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含抗痤疮剂微海绵的新型乳膏:配方研发与评估

Novel Cream Containing Microsponges of Anti-Acne Agent: Formulation Development and Evaluation.

作者信息

Osmani Riyaz Ali M, Aloorkar Nagesh H, Kulkarni Ajit S, Kulkarni Parthasarathi K, Hani Umme, Thirumaleshwar Shailesh, Bhosale Rohit R

机构信息

Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Sri Shivarathreeshwara Nagar, Mysore-570 015 (Karnataka), India.

出版信息

Curr Drug Deliv. 2015;12(5):504-16. doi: 10.2174/1567201812666150212122421.

Abstract

The rationale behind present work was to formulate a novel cream containing microsponges of miconazole nitrate to provide prolonged release. By means of quasi-emulsion solvent diffusion method using Eudragit RS-100 with different drug-polymer ratios microsponges were prepared. In the direction of optimizing microsponge formulation, diverse factors that affect microparticles physical properties were also investigated. Microsponges were characterized by SEM, DSC, FT-IR and particle size analysis, and also evaluated for morphology, drug loading and in vitro drug release. The drug polymer ratio reflected notable effect on drug content, encapsulation efficiency and particle size. It has been found that there was no chemical interaction between drug and polymers used as revealed by FT-IR and DSC spectra. SEM micrographs exposed that microsponges were spherical, with porous surface and have had 26.23 μm mean particle size. The microsponges were then incorporated in cream; which showed viscous modulus along with pseudoplastic behavior. In vitro drug release results depicted that microsponge with drug-polymer ratio of 1:2 was more efficient to give extended drug release of 78.28% at the end of 8 h; while conventional formulations get exhausted incredibly earlier by releasing 83.09% drug at the end of 4 h only. Thus the formulated cream containing microsponges of miconazole nitrate would be a promising alternative as compared to conventional therapy for secure and efficient treatment of acne and other topical infections.

摘要

目前这项工作的基本原理是制备一种含有硝酸咪康唑微海绵的新型乳膏,以实现药物的长效释放。采用准乳液溶剂扩散法,使用不同药物-聚合物比例的Eudragit RS-100制备微海绵。在优化微海绵制剂的过程中,还研究了影响微粒物理性质的各种因素。通过扫描电子显微镜(SEM)、差示扫描量热法(DSC)、傅里叶变换红外光谱(FT-IR)和粒度分析对微海绵进行表征,并对其形态、载药量和体外药物释放进行评估。药物与聚合物的比例对药物含量、包封效率和粒径有显著影响。FT-IR和DSC光谱显示,药物与所用聚合物之间没有化学相互作用。SEM显微照片显示,微海绵呈球形,表面多孔,平均粒径为26.23μm。然后将微海绵加入乳膏中,该乳膏表现出粘性模量和假塑性行为。体外药物释放结果表明,药物-聚合物比例为1:2的微海绵在8小时结束时更有效地实现了78.28%的药物缓释;而传统制剂在4小时结束时仅释放了83.09%的药物,更早地耗尽了药物。因此,与传统疗法相比,所制备的含有硝酸咪康唑微海绵的乳膏在安全有效地治疗痤疮和其他局部感染方面可能是一种有前途的替代方法。

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