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负载紫杉醇的硼化壳聚糖/海藻酸钠纳米粒作为用于局部宫颈癌药物递送的粘膜粘附系统的制剂与评价

Formulation and evaluation of paclitaxel-loaded boronated chitosan/alginate nanoparticles as a mucoadhesive system for localized cervical cancer drug delivery.

作者信息

Oluwadamilola Miriam Kolawole, Rosemary Ifeanafor Adaora, Adebimpe Ifade Wuraola, Olusola Akinleye Moshood, Prasopchai Patrojanasophon, Olanrewaju Silva Boladale, Adediran Osuntoki Akinniyi

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, University of Lagos, Lagos State, Nigeria.

Department of Pharmaceutical Chemistry, University of Lagos, Lagos State, Nigeria.

出版信息

J Drug Deliv Sci Technol. 2023 Sep;87. doi: 10.1016/j.jddst.2023.104810. Epub 2023 Aug 3.

Abstract

Cervical cancer remains a significant global health challenge, and there is a need for innovative drug delivery systems to improve the efficacy of anticancer drugs. In this study, we developed and evaluated boronated chitosan/alginate nanoparticles (BCHIALG NPs) as a localized mucoadhesive drug delivery system for cervical cancer. Boronated chitosan (BCHI) was synthesized by incorporating 4-carboxyphenylboronic acid onto chitosan (CHI), and boronated chitosan/alginate nanoparticles (BCHIALG NPs) with varying polymer ratios were prepared using an ionic gelation method. The physical properties, drug loading capacity/encapsulation efficiency, mucoadhesive properties, and drug release profile of the nanoparticles were evaluated. The BCHIALG NPs exhibited a size of less than 390 nm and demonstrated high drug encapsulation efficiency (98.1 - 99.8%) and loading capacity (326.9 - 332.7 μg/mg). Remarkably, the BCHIALG NPs containing 0.03% boronated chitosan and 0.07% alginate showed superior mucoadhesive capability compared to CHIALG NPs, providing sustained drug release and they showed the most promising results as a transmucosal drug delivery system for hydrophobic drugs like paclitaxel (PTX). To the best of our knowledge, this is the first report investigating BCHIALG NPs for cervical drug delivery. The new mucoadhesive paclitaxel formulation could offer an innovative strategy for improving cervical cancer treatment.

摘要

宫颈癌仍然是一项重大的全球健康挑战,因此需要创新的药物递送系统来提高抗癌药物的疗效。在本研究中,我们开发并评估了硼化壳聚糖/海藻酸钠纳米颗粒(BCHIALG NPs)作为一种用于宫颈癌的局部粘膜粘附药物递送系统。通过将4-羧基苯硼酸掺入壳聚糖(CHI)中来合成硼化壳聚糖(BCHI),并使用离子凝胶法制备了具有不同聚合物比例的硼化壳聚糖/海藻酸钠纳米颗粒(BCHIALG NPs)。评估了纳米颗粒的物理性质、载药量/包封率、粘膜粘附性质和药物释放曲线。BCHIALG NPs的粒径小于390 nm,表现出较高的药物包封率(98.1 - 99.8%)和载药量(326.9 - 332.7 μg/mg)。值得注意的是,含有0.03%硼化壳聚糖和0.07%海藻酸钠的BCHIALG NPs与CHIALG NPs相比,表现出优异的粘膜粘附能力,能够实现药物的持续释放,并且作为疏水性药物紫杉醇(PTX)的透粘膜药物递送系统显示出最有前景的结果。据我们所知,这是第一份研究BCHIALG NPs用于宫颈给药的报告。这种新型的粘膜粘附紫杉醇制剂可能为改善宫颈癌治疗提供一种创新策略。

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3
Vaginal drug delivery approaches for localized management of cervical cancer.阴道给药途径用于宫颈癌的局部治疗。
Adv Drug Deliv Rev. 2021 Jul;174:114-126. doi: 10.1016/j.addr.2021.04.009. Epub 2021 Apr 20.
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Cervical cancer.宫颈癌。
Lancet. 2019 Jan 12;393(10167):169-182. doi: 10.1016/S0140-6736(18)32470-X.

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