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Preparation and In Vitro Evaluation of Ethylcellulose and Polymethacrylate Resins Loaded Microparticles Containing Hydrophilic Drug

机译:载有亲水性药物的乙基纤维素和聚甲基丙烯酸酯树脂微粒的制备及体外评价

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摘要

Objective. The purpose of the recent study was to prepare and estimate sustained release of Ethylcellulose (300 cps) and Eudragit (RS 100 and RL 100) microparticles containing Propranolol hydrochloride used as a treatment of cardiovascular system, especially hypertension. Method. Propranolol hydrochloride was microencapsulated with different polymers (Ethylcellulose, Eudragit RS, and Eudragit RL) using modified hydrophobic (O/O) solvent evaporation method using 1 : 1 combination of acetone and isopropanol as the internal phase. Obtained microparticles were showing higher batch yield with higher encapsulation efficiency. Microparticles were prepared with different ratios of 1 : 1, 1 : 3, 1 : 5, and 1 : 7 (%, wt/wt) using span 80 (%, v/v) as a surfactant. Results. The influence of formulation factors like drug: polymer ratio, internal phase, and type of polymers on obtained microparticles was characterized with respect to particle size distribution, encapsulation efficiency, percentage yield, FTIR, and FE-SEM. Higher encapsulation efficiencies were obtained with various polymers like Ethylcellulose (96.63 ± 0.5) compared to Eudragit RS 100 (83.70 ± 0.6) and RL 100 (89.62 ± 0.6). The in vitro release study was characterized by initial burst. Conclusion. The result of study displays that Ethylcellulose and Eudragit loaded microparticles of Propranolol hydrochloride can be effectively prepared using modified hydrophobic emulsification solvent evaporation technique. Therefore, the modified hydrophobic emulsion technique can also be applied to the preparation of microparticles for low molecular weight and highly water soluble drugs.
机译:目的。这项最新研究的目的是制备和评估含有盐酸普萘洛尔的乙基纤维素(300µcps)和Eudragit(RS 100和RL 100)微粒的持续释放,这些微粒可用于治疗心血管系统,尤其是高血压。方法。盐酸普萘洛尔用不同的聚合物(乙基纤维素,Eudragit RS和Eudragit RL)微囊化,采用改进的疏水(O / O)溶剂蒸发法,以丙酮和异丙醇的1∶1:1组合作为内相。所获得的微粒显示出更高的批产量和更高的包封效率。使用跨度80(%,v / v)作为表面活性剂,以1∶1∶1、1∶3、1∶5和1∶7的不同比例制备微粒(%,wt / wt)。结果。相对于粒径分布,包封效率,收率,FTIR和FE-SEM,对药物,聚合物比例,内相和聚合物类型等配方因素对所得微粒的影响进行了表征。与Eudragit RS 100(83.70±0.6)和RL 100(89.62±0.6)相比,各种聚合物(如乙基纤维素(96.63±±0.5))获得的包封效率更高。体外释放研究的特征在于初始爆发。结论。研究结果表明,采用改进的疏水性乳化溶剂蒸发技术可有效制备盐酸普萘洛尔的乙基纤维素和负载Eudragit的微粒。因此,改进的疏水性乳液技术还可用于制备低分子量和高水溶性药物的微粒。

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