Shende Pravin K, Gaud R S, Bakal Ravindra, Patil Dipmala
SPP-School of Pharmacy and Technology Management, SVKM's NMIMS University, Mumbai, India.
SPP-School of Pharmacy and Technology Management, SVKM's NMIMS University, Mumbai, India.
Colloids Surf B Biointerfaces. 2015 Dec 1;136:105-10. doi: 10.1016/j.colsurfb.2015.09.002. Epub 2015 Sep 3.
The objective of the present work was to develop inclusion complexes of meloxicam with β-cyclodextrin- and β-cyclodextrin-based nanosponges to enhance their solubility and stability and to prolong release using different methods that included physical mixing, kneading and sonication. Particle size, zeta potential, encapsulation efficiency, stability study results, in vitro and in vivo drug release study results, FTIR, DSC and XRPD were used as characterization parameters. SEM (Scanning Electron Microscope) studies revealed that the particle sizes of the inclusion complexes of meloxicam were within the range of 350 ± 5.69-765 ± 13.29 nm. The zeta potentials were sufficiently high to obtain stable formulations. In vitro and in vivo release studies revealed the controlled release of meloxicam from the nanosponges for 24h. The interaction of the meloxicam with the nanosponges was confirmed by FTIR and DSC. A XRPD study revealed that the crystalline nature of meloxicam was changed to an amorphous form due to the complexation with the nanosponges. A stability study revealed that the meloxicam nanosponges were stable. Therefore, β-cyclodextrin-based nanosponges represent a novel approach for the controlled release of meloxicam for anti-inflammatory and analgesic effects.
本研究的目的是开发美洛昔康与β-环糊精及基于β-环糊精的纳米海绵的包合物，以提高其溶解度和稳定性，并使用包括物理混合、捏合和超声处理在内的不同方法延长释放。粒径、zeta电位、包封率、稳定性研究结果、体外和体内药物释放研究结果、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和X射线粉末衍射（XRPD）用作表征参数。扫描电子显微镜（SEM）研究表明，美洛昔康包合物的粒径在350±5.69-765±13.29nm范围内。zeta电位足够高，可获得稳定的制剂。体外和体内释放研究表明，纳米海绵中美洛昔康可控制释放24小时。FTIR和DSC证实了美洛昔康与纳米海绵之间的相互作用。XRPD研究表明，由于与纳米海绵络合，美洛昔康的结晶性质转变为无定形形式。稳定性研究表明，美洛昔康纳米海绵是稳定的。因此，基于β-环糊精的纳米海绵代表了一种用于美洛昔康控释以实现抗炎和镇痛作用的新方法。
