用基于TOPSIS的田口设计方法提高PLGA纳米颗粒的多柔比星负载量:水相的影响

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-09-24 DOI:10.1007/s12247-024-09868-0
Hayrettin Tonbul, Gözde Ultav
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引用次数: 0

摘要

目的 PLGA 纳米颗粒是所有聚合物纳米颗粒中研究最多的给药系统之一。虽然已有几种 PLGA 微粒系统成功开发并上市销售,但遗憾的是,PLGA 纳米颗粒系统在从体外到临床和市场转化方面进展甚微。其中一个主要原因是 PLGA 纳米颗粒的药物负载能力非常低。这种情况在某些药物(如多柔比星)中变得更加棘手。多柔比星是一种非常有趣的分子,其溶解度和特性会随着 pH 值以及介质中各种离子和化合物的存在而发生显著变化。多柔比星的这一特性可能会直接影响多柔比星在 PLGA 纳米颗粒中的载药量。本研究旨在提高多柔比星在 PLGA 纳米粒子中的载药量,同时使平均粒径和多分散指数处于可接受的范围内。方法采用基于田口试验设计(TOPSIS-based Taguchi experimental design)的方法,主要考察水相添加剂对药物载量、包封效率、粒径和多分散指数的影响。结果结果表明,与空白水作为水相相比,使用 PBS 和 HEPES 可以改善总体结果。这些发现将对负载多柔比星的 PLGA 纳米粒子领域的研究人员今后的研究大有裨益。
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Improving the Doxorubicin Loading to PLGA Nanoparticles with TOPSIS-Based Taguchi Design Approach: Effect of the Water Phase

Purpose

PLGA nanoparticles are one of the most investigated drug delivery systems among all polymeric nanoparticles. Although there are several successfully developed and marketed microparticulate PLGA systems, unfortunately, there was little progress in the in vitro to clinic and marketing translation of PLGA nanoparticulate systems. One of the main reasons is the very low drug-loading capacity of PLGA nanoparticles. This situation becomes more problematic in some drugs such as doxorubicin. Doxorubicin is a very interesting molecule whose solubility and characteristics dramatically change depending on pH and the presence of various ions and compounds in the medium. This property of the doxorubicin probably directly influences the drug loading of the doxorubicin to PLGA nanoparticles. In this study, it was aimed to improve the doxorubicin loading to PLGA nanoparticles while the average particle size and polydispersity index are in the acceptable ranges.

Method

TOPSIS-based Taguchi experimental design was adopted and the effect mainly water phase additive on drug loading, encapsulation efficiency, particle size, and polydispersity index were investigated.

Result

Results show that generally using PBS and HEPES improves the overall results when compared with blank water as the water phase.

Conclusion

Within the study, TOPSIS-based Taguchi design was successfully applied to the optimization of a PLGA nanoparticle formulation, and the optimum water phase additive was determined. These findings will be very beneficial to the researcher in the field of doxorubicin-loaded PLGA nanoparticles in their future studies.

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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