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Analysis of Process and Formulation Variables on Chitosan based Losartan Potassium Nanoparticles: Preparation, Validation and in Vitro Release Kinetics

Author(s):

Manisha Singh*, Ramneek Kaur, Rashi Rajput, Sachin Kumar, Malvika Sharma, Aishwarya Sharma and Udita Srivastava  

Abstract:


Background - Although many potential therapeutic compounds have been discovered and have exhibited a promising recovery but their effective delivery in the human system always remained questionable with many pharmacological constraints in delivering them. Nanomedicine concept has shown assuring potential to overcome from the drug delivery complications in the present treatment methods. Losartan potassium (LP) is indicated in the management of hypertension, owing to its moderate bioavailability (32%) and a number of side effects due to the oral dosage forms of LP, a nanoparticulate dosage delivery would be beneficial.

Objective - The present study is focused to develop a nanoparticle system of Losartan potassium, an Angiotensin II receptor antagonist and a well-known promising antihypertensive drug, to conquer its limitation of bioavailability and reduced along with potential adverse effects.

Method -They were developed by ionic gelation method using chitosan (CH) and Tripolyphosphate (TPP) for cross linkage in various optimising ratios. After the successful optimisation and synthesis of LP-NP’s, it was further characterized by Particle size analysis (PSA), polydispersity index (PDI), Zeta potential (ZP), TEM analysis with in vitro cyto toxicity and permeability evaluation.

Results - The results showed the average size of 123.5 ± 1.23nm with polydispersibility score of 0.257 ± 0.079 and charge of -2.74 mv respectively. Further, Transmission electron microscopy (TEM) images showed size range nearly in conformity with DLS findings with spherical and smooth morphology. In vitro drug release kinetics estimation showed sustained release routine of drug. In addition, the cytotoxicity studies done on Jurkat cell line displayed lesser cytotoxicity of LP-NPs (99.3 ± 2.28% and 98.17 ± 1.86%) in comparison to the LP (95.3 ± 2.1% and 91.7 ± 1.07%) at different time periods (12 hours and 24 hours).

Conclusion - The aforementioned results confirm the effective fabrication of LP-NPs and indicate that it may further be used on higher model systems to investigate the above parameters and its enhanced effectiveness in hypertension.

Keywords:

Antihypertensive , Chitosan , Particle size analysis , drug release kinetics , Transmission electron microscopy , polymeric nanoparticle

Affiliation:

Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307, Department of Biotechnology, Jaypee Institute of Information Technology, Noida 201307



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