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Abstract

PLGA Nanoparticles for Delivery of Losartan Potassium through Intranasal Route: Development and Characterization

Cardiovascular disease caused 2.3 million deaths in India in the year 1990, and this is projected to double by the year 2020. Losartan Potassium and ACE receptor blocker is a drug of choice. The objective of the work was to develop a delivery system that prevents the high first pass metabolism of the antihypertensive drug with sustained release by reducing dosing frequency to effective management of Hypertension.The Two level-Three factor (23) optimization model was used to determine the optimized formulation. The independent variables selected for optimization of formulation was Drug: Polymer ratio, Surfactant concentration and Stirring speed. The dependent variables are Particle size and Entrapment efficiency. The formulation was optimized on the basis of dependent variables. The Entrapment Efficiency of optimized formulation was found to be 87 %, Zeta potential of that formulation was -16.6 mV and Particle size was found to be 295.3 nm. The Scanning Electron Microscopy (SEM) image does not exactly shows the Nanoparticle size, but it can be concluded from the image of that particles are of 250 nm. The In-vitro release study was done using Dialysis bag, it releases 84% drug in 48 hours. The release pattern follows Korsemeyer- Peppas Model. The In-vivo fluorescent study was done and presence of green colour confirms that the Nanoparticles of optimized formulation was able to penetrate the nasal epithelium.No major changes in the content of drug was observed at the end of 3 months during Stability study. So data of stability studies revealed that formulation will be stable for longer period of time


Author(s): Ajay Verma*, Sanjay Ratnawat, Arun K. Gupta, Sanjay Jain

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