Research Lab, GIET School of Pharmacy, NH-5, Chaitanya Nagar, Rajahmundry-533 294, India.
Drug Deliv. 2011 Apr;18(3):198-207. doi: 10.3109/10717544.2010.528069. Epub 2010 Oct 28.
The use of glucocorticoids in the treatment of rheumatoid arthritis has been widely employed, but, owing to their systemic side-effects and also their susceptibility to the first pass metabolism, their use is being discouraged. To circumvent this, triamcinolone (TA) were encapsulated in chitosan microspheres with glutaraldehyde as the cross-linking agent to achieve a prolonged drug release. The percentage of drug loading, encapsulation efficiency, and surface morphology by Scanning electron microscopy (SEM), Phase transition by Differential scanning colorimetry (DSC), as well as Fourier transform infrared spectroscopy (FTIR) studies was carried out to characterize the chitosan microspheres. In-vitro and in-vivo release studies revealed that microspheres were able to control the release of TA with a uniform release pattern up to a period of 36 days and thereafter an extended release up to 63 days. The clinical parameters were investigated for changes in paw volume, hematological parameters like Erythrocyte sedimentation rate (ESR), Paced cell volume (PCV), Total leucocyte count (TLC), Hb, and Differential cell count (DCC) in Fruend's complete adjuvant induced arthritic rats. Histopathological findings as well as radiology (X-ray) further confirmed the effectiveness of TA encapsulated microspheres in mitigating the rat arthritic model.
在类风湿性关节炎的治疗中，糖皮质激素的应用已经得到了广泛的应用，但是由于其全身副作用以及首过代谢的易感性，其应用受到了限制。为了克服这一问题，我们采用戊二醛作为交联剂，将曲安奈德（TA）包封在壳聚糖微球中，以实现药物的长效释放。通过扫描电子显微镜（SEM）进行药物载药量、包封效率和表面形态的研究，通过差示扫描量热法（DSC）进行相转变研究，以及傅里叶变换红外光谱（FTIR）研究来表征壳聚糖微球。体外和体内释放研究表明，微球能够控制 TA 的释放，具有均匀的释放模式，可达 36 天，此后可延长至 63 天。在弗氏完全佐剂诱导的关节炎大鼠中，我们研究了临床参数（如爪体积、红细胞沉降率（ESR）、红细胞压积（PCV）、白细胞总数（TLC）、血红蛋白（Hb）和白细胞分类计数（DCC）的变化）。组织病理学和放射学（X 射线）发现进一步证实了 TA 包封微球在减轻大鼠关节炎模型方面的有效性。
