Chaiwarit Tanpong, Sommano Sarana Rose, Rachtanapun Pornchai, Kantrong Nutthapong, Ruksiriwanich Warintorn, Kumpugdee-Vollrath Mont, Jantrawut Pensak
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Plant Bioactive Compound Laboratory (BAC), Department of Plant and Soil Sciences, Faculty of Agriculture, Chiang Mai University, Chiang Mai 50200, Thailand.
Polymers (Basel). 2022 Apr 24;14(9):1736. doi: 10.3390/polym14091736.
Polymeric nanoparticles are one method to modify the drug release of small hydrophilic molecules. In this study, clindamycin HCl was used as a model drug loaded in carboxymethyl chitosan nanoparticles cross-linked with Ca2+ ions (CMCS-Ca2+). The ultrasonication with experimental design was used to produce CMCS-Ca2+ nanoparticles loading clindamycin HCl. The model showed that the size of nanoparticles decreased when amplitude and time increased. The nanoparticle size of 318.40 ± 7.56 nm, decreased significantly from 543.63 ± 55.07 nm (p < 0.05), was obtained from 75% of amplitude and 180 s of time, which was one of the optimal conditions. The clindamycin loading content in this condition was 34.68 ± 2.54%. The drug content in nanoparticles showed an inverse relationship with the size of the nanoparticles. The sodium carboxymethylcellulose film loading clindamycin HCl nanoparticles exhibited extended release with 69.88 ± 2.03% drug release at 60 min and a gradual increase to 94.99 ± 4.70% at 24 h, and demonstrated good antibacterial activity against S. aureus and C. acne with 40.72 ± 1.23 and 48.70 ± 1.99 mm of the zone of inhibition at 24 h, respectively. Thus, CMCS-Ca2+ nanoparticles produced by the ultrasound-assisted technique could be a potential delivery system to modify the drug release of small hydrophilic antibiotics.
聚合物纳米颗粒是一种改变小亲水分子药物释放的方法。在本研究中,盐酸克林霉素用作载于与Ca2+离子交联的羧甲基壳聚糖纳米颗粒(CMCS-Ca2+)中的模型药物。采用带有实验设计的超声处理来制备载有盐酸克林霉素的CMCS-Ca2+纳米颗粒。模型显示,当振幅和时间增加时,纳米颗粒的尺寸减小。在75%的振幅和180秒的时间条件下获得的纳米颗粒尺寸为318.40±7.56nm,较543.63±55.07nm显著减小(p<0.05),这是最佳条件之一。在此条件下克林霉素的负载量为34.68±2.54%。纳米颗粒中的药物含量与纳米颗粒的尺寸呈反比关系。载有盐酸克林霉素纳米颗粒的羧甲基纤维素钠膜表现出缓释特性,在60分钟时药物释放率为69.88±2.03%,在24小时时逐渐增加至94.99±4.70%,并且对金黄色葡萄球菌和痤疮丙酸杆菌显示出良好的抗菌活性,在24小时时抑菌圈直径分别为40.72±1.23和48.70±1.99mm。因此,通过超声辅助技术制备的CMCS-Ca2+纳米颗粒可能是一种改变小亲水性抗生素药物释放的潜在递送系统。