Sethi Aisha, Ahmad Mahmood, Khan Waheed S
Faculty of Pharmacy and Alternative Medicines, the Islamia University of Bahawalpur, Bahawalpur, Pakistan.
Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan.
Pak J Pharm Sci. 2019 May;32(3 (Supplementary)):1137-1143.
The aim of study was cross linking of high molecular weight chitosan nanoparticles containing 5-fluorouracil to improve dissolution rate and ultimately enhance its bioavailability by reverse emulsion/micelles method and cross-linking agent i.e. glutaraldehyde (GA 25% aqueous solution in water). The nature and outer morphologies were evaluated by scanning electron microscopy (SEM). Drug release models were functional to support way from cross linked NPs. Cross linking of 5-fluorouracil with glutaraldehyde improved dissolution rate. Mean dissolution time of 5-fluorouracil decreased significantly upon reverse emulsion/cross linking as encapsulated drug is protective and thermally stable within cross linked chitosan NPs. FTIR studies showed formation of intermolecular hydrogen bonding between 5-fluorouracil and GA-co-CHNPs. DSC studies indicated a less crystalline state of 5-fluorouracil in cross linking. SEM showed spherical nanoparticles with somewhat rough surface. 5-FU release followed Korsmeyer-Peppas model which indicate diffusion and dissociation control drug release from GA-co-CH-NPs. 5-FU cross linked chitosan nanoparticles can be safe and useful tool for other chemotherapeutic agents.
本研究的目的是通过反相乳液/胶束法以及交联剂戊二醛(25%戊二醛水溶液)对含5-氟尿嘧啶的高分子量壳聚糖纳米颗粒进行交联,以提高其溶解速率并最终提高其生物利用度。通过扫描电子显微镜(SEM)评估其性质和外部形态。药物释放模型有助于支持交联纳米颗粒的释放方式。5-氟尿嘧啶与戊二醛交联提高了溶解速率。反相乳液/交联后,5-氟尿嘧啶的平均溶解时间显著缩短,因为包封药物在交联壳聚糖纳米颗粒内具有保护作用且热稳定性良好。傅里叶变换红外光谱(FTIR)研究表明5-氟尿嘧啶与戊二醛交联的壳聚糖纳米颗粒(GA-co-CHNPs)之间形成了分子间氢键。差示扫描量热法(DSC)研究表明交联过程中5-氟尿嘧啶的结晶状态降低。扫描电子显微镜显示为表面略显粗糙的球形纳米颗粒。5-氟尿嘧啶的释放遵循Korsmeyer-Peppas模型,表明药物从GA-co-CH-NPs中释放受扩散和解离控制。5-氟尿嘧啶交联壳聚糖纳米颗粒可能是用于其他化疗药物的安全且有用的工具。