盐酸氨溴索的微球制剂:秋葵(Abelmoschus esculentus)粘液作为缓释聚合物的影响。

IF 4.4 3区 医学 Q2 ENGINEERING, BIOMEDICAL Progress in Biomaterials Pub Date : 2020-06-01 Epub Date: 2020-06-05 DOI:10.1007/s40204-020-00132-5
Adenike Okunlola, Michael Ayodele Odeniyi, Matthew Ikhuoria Arhewoh
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引用次数: 0

摘要

盐酸氨溴索(AH)是一种分泌释放型祛痰剂,是持续给药的理想选择。粘液质是一种可生物降解、价格低廉的微球制剂载体。本研究旨在使用从秋葵荚果中提取的秋葵粘液与海藻酸钠以不同的聚合物/药物比例制备秋葵氨酚微球。对秋葵粘液的形态、溶胀性、粘度和流动性进行了表征。采用离子乳化法制备了 AH 微球,并对其尺寸、夹持效率、膨胀指数和溶解时间(t50)进行了表征。采用 2 乘 3 的全因子实验设计,使用三个因子(秋葵粘液/精氨酸比率 X1;药物/聚合物比率 X2;聚合物浓度 X3),每个因子有两个水平,以确定配方变量对反应的影响。优化后的 AH 微球配方大小为 250.91 ± 16.22 至 462.10 ± 23.85 µm;膨胀指数为 1.35 ± 0.05 和 3.20 ± 0.03,夹带率为 55.70 ± 3.55-94.11 ± 4.50%。从溶解时间(t50)2.85±1.03-7.50±0.96 h 可以看出,微球具有长时间持续释放 AH 的特性。药物释放动力学一般遵循零阶,这意味着释放过程是恒定的,与药物的初始浓度无关。聚合物浓度对微球大小、夹持效率和溶解时间的影响最大,而秋葵/海藻酸比例对溶胀的影响最大。秋葵粘液是一种合适的聚合物,可以替代合成聚合物来维持盐酸氨溴索的释放。
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Microsphere formulations of ambroxol hydrochloride: influence of Okra (Abelmoschus esculentus) mucilage as a sustained release polymer.

Ambroxol hydrochloride (AH), a secretion-releasing expectorant, is a good candidate for sustained delivery. Mucilages are biodegradable, inexpensive carriers in microsphere formulations. The study aimed to prepare microspheres of AH using Okra mucilage obtained from pods of Abelmoschus esculentus combined with sodium alginate at various polymer/drug ratios. Okra mucilage was characterized for morphology, swelling, viscosity and flow properties. AH microspheres were prepared by ionic emulsification method and characterized using size, entrapment efficiency, swelling index and dissolution time (t50). A full 2 by 3 factorial experimental design using three factors (Okra mucilage/alginate ratio X1; drug/polymer ratio X2; and polymer concentration X3), each at two levels, was used to determine the effects of formulation variables on the responses. Optimized formulations of AH microspheres had sizes ranging from 250.91 ± 16.22 to 462.10 ± 23.85 µm; swelling index 1.35 ± 0.05 and 3.20 ± 0.03 and entrapment 55.70 ± 3.55-94.11 ± 4.50%. The microspheres exhibited sustained release of AH over a prolonged period as revealed by the dissolution time (t50) 2.85 ± 1.03-7.50 ± 0.96 h. Drug release kinetics generally followed zero order, implying that the process is constant and independent of the initial concentration of drug. Polymer concentration had the highest influence on microsphere size, entrapment efficiency and dissolution time while Okra/alginate ratio had the highest influence on swelling. Okra mucilage was a suitable polymer that could serve as an alternative to synthetic polymers in sustaining the release of ambroxol hydrochloride.

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来源期刊
Progress in Biomaterials
Progress in Biomaterials MATERIALS SCIENCE, BIOMATERIALS-
CiteScore
9.60
自引率
4.10%
发文量
35
期刊介绍: Progress in Biomaterials is a multidisciplinary, English-language publication of original contributions and reviews concerning studies of the preparation, performance and evaluation of biomaterials; the chemical, physical, biological and mechanical behavior of materials both in vitro and in vivo in areas such as tissue engineering and regenerative medicine, drug delivery and implants where biomaterials play a significant role. Including all areas of: design; preparation; performance and evaluation of nano- and biomaterials in tissue engineering; drug delivery systems; regenerative medicine; implantable medical devices; interaction of cells/stem cells on biomaterials and related applications.
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