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Current Computer-Aided Drug Design

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ISSN (Print): 1573-4099
ISSN (Online): 1875-6697

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Research Article

Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (211)) Orthogonal Array Design

Author(s): Ganesan Poovi and Narayanasamy Damodharan*

Volume 17, Issue 1, 2021

Published on: 20 March, 2020

Page: [144 - 159] Pages: 16

DOI: 10.2174/1573409916666200320162948

Price: $65

Abstract

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach.

Methods: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly watersoluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (211)) orthogonal array design by applying computer optimization technique.

Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggest that the cause of cell death is primarily from the effect of TMX present in NLCs.

Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

Keywords: Solid lipid nanoparticle, nanostructured lipid carrier, Taguchi (L12 (211)), orthogonal array design, tamoxifen, cytotoxicity study.

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