用于局部用药的姜黄素 12-羟基硬脂酸三醋酸有机凝胶的制备与表征

Duaa Razaq, Masar Basim Mohsin Mohamed, Lina A. Dahabiyeh
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摘要

背景:姜黄素(CUR)及其衍生物具有多种生物活性,如抗氧化、抗炎、抗肿瘤、抗微生物、抗寄生虫以及治疗皮肤病等。由于姜黄素存在水溶性低和生物利用度低等物理化学限制,我们开发了姜黄素有机凝胶作为外用给药系统,以克服这些限制。众所周知,12-羟基硬脂酸(12-HSA)是一种能够胶凝有机液相的低分子量有机凝胶(LMOGs)。将三醋精中不同浓度的(12-羟基硬脂酸)(50 毫克 CUR)胶凝并应用于各种检查:片剂流变学、油结合能力、pH 值测量、铺展性、体外药物释放、抗菌活性和振荡流变学研究。结果表明,有机凝胶从固态到液态的转变温度高于正常体温,这有助于有机凝胶保持形状;它们具有良好的涂抹性,有机凝胶的 pH 值在皮肤安全范围内。体外释放数据显示,4% 12HSA+5%CUR +TA (4TA)在 6 小时后的释放率为 100%。所选的 4TA 在振幅扫描测试中表现出良好的粘弹性,在频率扫描测试中表现出与频率无关的特性。CUR 对伤口损伤部位的金黄色葡萄球菌、化脓性链球菌、变形杆菌和大肠杆菌具有良好的抗菌作用,这表明 4TA 有机凝胶可用于局部伤口愈合。
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Formulation and Characterization of Curcumin 12-Hydroxystearic Acid in Triacetin Organogel for Topical Administration
Background: Curcumin (CUR) and its derivatives have shown a wide variety of biological activities, such as anti-oxidant, anti-inflammatory, anti-tumor, antimicrobial and antiparasitic effects as well as for the treatment of skin diseases. Due to its physico-chemical limitations such as low aqueous solubility and low bioavailability, we developed curcumin organogel as a topical delivery system to overcome those limitations. The12-hydroxystearic acid (12-HSA) is well known as a low-molecular-weight organogelators (LMOGs) capable of gelling an organic liquid phase. Different concentrations of (12-HSA) in triacetin with 50 mg CUR were gelled and applied for various examinations: tabletop rheology, oil binding capacity, pH measurement, spreadability, in vitro drug release, antibacterial activity and oscillatory rheology studies. The results revealed that the organogels transition temperatures from solid to liquid were greater than the normal body temperature, this helped the organogels keep their shape; they had good spreadability,and the organogels pH levels were within the safe range for the skin . In vitro release data showed that 4% 12HSA+5%CUR +TA (4TA) gave us 100% release after 6 hours. The selected 4TA illustrated good viscoelastic properties in the amplitude sweep test and a frequency-independent as seen in the frequency sweep test. CUR has good antibacterial action against Staphylococcus aureus; Streptococcus pyrogen, Proteus mirabilis, and Escherichia coli, which prevail at the site of wound injury as this pointed out that 4TA organogel can be used for topical wound healing.
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