Samprasit Wipada, Akkaramongkolporn Prasert, Ngawhirunpat Tanasait, Rojanarata Theerasak, Kaomongkolgit Ruchadaporn, Opanasopit Praneet
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, NakhonPathom 73000, Thailand.
Department of Oral Diagnosis, Faculty of Dentistry, Naresuan University, Phitsanulok 65000, Thailand.
Int J Pharm. 2015 Jun 20;487(1-2):213-22. doi: 10.1016/j.ijpharm.2015.04.044. Epub 2015 Apr 18.
Fast release and taste masking of meloxicam (MX)-loaded polyvinylpyrrolidone (PVP)/cyclodextrin (CD) nanofiber mats were developed using an electrospinning process. CDs were blended to improve the stability of the mats. The morphology and diameter of the mats were determined using scanning electron microscopy (SEM); physical and mechanical properties were also studied. The MX content, disintegration time, MX release and cytotoxicity of the mats were investigated. In vivo studies were also performed in healthy human volunteers. The results indicated that the mats were successfully prepared with fiber in the nanometer range. MX was well incorporated into the mats, with an amorphous form. The mats showed suitable tensile strength. CDs improved the physical stability by their cage-like supramolecular structure to protect from humidity and moisture, and create bead free nanofiber mats. The nanofiber mats with CDs were physically stable without any hygroscopicity and fusion. A fast disintegration and release of MX was achieved. Moreover, this mat released MX faster than the MX powder and commercial tablets. The cytotoxicity test revealed that mats were safe for a 5-min incubation. The disintegration studies indicated that in vivo disintegration agreed with the in vitro studies; the mat rapidly disintegrated in the mouth. The less bitter of MX was occurred in the mats that incorporated CD, menthol and aspartame. In addition, this mat was physical stable for 6 months. The results suggest that these mats may be a good candidate for fast dissolving drug delivery systems of bitter drugs to increase the palatability of dosage forms.
采用静电纺丝工艺制备了载有美洛昔康(MX)的聚乙烯吡咯烷酮(PVP)/环糊精(CD)纳米纤维垫,以实现快速释放和掩味。将环糊精混合以提高垫的稳定性。使用扫描电子显微镜(SEM)测定垫的形态和直径;还研究了其物理和机械性能。研究了垫的美洛昔康含量、崩解时间、美洛昔康释放和细胞毒性。还在健康人类志愿者中进行了体内研究。结果表明,成功制备了纳米级纤维的垫。美洛昔康以无定形形式很好地掺入垫中。垫表现出合适的拉伸强度。环糊精通过其笼状超分子结构提高了物理稳定性,以防止受潮和吸湿,并形成无珠纳米纤维垫。含有环糊精的纳米纤维垫物理稳定,无任何吸湿性和融合现象。实现了美洛昔康的快速崩解和释放。此外,这种垫释放美洛昔康的速度比美洛昔康粉末和市售片剂更快。细胞毒性试验表明,垫在5分钟孵育时是安全的。崩解研究表明,体内崩解与体外研究一致;垫在口腔中迅速崩解。含有环糊精、薄荷醇和阿斯巴甜的垫中美洛昔康的苦味较小。此外,这种垫在6个月内物理稳定。结果表明,这些垫可能是苦味药物快速溶解给药系统增加剂型适口性的良好候选者。