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Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents. The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics. Imatinib mesylate-loaded nanoliposomes were formulated by the two-step emulsification process using a high-speed homogenizer system and probe-type ultrasonicator. The Box-Behnken design was utilized to optimize the process parameters. The mean particle size of nanoliposomes was found to be 211 nm to 623.3 nm with a low value of polydispersity index (0.005 to 0.7). Zeta potential values varied from ‒27.6 mV to ‒9.2 mV in uncoated nanoliposomes to +27.5 mV in chitosan-coated nanoliposomes. The encapsulation efficiency in formulation NLP-H8 containing 200 mg of phosphatidylcholine, homogenization speed of 12000 rpm, and 7 min of sonication time was found to be 76.49% without the coating and 85.4% in 0.2% w/v chitosan-coated nanoliposomes. TEM image confirmed the spherical shape of nanoliposomes. In-vitro drug release study demonstrated that the optimized nanoliposomal formulations released 84.67% of the loaded drug after 24 h in 0.1 N HCl. The IC50 value of formulation NLP-H8 was found to be 7.98 μM. Nanoliposomal formulations were prepared successfully with suitable size, morphology, encapsulation efficiency, and drug release. The models developed in this study may be utilized further as a response surface for the various parameters of nanoliposomes.


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Optimization Studies on Imatinib Mesylate Loaded Nanoliposomes Using Box-Behnken Design

Show Author's information Mandeep Dahiya1#Rajendra Awasthi2#Gaurav Gupta3Sachin Kumar Singh4Monica Gulati4Niraj Kumar Jha5Saurabh Kumar Jha5Ankur Sharma6Parteek Prasher7Krishnan Anand8Dinesh Kumar Chellappan9Kamal Dua10Harish Dureja1( )
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India
Amity Institute of Pharmacy, Amity University Uttar Pradesh, Noida, 201313, India
School of Pharmaceutical Sciences, Suresh Gyan Vihar University, Jaipur, Rajasthan, India
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, Punjab, India
Department of Biotechnology, School of Engineering and Technology (SET), Sharda University, Uttar Pradesh, Noida, 201301, India
Department of Life Sciences, School of Basic Science and Research (SBSR), Sharda University, Greater Noida, 201310, India
Department of Chemistry, University of Petroleum & Energy Studies, Energy Acres, Dehradun, 248007, India
Department of Chemical Pathology, School of Pathology, Faculty of Health Sciences and Na-tional Health Laboratory Service, University of the Free State, Bloemfontein, South Africa
Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur, 57000, Malaysia
Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo NSW, 2007, Australia

#These authors have contributed equally to this work and share first authorship.

Abstract

Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents. The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics. Imatinib mesylate-loaded nanoliposomes were formulated by the two-step emulsification process using a high-speed homogenizer system and probe-type ultrasonicator. The Box-Behnken design was utilized to optimize the process parameters. The mean particle size of nanoliposomes was found to be 211 nm to 623.3 nm with a low value of polydispersity index (0.005 to 0.7). Zeta potential values varied from ‒27.6 mV to ‒9.2 mV in uncoated nanoliposomes to +27.5 mV in chitosan-coated nanoliposomes. The encapsulation efficiency in formulation NLP-H8 containing 200 mg of phosphatidylcholine, homogenization speed of 12000 rpm, and 7 min of sonication time was found to be 76.49% without the coating and 85.4% in 0.2% w/v chitosan-coated nanoliposomes. TEM image confirmed the spherical shape of nanoliposomes. In-vitro drug release study demonstrated that the optimized nanoliposomal formulations released 84.67% of the loaded drug after 24 h in 0.1 N HCl. The IC50 value of formulation NLP-H8 was found to be 7.98 μM. Nanoliposomal formulations were prepared successfully with suitable size, morphology, encapsulation efficiency, and drug release. The models developed in this study may be utilized further as a response surface for the various parameters of nanoliposomes.

Keywords: cytotoxicity, Box-Behnken design, Nanoliposome, Ultrasonication, Emulsification, Imatinib mesylate

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Publication history

Received: 17 September 2021
Accepted: 20 March 2022
Published: 22 April 2022
Issue date: March 2022

Copyright

© Mandeep Dahiya, Rajendra Awasthi, Gaurav Gupta, Sachin Kumar Singh, Monica Gulati, Niraj Kumar Jha, Saurabh Kumar Jha, Ankur Sharma, Parteek Prasher, Krishnan Anand, Dinesh Kumar Chellappan, Kamal Dua, and Harish Dureja.

Acknowledgements

Acknowledgements

This work was supported by the grant-in-aid to the Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India, under the plan of Major Research Project [F.No.-43-485/2014(SR)] by University Grants Commission, India.

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This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

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