Khan Mohammad Ashif, Akhtar Nida, Sharma Vijay, Pathak Kamla
Department of Pharmaceutics, Rajiv Academy for Pharmacy, N.H. #2, Delhi Mathura Road, P.O. Chhattikara, Mathura-281001, India.
Pharmaceutics. 2015 Apr 27;7(2):43-63. doi: 10.3390/pharmaceutics7020043.
Curcumin suffers from the limitation of poor solubility and low dissolution that can lead to limited applications. The investigation was aimed to substantiate the potentiality of melt sonocrystallized gastroretentive tablets of curcumin. Melt sonocrystallized curcumin (MSC CMN) was developed and its therapeutic potential was validated by in vitro cytotoxicity studies against Human oral cancer cell line KB. MSC curcumin was then formulated as floating tablet and evaluated. MSC form of CMN exhibited 2.36-fold and 2.40-fold solubility enhancement in distilled water and phosphate buffer, pH 4.5, respectively, better flow properties and intrinsic dissolution rate (0.242 ± 1.42 and 0.195 ± 1.26 mg/cm2/min) in comparison to its original form. The GI50 value of MSC CMN was found to be less than 10, specifying inhibition of growth more effectively at its least concentration by 50%. The gastroretentive-floating tablet (Formulation F4) displayed controlled drug release (96.22% ± 1.43%) for over 12 h. The present study revealed melt sonocrystallization can be used to produce particles with superior biopharmaceutical properties without the use of organic solvents or the addition of other excipients, and amenable to formulation in to a pharmaceutical dosage form.
姜黄素存在溶解度差和溶出度低的局限性,这可能导致其应用受限。本研究旨在证实姜黄素熔融声结晶胃滞留片的潜力。制备了熔融声结晶姜黄素(MSC CMN),并通过针对人口腔癌细胞系KB的体外细胞毒性研究验证了其治疗潜力。然后将MSC姜黄素制成漂浮片并进行评价。与原始形式相比,CMN的MSC形式在蒸馏水和pH 4.5的磷酸盐缓冲液中的溶解度分别提高了2.36倍和2.40倍,具有更好的流动性和固有溶出速率(分别为0.242±1.42和0.195±1.26 mg/cm²/min)。发现MSC CMN的GI50值小于10,表明在最低浓度下能更有效地抑制50%的生长。胃滞留漂浮片(制剂F4)在12小时以上显示出控释效果(96.22%±1.43%)。本研究表明,熔融声结晶可用于制备具有优异生物药剂学性质的颗粒,无需使用有机溶剂或添加其他辅料,并且适合制成药物剂型。