Implication of Nanotechnology for Pulmonary Delivery of Docetaxel

Q3 Pharmacology, Toxicology and Pharmaceutics

Jordan Journal of Pharmaceutical Sciences Pub Date : 2023-07-24 DOI:10.35516/jjps.v16i2.1527

Alaa Abudayah

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Abstract

Docetaxel (Taxotere®) is a taxoid antineoplastic agent used in the treatment of various cancers. Docetaxel belongs to class IV drugs in the Biopharmaceutics Classification System (BCS), and their clinical use is limited due to their extreme hydrophobicity, low water solubility, low bioavailability, and high toxicity. This study aims to prepare nanoparticles for pulmonary delivery of Docetaxel with enhanced solubility and dissolution targeting pulmonary tissues. Accordingly, PLGA-Docetaxel nanoparticles (NPs) were prepared by nanoprecipitation method and coated with Carboxymethyl chitosan to investigate its effectiveness as inhaled anticancer therapy. Four formulations had been prepared to reach the highest loading capacity (LC%) and encapsulation efficiency (EE%) and to study the effect of the amount of Carboxymethyl chitosan on the drug release. The sizes, charges, homogeneity, surface morphology, LC% and EE% of the NPs were determined. The NPs were characterized using FTIR and XRD. In vitro release profiles of Docetaxel from PLGA NPs, at pH 5.5, 6.5, and 7.4 were determined. The sizes of the four formulations ranged between 227.7± 9.5 and 306.4 ± 27.4. All prepared formulations showed acceptable monodispersity with positive charges. The EE% was above 99% and the LC% ranged between 31-63%. The in vitro release of Docetaxel show an inverse relation to the amounts of Carboxymethyl chitosan used and the pH of the dissolution medium. In conclusion, coating PLGA NPs with Carboxymethyl chitosan may be used as a good carrier for pulmonary delivery of Docetaxel

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纳米技术在多西他赛肺部给药中的应用

多西他赛(Taxotere®)是一种用于治疗各种癌症的类taxetaxel抗肿瘤药物。多西紫杉醇在生物制药分类系统(BCS)中属于IV类药物，由于其极疏水性、低水溶性、低生物利用度和高毒性，其临床应用受到限制。本研究旨在制备多西紫杉醇肺递送纳米颗粒，增强其溶解度和溶出性，靶向肺组织。为此，采用纳米沉淀法制备了plga -多西紫杉醇纳米颗粒(NPs)，并以羧甲基壳聚糖包被，研究其吸入抗癌效果。以羧甲基壳聚糖的最高载药量(LC%)和包封率(EE%)为目标，研究了羧甲基壳聚糖用量对药物释放的影响。测定了NPs的尺寸、电荷、均匀性、表面形貌、LC%和EE%。用FTIR和XRD对NPs进行了表征。测定多西他赛在pH为5.5、6.5和7.4时在PLGA NPs中的体外释放谱。四种剂型的大小范围为227.7±9.5 ~ 306.4±27.4。所有制备的配方均表现出可接受的带正电荷的单分散性。EE%在99%以上，LC%在31 ~ 63%之间。多西紫杉醇的体外释放量与羧甲基壳聚糖的用量和溶出介质的pH值成反比。综上所述，羧甲基壳聚糖包覆PLGA NPs可作为多西紫杉醇肺给药的良好载体

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Jordan Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

1.70

自引率

0.00%

发文量

期刊介绍： The Jordan Journal of Pharmaceutical Sciences (JJPS) is a scientific, bi-annual, peer-reviewed publication that will focus on current topics of interest to the pharmaceutical community at large. Although the JJPS is intended to be of interest to pharmaceutical scientists, other healthy workers, and manufacturing processors will also find it most interesting and informative. Papers will cover basic pharmaceutical and applied research, scientific commentaries, as well as views, reviews. Topics on products will include manufacturing process, quality control, pharmaceutical engineering, pharmaceutical technology, and philosophies on all aspects of pharmaceutical sciences. The editorial advisory board would like to place an emphasis on new and innovative methods, technologies, and techniques for the pharmaceutical industry. The reader will find a broad range of important topics in this first issue.