Gupta Minakshi, Marwaha Rakesh Kumar, Dureja Harish
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak -124001, Haryana, India.
Pharm Nanotechnol. 2017;5(4):301-309. doi: 10.2174/2211738505666171004124109.
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.
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.
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.
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.
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.
纳米颗粒药物递送的发展引发了人们迅速增长的兴趣，主要针对抗癌药物，因为它有望解决与抗癌药物相关的几个问题，如水溶性差、治疗指数低、非特异性分布和全身毒性高等。
本研究的目的是研究壳聚糖浓度、三聚磷酸钠（STPP）浓度和STPP体积等各种关键变量对吉非替尼负载纳米颗粒各种特性的影响。
采用离子凝胶法，使用不同浓度的壳聚糖（0.1-1% w/v）、STPP（0.2-1.5% w/v）和不同体积的STPP（8-20 ml）制备了13种聚合物纳米颗粒制剂。甘露醇（5% w/v）用作冷冻保护剂。对制备的纳米颗粒制剂进行了各种参数的表征，如粒径、zeta电位、工艺产率、包封率、药物含量和体外药物释放。
含有0.1% w/v壳聚糖和10 ml体积的0.2% w/v STPP的纳米颗粒制剂NF-1在粒径（123.8nm）、多分散指数（0.247）、zeta电位（+30.4 mV）、工艺产率（68.09%）、药物含量（74.32%）、包封率（70.52%）和24小时内释放（56.2%）药物方面表现出最佳结果。体外药物释放分析表明吉非替尼从纳米颗粒中持续释放，并符合Korsmeyer-Peppas模型。
可以在低浓度的壳聚糖和STPP以及低体积的STPP条件下制备具有所需特性的纳米颗粒制剂。所制备的纳米颗粒可能被证明是治疗癌症的最佳选择。
