Development and Characterization of Gefitinib Loaded Polymeric Nanoparticles by Ionic Gelation Method
Minakshi Gupta1, Rakesh Kumar Marwaha1, Harish Dureja1
1Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak -124001, Haryana, India.
Background:
There is a rapidly growing interest in the development of nanoparticle drug delivery mainly for anticancer drugs as it promises to solve several problems associated with anticancer drugs such as poor water solubility, low therapeutic index, nonspecific distribution and higher systemic toxicity, etc.
Objective:
The objective of the study was to investigate the effect of various critical variables like, concentration of chitosan, concentration of sodium tripolyphosphate (STPP) and volume of STPP on various characteristics of gefitinib loaded nanoparticles.
Methods:
Thirteen formulations of the polymeric nanoparticles were prepared using various concentrations of chitosan (0.1-1% w/v), STPP (0.2-1.5% w/v) and different volumes of STPP (8-20 ml) by ionic gelation method. Mannitol (5% w/v) was used as cryoprotectant. The prepared nanoparticle formulations were characterized for various parameters like particle size, zeta potential, process yield, encapsulation efficiency, drug content, and in vitro drug release.
Results:
The nanoparticle formulation NF-1 containing 0.1% w/v of chitosan and 10 ml volume of 0.2% w/v STPP showed best results in terms of particle size (123.8nm), polydispersity index (0.247), zeta potential (+30.4 mV), process yield (68.09%), drug content (74.32%), encapsulation efficiency (70.52%) and released (56.2 %) drug over a period of 24 h. The in vitro drug release analysis showed sustained release of gefitinib from nanoparticles and followed Korsmeyer-Peppas model.
Conclusion:
The nanoparticle formulation with desired characteristics can be prepared at low concentration of chitosan and STPP along with low volume of STPP. The formulated nanoparticles may prove to be the best option for the treatment of cancer.
Insights
Researchers developed optimized gefitinib-loaded nanoparticles using chitosan and sodium tripolyphosphate (STPP). These nanoparticles offer sustained drug release, showing promise for improved anticancer therapy.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Materials Science
Background:
- Nanoparticle drug delivery is crucial for improving anticancer agents.
- Challenges include poor solubility, low therapeutic index, and systemic toxicity.
- Nanoparticles offer solutions to these limitations.
Purpose of the Study:
- To optimize gefitinib-loaded nanoparticles.
- Investigate the impact of chitosan and sodium tripolyphosphate (STPP) concentrations and volume.
- Characterize nanoparticle properties for effective drug delivery.
Main Methods:
- Ionic gelation method used to prepare thirteen nanoparticle formulations.
- Varied concentrations of chitosan (0.1-1% w/v) and STPP (0.2-1.5% w/v).
- Evaluated particle size, zeta potential, yield, encapsulation, drug content, and in vitro release.
Main Results:
- Formulation NF-1 (0.1% chitosan, 0.2% STPP, 10 ml STPP) showed optimal characteristics.
- Achieved particle size of 123.8nm, zeta potential of +30.4 mV, and 70.52% encapsulation efficiency.
- Demonstrated sustained gefitinib release over 24 hours, following the Korsmeyer-Peppas model.
Conclusions:
- Optimized gefitinib nanoparticles can be prepared using low concentrations of chitosan and STPP.
- These nanoparticles represent a promising approach for cancer treatment.
- Sustained drug release enhances therapeutic potential.
