Polym. 2018;193:89-98. doi: 10.1016/j.carbpol.2018.03.087, PMID 29773401.

Duangjit S, Kraisit P, Luangtana Anan M. An investigation of propranolol-loaded chitosan nanoparticles for transmucosal delivery: physical characterization. Thai J Pharm Sci. 2016;40:25-8.

Kraisit P, Sarisuta N. Development of triamcinolone acetonide-loaded nanostructured lipid carriers (NLCs) for buccal drug delivery using the box-behnken design. Molecules. 2018;23(4):E982. doi: 10.3390/molecules23040982, PMID 29690622.