Targeting Cancer with Sweet Precision: Saccharide-Grafted Erlotinib for Enhanced Drug Delivery

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-09-28 DOI:10.1007/s12247-024-09871-5

Isha Shete, Smita Kumbhar, Rakesh Dhavale, Manish Bhatia

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Abstract

Purpose

This study aims to enhance the targeting of erlotinib by grafting saccharides—galactose, pectin, and chitosan via oxalyl chloride-mediated processes. The objective is to evaluate the potential of these saccharide derivatives as ligands for targeted drug delivery, particularly to improve therapeutic efficacy in cancer treatments.

Methods

Saccharides (galactose, pectin, and chitosan) were chemically grafted onto erlotinib, forming conjugates. Characterization was conducted using 1H NMR, differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR). The conjugates’ drug delivery efficiency was tested using A549 cell lines to assess their efficacy in targeting cancer cells.

Results

Characterization confirmed the successful grafting of saccharides onto erlotinib, as evidenced by 1H NMR, DSC, and FTIR. The in vitro drug release study demonstrated enhanced targeting efficiency of the saccharide-erlotinib conjugates, with improved cell-specific distribution and potential therapeutic benefits.

Conclusions

Grafting saccharides onto erlotinib offers a promising approach to enhance drug absorption, reduce degradation, and minimize side effects in cancer therapy. This targeted drug delivery strategy represents a significant advancement in biomedical engineering for optimizing cancer treatment efficacy.

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精准锁定癌症：多糖接枝厄洛替尼增强给药效果

目的本研究旨在通过草酰氯介导的工艺接枝糖类--半乳糖、果胶和壳聚糖，增强厄洛替尼的靶向性。目的是评估这些糖衍生物作为配体用于靶向给药的潜力，特别是提高癌症治疗的疗效。方法将糖（半乳糖、果胶和壳聚糖）化学接枝到厄洛替尼上，形成共轭物。采用 1H NMR、差示扫描量热法（DSC）和傅立叶变换红外光谱法（FTIR）对共轭物进行了表征。结果表征结果表明，1H NMR、DSC 和傅立叶变换红外光谱证明糖类成功接枝到厄洛替尼上。体外药物释放研究表明，糖类-厄洛替尼共轭物的靶向效率得到提高，细胞特异性分布得到改善，具有潜在的治疗效果。这种靶向给药策略代表了生物医学工程在优化癌症疗效方面的重大进展。

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

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.