Kumar Arun, Behl Tapan, Uniyal Toshi, Chadha Swati
Chitkara College of Pharmacy, Chitkara University, Punjab, India.
Department of Pharmacy, Jaypee University of Information Technology, Waknaghat, Solan, Himachal Pradesh, India.
Pharm Nanotechnol. 2020;8(5):418-432. doi: 10.2174/2211738508666200907110444.
Antimalarial therapy remains the utmost effective means for the management of malarial parasites in the liver and red blood cells. The application of these therapeutic agents is hampered by their improper application, hepato-toxicity caused by their continuous use, and degradation by hepatic enzymes.
Recent advancements in drug delivery applications have shown potential in improving the pharmacological properties of artemether. Nanostructured lipid carriers (NLCs) loaded chitosan (CH)/Carbopol (CB) hybrid gel was prepared using glycerol monostearate (GMS) as solid lipid and clove oil as a liquid lipid for artemether (ART) and curcumin (CR) for its localized effect on the liver.
The smaller particle size (118 ± 1.0 nm) and high zeta potential (- 41.1 ± 6.46 mV) confirm the formulation and stability of NLCs. On the other hand, the shape and morphology of prepared NLCs and gel showed a spherical and wrinkled surface with a size range of 150-250 nm. The release studies of the NLC's showed a controlled release of artemether ( 92%) and curcumin (~ 83%) for up to 30 h. Photostability data showed that, approximately, ~86.5 ± 0.3% and ~60 ± 0.9% of nanoencapsulated artemether and curcumin were still detected on exposure to sunlight, respectively. It has been found from the permeation study that 69.8% and 49.1% of the drug was permeated across the mucus membrane in 24 h with a significant increase (P < 0.05) in flux as well as permeability coefficients.
The overall results showed that prepared CH/CB/NLCs hybrid gel could be a promising vehicle for the effective delivery of ART and CR for the management of malarial parasites. Lay Summary: Antimalarial therapy remains the utmost effective means for the management of malarial parasites in liver and red blood cells. Recent advancements in drug delivery applications have shown potential in improving the pharmacological properties of artemether. Application of these therapeutic agents hampered by their improper application, hepato-toxicity caused by their continuous use and degradation by hepatic enzymes. To manage the above issues, we synthesize nanostructured lipid carriers (NLC's) loaded chitosan (CH)/Carbopol (CB) hybrid gel using glycerol monostearate (GMS) as solid lipid and clove oil as liquid lipid for artemether (ATR) and curcumin (CR) for its local action in liver and the major criteria were to find a protective barrier with hepatoprotective nature of the curcumin.
抗疟治疗仍然是控制肝脏和红细胞中疟原虫的最有效手段。这些治疗药物的应用受到不当使用、持续使用导致的肝毒性以及被肝酶降解的阻碍。
药物递送应用的最新进展显示出改善蒿甲醚药理特性的潜力。使用单硬脂酸甘油酯（GMS）作为固体脂质、丁香油作为液体脂质制备负载壳聚糖（CH）/卡波姆（CB）杂化凝胶的纳米结构脂质载体（NLCs），用于蒿甲醚（ART）和姜黄素（CR），以实现其对肝脏的局部作用。
较小的粒径（约118±1.0 nm）和高zeta电位（-41.1±6.46 mV）证实了NLCs的制剂和稳定性。另一方面，制备的NLCs和凝胶的形状和形态显示为球形且表面有皱纹，尺寸范围为150 - 250 nm。NLCs的释放研究表明，蒿甲醚（约92%）和姜黄素（约83%）在长达30小时内呈现控释。光稳定性数据表明，纳米包封的蒿甲醚和姜黄素在暴露于阳光下时，分别仍可检测到约86.5±0.3%和约60±0.9%。渗透研究发现，24小时内69.8%和49.1%的药物透过黏膜，通量和渗透系数均显著增加（P<0.05）。
总体结果表明，制备的CH/CB/NLCs杂化凝胶可能是有效递送ART和CR以控制疟原虫的有前景的载体。简述：抗疟治疗仍然是控制肝脏和红细胞中疟原虫的最有效手段。药物递送应用的最新进展显示出改善蒿甲醚药理特性的潜力。这些治疗药物的应用受到不当使用、持续使用导致的肝毒性以及被肝酶降解的阻碍。为解决上述问题，我们使用单硬脂酸甘油酯（GMS）作为固体脂质、丁香油作为液体脂质制备负载壳聚糖（CH）/卡波姆（CB）杂化凝胶的纳米结构脂质载体（NLCs），用于蒿甲醚（ATR）和姜黄素（CR），以实现其在肝脏中的局部作用，主要目标是找到具有姜黄素肝保护性质的保护屏障。
