Gugu Thaddeus H, Eze Christopher O, Kenechukwu Franklin C, Khumaini Mudhar Bintang Muhammd A, Patil Sanjay B, Basarkar Ganesh D, Attama Anthony A, Ibezim Emmanuel C, Upasani Chandrashekhar D, Srichana Teerapol
Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka. Enugu State, Nigeria.
Drug Delivery System Excellence Center, Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
Heliyon. 2023 Jun 7;9(6):e16963. doi: 10.1016/j.heliyon.2023.e16963. eCollection 2023 Jun.
This research investigates the potentials of prodigiosinPG derived from bacteria and its formulations against triplenegative breast (TNB), lung, and colon cancer cells. The PG was extracted from using continuous batch culture, characterized, and formulated into lyophilized parenteral nanoparticles (PNPs). The formulations were characterized with respect to entrapment efficiency (EE), DSC, FT-IR, TEM, and proton nuclear magnetic resonance (1H NMR) spectroscopy. drug release was evaluated in phosphate buffer (pH 7.4) while acute toxicity, hematological and histopathological studies were performed on rats. The cytotoxicity was evaluated against TNB (MCF-7), lung (A-549), and colon (HT-29) cancer cell lines. High EE (92.3 ± 12%) and drug release of up to 89.4% within 8 h were obtained. DSC thermograms of PG and PG-PNPs showed endothermic peaks indicating amorphous nature. The FT-IR spectrum of PG-PNPs revealed remarkable peaks of pure PG, indicating no strong chemical interaction between the drug and excipients. The TEM micrograph of the PG-PNPs showed nano-sized formulations (20-30 nm) whose particles were mostly lamellar and hexagonal structures. The 1H NMR result revealed the chemical structure of PG showing all assigned proton chemical shifts. Toxicity results of the PG and its formulation up to a concentration of 5000 mg/kg showed insignificant vacuolar changes of hepatocytes in the liver, with normal renal medulla and cortex in the kidney. The PG and PG-PNPs inhibited the growth of breast, lung, and colon cell lines. The nano-sized lipid formulation (PG-PNPs) showed potential in PG delivery and cancer treatments.
本研究调查了源自细菌的灵菌红素(PG)及其制剂对三阴性乳腺癌(TNB)、肺癌和结肠癌细胞的作用潜力。通过连续分批培养从[未提及具体来源]中提取PG,对其进行表征,并将其制成冻干肠胃外纳米颗粒(PNPs)。对制剂进行了包封率(EE)、差示扫描量热法(DSC)、傅里叶变换红外光谱(FT-IR)、透射电子显微镜(TEM)和质子核磁共振(1H NMR)光谱表征。在磷酸盐缓冲液(pH 7.4)中评估药物释放,同时对大鼠进行急性毒性、血液学和组织病理学研究。评估了PG对TNB(MCF-7)、肺癌(A-549)和结肠(HT-29)癌细胞系的细胞毒性。获得了高达92.3±12%的高包封率以及8小时内高达89.4%的药物释放率。PG和PG-PNPs的DSC热谱图显示吸热峰,表明为无定形性质。PG-PNPs的FT-IR光谱显示出纯PG的明显峰,表明药物与辅料之间没有强烈的化学相互作用。PG-PNPs的TEM显微照片显示纳米级制剂(20 - 30纳米),其颗粒大多为层状和六边形结构。1H NMR结果揭示了PG的化学结构,显示了所有指定的质子化学位移。PG及其制剂在浓度高达5000毫克/千克时的毒性结果显示,肝脏中肝细胞的空泡变化不显著,肾脏的肾髓质和皮质正常。PG和PG-PNPs抑制了乳腺癌、肺癌和结肠癌细胞系的生长。纳米级脂质制剂(PG-PNPs)在PG递送和癌症治疗方面显示出潜力。