微波辅助微乳液经皮递送酮洛芬固体脂质纳米颗粒的抗炎作用

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Accounts of Chemical Research Pub Date : 2022-01-26 DOI:10.2174/2772270816666220126105802
Swati Changdeo Jagdale, Manisha Suresh Bafna, Anuruddha R Chabukswar
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引用次数: 0

摘要

目的:利用微波法制备酮洛芬(Ketoprofen,KP)的固体脂质纳米粒(SLNs)。酮洛芬(Ketoprofen,KP)是 2-(3-苯酚苯基)丙酸,具有消炎、镇痛和解热作用。这种药物的半衰期很短,只有 120 分钟。属于 BCS 二级药物。由于药物的酸性,胃刺激是给药的主要限制因素。本研究的目的是开发经皮给药的固体脂质纳米颗粒:方法:采用微波辅助微乳技术开发固体脂质纳米颗粒。硬脂酸用作脂质,吐温 80 用作表面活性剂。通过改变脂质类型和输入能量瓦数,配制出不同批次的产品。对 SLN 进行了 zeta 电位、药物夹带、粒度和体外药物释放评估。通过差示扫描量热法和粉末 X 射线衍射法测定了结晶度。对 M4 批次 SLNs 的抗炎活性进行了评估。为 M4 批次制备了凝胶。结果:结果:SLN 研制成功。根据尺寸、夹持效率、稳定性和药物释放情况,选择了 M4 批次。SLN的包埋效率为74.8%。溶解度提高了 40 倍。粒径为 682.9 nm,平均粒径为 1047 nm。PDI 为 0.685。Zeta 电位为 -29.5 mV。在体外药物释放过程中,M4 SLNs 批次凝胶出现猝灭释放,随后控制释放 8 小时:结论:微波辅助微乳液技术成功制备了 SLNs。成功研制出了具有抗炎活性的透皮给药 SLNs。
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Transdermal Anti-Inflammatory Delivery for Solid Lipid Nanoparticles of Ketoprofen by Microwave-Assisted Microemulsion.

Purpose: To prepare solid lipid nanopaticles (SLNs) of Ketoprofen (KP) using microwave method. Ketoprofen (KP) is 2-(3-benzolphenyl) propionic acid with anti-inflammatory, analgesic and antipyretic property. The drug has short half-life of 120 mins. It belongs to BCS Class II drug. Gastric irritation is a major limitation for delivery because of acidic nature of the drug. Development of solid lipid nanoparticles with its transdermal drug delivery was the aim of present work.

Methods: Microwave-assisted microemulsion technique was used for the development of solid lipid nanoparticles. Stearic acid was used as lipid and tween 80 was used as surfactant. By varying the type of lipid and input energy watt, batches were formulated. SLNs were evaluated for zeta potential, drug entrapment, particle size and in-vitro drug release. Crystallinity behaviour was determined by differential scanning calorimetry and powder X-ray diffraction. Anti-inflammatory activity was evaluated for batch M4 of SLNs. The gel was prepared for M4 batch. It was evaluated for viscosity, pH, drug content, in-vitro and ex-vivo diffusion study.

Results: SLN were developed successfully. Based on the size, entrapment efficiency, stability and drug release, batch M4 was selected. SLNs showed 74.8% entrapment efficiency. Forty-fold improvement was observed in the solubility. The particle size was of 682.9 nm and average size of 1047 nm. PDI was 0.685. Zeta potential was -29.5 mV. M4 SLNs batch of gel showed burst release followed by a controlled release for 8 hrs in in-vitro drug release.

Conclusion: SLNs were successfully prepared by Microwave-assisted microemulsion technique. SLNs with anti-inflammatory activity was successfully developed with its transdermal delivery.

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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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