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用于增强皮肤滞留局部递送的载姜黄素纳米结构脂质载体:优化、放大、体外表征及离体皮肤沉积评估

Curcumin loaded nanostructured lipid carriers for enhanced skin retained topical delivery: optimization, scale-up, in-vitro characterization and assessment of ex-vivo skin deposition.

作者信息

Rapalli Vamshi Krishna, Kaul Vedhant, Waghule Tejashree, Gorantla Srividya, Sharma Swati, Roy Aniruddha, Dubey Sunil Kumar, Singhvi Gautam

机构信息

Industrial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani333031, India.

出版信息

Eur J Pharm Sci. 2020 Sep 1;152:105438. doi: 10.1016/j.ejps.2020.105438. Epub 2020 Jun 27.

Abstract

Nanostructured lipid carriers (NLC) have become a promising drug delivery system for topical delivery of drugs. Delivery of lipophilic drugs with improved stability and entrapment efficiency is one of the foremost benefits of NLC based formulations. The objective of the present study was to improve the permeation of poorly soluble curcumin into topical skin layers for the treatment of chronic inflammatory disorder psoriasis and microbial mediated acne vulgaris. Hot emulsification followed by probe sonication method was employed for the preparation of the curcumin loaded NLC. Further, in-vitro and ex-vivo characterization was performed for designed NLC. The designed NLC showed a mean particle size 96.2 ± 0.9 nm, entrapment efficiency of 70.5 ± 1.65% and zeta potential of -15.2 ± 0.566 mV. Curcumin-NLC showed extended in-vitro release upto 48 hours, whereas free curcumin showed 100% drug release within 4 hours. Ex-vivo skin permeation studies revealed 3.24 fold improved permeation and skin retention in the case of curcumin loaded NLC gel compared to free curcumin gel. The cell viability studies demonstrated the formulation components showed no toxicity towards keratinocyte cells. In keratinocyte cells, improved cell uptake was observed for curcumin-NLC compared to free curcumin dispersion. The results suggested that the NLC based formulation had potential to improve the efficacy of curcumin.

摘要

纳米结构脂质载体(NLC)已成为一种很有前景的用于局部给药的药物递送系统。递送亲脂性药物时稳定性和包封效率得到提高,这是基于NLC的制剂最重要的优势之一。本研究的目的是提高难溶性姜黄素渗透到局部皮肤层的能力,以治疗慢性炎症性疾病银屑病和微生物介导的寻常痤疮。采用热乳化后探针超声法制备负载姜黄素的NLC。此外,对设计的NLC进行了体外和离体表征。设计的NLC平均粒径为96.2±0.9nm,包封效率为70.5±1.65%,zeta电位为-15.2±0.566mV。姜黄素-NLC在体外释放长达48小时,而游离姜黄素在4小时内药物释放率为100%。离体皮肤渗透研究表明,与游离姜黄素凝胶相比,负载姜黄素的NLC凝胶的渗透和皮肤滞留提高了3.24倍。细胞活力研究表明制剂成分对角质形成细胞无毒性。在角质形成细胞中,与游离姜黄素分散体相比,姜黄素-NLC的细胞摄取得到改善。结果表明基于NLC的制剂有潜力提高姜黄素的疗效。

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