加载 Plumbagin 的 pH 值响应型阴道纳米制剂的抗菌、抗真菌和细胞毒性潜力

IF 3.1 4区 生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Applied Biochemistry and Biotechnology Pub Date : 2024-06-27 DOI:10.1007/s12010-024-04987-3
Tamil Mani Subi, Nandhakumar Selvasudha, Sivakumar Priyadharshini, Pradeep Kumar, Rakesh Singh, Hannah Rachel Vasanthi
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引用次数: 0

摘要

Plumbagin 是一种萘醌,产自 Plumbago 植物的根部,具有抗癌活性。由于其溶解性和生物利用度较差,Plumbagin 在生物医学领域的转化应用受到限制。因此,本研究采用等压凝胶技术制备了具有聚乳酸(PLA)-壳聚糖聚合物外衣的 pH 响应型铅蓝蛋白阴道纳米制剂。在制备的四种(F1、F2、F3、F4)纳米制剂中,F3 通过傅立叶变换红外光谱(FTIR)、X 射线衍射(XRD)和热分析证明了聚合物与昆布素良好的相互作用。F3 的正 zeta 电位(48.4 ± 5.57 mV)、最佳尺寸(694 ± 65.76 nm)、低 PDI(0.157)和良好的包封效率(77.8 ± 3.62%)均十分显著。间接载药量法(58.35 ± 5.00%)证实,1 毫克 F3 中的药物含量约为 495.44 ± 5.00 µg plumbagin。通过 TEM 分析确认了药物负载模式,通过 SEM 分析确认了纳米复合材料的球形形态。在 pH 值分别为 4.5 和 7 的模拟阴道液中,F3 制剂在 24 小时内的药物释放率分别为 46%和 25.2%,且具有持续释放和聚乳酸水解作用。在所有评估的纳米制剂中,纳米制剂 F3 具有良好的理化特性,对各种真菌和细菌菌株具有良好的抗真菌和抗细菌活性。F3 具有很强的细胞毒性,对 HeLa 细胞的 IC50 为 3.6 ± 0.12 µg/ml,对 SiHa 细胞的 IC50 为 0.81 ± 0.01 µg/ml。总之,纳米制剂 F3 对阴道感染具有强效抗菌活性,对宫颈癌细胞株具有细胞毒性。
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Antibacterial, Antifungal, and Cytotoxic Potential of PlumbaginLoaded pH-Responsive Vaginal Nanoformulations.

Plumbagin is a naphthoquinone from the roots of the Plumbago species and exhibits anticancer activity. Translational usage of plumbagin in biomedical sciences is restricted due to its poor solubility and bioavailability. Therefore, pH-responsive plumbagin-loaded vaginal nanoformulations with polylactic acid (PLA)-chitosan polymeric coat were fabricated by inotropic gelation technique. Among the four (F1, F2, F3, F4) nanoformulations prepared, F3 exhibited good interaction of polymers with plumbagin as evidenced by FTIR, XRD, and thermal analysis. The positive zeta potential (48.4 ± 5.57 mV), optimal size (694 ± 65.76 nm), low PDI (0.157), and good encapsulation efficiency (77.8 ± 3.62%) of F3 were significant. The indirect method of drug loading (58.35 ± 5.00%) confirmed the drug content of about 495.44 ± 5.00 µg of plumbagin in 1 mg of F3. The drug loading pattern was confirmed by TEM analysis, and the spherical morphology of the nanocomposite was confirmed by SEM analysis. F3 formulation showed 46% and 25.2% of drug release in 24 h in simulated vaginal fluid at pH 4.5 and 7 respectively with sustained release and hydrolyses of lactic acid from PLA. Among all the nanoformulations evaluated, nanoformulation F3 with promising physicochemical properties showed good antifungal and antibacterial activity against various fungal and bacterial strains. F3 exhibited potent cytotoxicity with an IC50 of 3.6 ± 0.12 µg/ml for HeLa and an IC50 of 0.81 ± 0.01 µg/ml for SiHa cells. Altogether, the nanoformulation F3 exhibited potent antimicrobial activity against vaginal infections and cytotoxicity against cervical cancer cell lines.

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来源期刊
Applied Biochemistry and Biotechnology
Applied Biochemistry and Biotechnology 工程技术-生化与分子生物学
CiteScore
5.70
自引率
6.70%
发文量
460
审稿时长
5.3 months
期刊介绍: This journal is devoted to publishing the highest quality innovative papers in the fields of biochemistry and biotechnology. The typical focus of the journal is to report applications of novel scientific and technological breakthroughs, as well as technological subjects that are still in the proof-of-concept stage. Applied Biochemistry and Biotechnology provides a forum for case studies and practical concepts of biotechnology, utilization, including controls, statistical data analysis, problem descriptions unique to a particular application, and bioprocess economic analyses. The journal publishes reviews deemed of interest to readers, as well as book reviews, meeting and symposia notices, and news items relating to biotechnology in both the industrial and academic communities. In addition, Applied Biochemistry and Biotechnology often publishes lists of patents and publications of special interest to readers.
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