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Microfluidics nanoprecipitation of telmisartan nanoparticles: effect of process and formulation parameters

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Abstract

A continuous microfluidic nanoprecipitation process has been investigated to prepare nanosized particles of a poorly water-soluble drug telmisartan (TEL), thereby enhancing its solubility and bioavailability. The present work aims to overcome agglomeration of drug particles by controlling the surface forces between the particles using various polymers like Polyvinylpyrrolidone K-30 (PVP K-30), Polyvinylpyrrolidone K-90 (PVP K-90), Poloxamer 188, Poloxamer 407, and hydroxypropyl methylcellulose (HPMC). The effect of process parameters such as solvent-to-antisolvent ratio, polymer-to-drug ratio, microchannel length, and solvent flow rate on drug particle size and polydispersity index (PDI) has been studied. The drug–polymer interaction investigated through X-ray diffraction (XRD) and Fourier transform infrared (FTIR) analysis revealed a significant reduction in peak intensity for Poloxamer 407 with no drug–polymer interaction. Also, the surface morphology of recrystallised TEL nanoparticles examined using field emission scanning electron microscopy (FESEM) showed clear and nearly uniform shaped particles. Poloxamer 407-based formulation of TEL exhibited minimum drug agglomeration with least particle size 369 nm and PDI value 0.049. The minimum particle size was achieved at solvent-to-antisolvent ratio 1:2, 1:1 polymer-to-drug ratio, microchannel length of 60 cm, and solvent flow rate of 30 mL/h. Thus, the microfluidic technique resulted in the production of TEL nanoparticles with narrow size distribution and useful morphological characteristics.

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Abbreviations

APIs:

Active pharmaceutical ingredients

BCS:

Biopharmaceutical Classification System

FESEM:

Field emission scanning electron microscopy

FTIR:

Fourier transform infrared

HPMC:

Hydroxypropyl methylcellulose

PDI:

Polydispersity index

PEO:

Polyethylene oxide

PPO:

Polypropylene oxide

PVP K-30:

Polyvinylpyrrolidone K-30

PVP K-90:

Polyvinylpyrrolidone K-90

TEL:

Telmisartan

XRD:

X-ray diffraction

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Acknowledgements

The corresponding author would like to acknowledge Science and Engineering Research Board, Department of Science and Technology, Government of India (sanctioned no. EEQ/2018/001001, dated 23-05-2019) for financial support.

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  1. Department of Chemical Engineering, S. V. National Institute of Technology, Surat, Gujarat, 395007, India

    Preena Shrimal, Girirajsinh Jadeja & Sanjaykumar Patel

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  1. Preena Shrimal
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  2. Girirajsinh Jadeja
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  3. Sanjaykumar Patel
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Correspondence to Sanjaykumar Patel.

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Shrimal, P., Jadeja, G. & Patel, S. Microfluidics nanoprecipitation of telmisartan nanoparticles: effect of process and formulation parameters. Chem. Pap. 75, 205–214 (2021). https://doi.org/10.1007/s11696-020-01289-w

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  • DOI: https://doi.org/10.1007/s11696-020-01289-w

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