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虾青素作为一种新型纳米结构脂质载体在局部递药系统中的开发与评价

Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery.

机构信息

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Benxi, 117004, China.

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, NO.26, Huatuo Street, Xihu District, Benxi City, 117004, Liaoning Province, China.

出版信息

AAPS PharmSciTech. 2020 Nov 11;21(8):318. doi: 10.1208/s12249-020-01822-w.

Abstract

The study is designed to formulate, optimize, and evaluate astaxanthin (ASTA)-loaded nanostructured lipid carrier (NLC) with an aim to improve its stability, water solubility, skin permeability and retention and reduce drug-related side effects. ASTA was extracted from Haematococcus pluvialis. ASTA-NLC was formulated by the technique of melt emulsification-ultrasonic and optimized taking solid:liquid lipid ratio, total lipid:drug ratio, drug concentration, emulsifier types, and amounts as independent variables with particle sizes (PS) and entrapment efficiency (EE) as dependent variables. The optimized formulation (N21) exhibited spherical surfaced stable nanoparticles of 67.4 ± 2.1 nm size and 94.3 ± 0.5% EE. Formulation N21 was then evaluated for its physiological properties, physicochemical properties, drug content, in vitro release and skin penetration, and retention analysis. The ASTA-NLC was found to be nonirritating, homogenous, and with excellent stability and water solubility. In vitro release studies showed the cumulative release rate of NLC was 83.0 ± 3.4% at 48 h. The skin penetration and retention studies indicated that cumulative permeability was 174.10 ± 4.38 μg/cm and the retention was 8.00 ± 1.62 μg/cm within 24 h. It can be concluded that NLC serves as a promising carrier for site specific targeting with better stability and skin penetration.

摘要

本研究旨在制备、优化和评价负载虾青素(ASTA)的纳米结构脂质载体(NLC),以提高其稳定性、水溶性、皮肤渗透性和滞留性,并降低药物相关的副作用。ASTA 从雨生红球藻中提取。采用熔融乳化-超声技术制备 ASTA-NLC,并以固液脂质比、总脂质与药物比、药物浓度、乳化剂种类和用量为自变量,以粒径(PS)和包封率(EE)为因变量进行优化。优化后的配方(N21)表现出粒径为 67.4 ± 2.1nm、包封率为 94.3 ± 0.5%的球形表面稳定纳米粒子。然后对配方 N21 的生理性质、理化性质、药物含量、体外释放和皮肤渗透、保留分析进行评价。结果表明,ASTA-NLC 无刺激性、均匀、稳定性和水溶性良好。体外释放研究表明,NLC 在 48h 时的累积释放率为 83.0 ± 3.4%。皮肤渗透和保留研究表明,24h 内累积渗透量为 174.10 ± 4.38μg/cm,滞留量为 8.00 ± 1.62μg/cm。综上所述,NLC 作为一种有前途的载体,具有更好的稳定性和皮肤渗透性,可实现靶向定位。

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