IMPLEMENTATION OF FACTORIAL DESIGN TO OPTIMIZE THE FORMULATION METHOD OF EZETIMIBE POLYMERIC NANOPARTICLE BY HOMOGENIZATION CUM ULTRA-SONICATION METHOD

BALA NAGAMANI D.; BHASKAR REDDY K.; SESHA MAHESWARAMMA K.; BRITO RAJ S.

doi:10.22159/ijap.2022v14i2.43783

Authors

BALA NAGAMANI D. Jawaharlal Nehru Technological University Anantapur, Anantapur, Andhra Pradesh, India https://orcid.org/0000-0002-4579-5420
BHASKAR REDDY K. Department of Pharmaceutics, Sri Venkateswara College of Pharmacy, RVS Nagar, Chittoor-517127, Andhra Pradesh, India
SESHA MAHESWARAMMA K. Department of Chemistry, JNTUA College of Engineering (Autonomous), Pulivendula 516390, Andhra Pradesh, India
BRITO RAJ S. Chettinad School of Pharmaceutical Sciences, Chettinad Academy of Research and Education, Chettinad Health city, Kelambakkam 603103, Chengalpattu District, Tamilnadu, India https://orcid.org/0000-0001-5987-3031

DOI:

https://doi.org/10.22159/ijap.2022v14i2.43783

Keywords:

Optimization, Ezetimibe, Polymeric Nanoparticle, 23 factorial design, Homogenization, Ultrasonication

Abstract

Objective: The objective of this study is to use a 2³ factorial design to optimize the formulation factors of Ezetimibe polymeric nanoparticle.

Methods: By varying formulation variables such as polymer concentration (hydroxyl propyl methyl cellulose composition) and process variables such as homogenization time (min) and ultra-sonication time, the formulation of polymeric nanoparticles was designed using a 2³ factorial design and prepared using the homogenization cum ultra-sonication method (min). Particle size (nm), zeta potential (mV), polydispersity index, entrapment efficiency (%), drug content, in vitro drug release, in vitro release kinetic studies, and stability studies were used to analyse and optimize polymeric nanoparticles according to ICH criteria.

Results: R7 formulation showed predicted and desired less particle size 87.0±3.64 nm; maximum zeta potential-33.4±2.32 mV; desired polydispersity index 0.488±0.20; maximum entrapment efficiency of 96.45±2.42 % and controlled dissolution release pattern of about 90.42±3.56% in 24h.

Conclusion: The polymeric nanoparticle was formulated and optimized by the parameters like Particle Size (PS in nm), Polydispersity Index (PI), Zeta potential (Zp in mV), % Entrapment Efficiency and in vitro drug release for 24 h were evaluated. These parameters showed significant changes while formulating polymeric nanoparticles along with various formulation and process variables. From the release pattern data it was observed that PNs show a significant improvement of dissolution character of Ezetamibe. According to the findings, PNs have a controlled drug release pattern and can be used as a suitable drug delivery carrier for low solubility and poorly bioavailable drugs like Ezetamibe to improve its dissolution.

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