四氢香豆素超变形纳米胶囊乳膏的配方、优化及抗氧化性能评价

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2022-12-17 DOI:10.1007/s12247-022-09696-0
Ankita Kanshide, Malleswara Rao Peram, Nagesh Chandrasekhar, Arzoo Jamadar, Vijay Kumbar, Manohar Kugaji
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引用次数: 1

摘要

目的四氢姜黄素(THC)具有出色的抗炎和抗氧化特性,但其较差的水溶性限制了它在药物和化妆品配方中的应用。本研究旨在开发、优化和表征一种纳米囊状乳膏负载的四氢姜黄素转移体(THC-TFs),以改善其局部给药效果并增强其抗氧化活性。方法采用薄膜水合技术制备四氢姜黄素转移体,并对囊泡大小、ZETA电位、夹带效率和皮肤渗透性进行表征。结果优化后的四氢大麻酚-TF(OPT-THC-TF)悬浮液的囊泡大小为 212 ± 4.78 nm,zeta 电位为 -40.3 mV,夹带效率为 83.74 ± 0.21。荧光显微镜显示,转移体渗透到了皮肤深层。体内皮肤渗透试验表明,与传统的 THC 乳霜相比,OPT-THC-TF 乳霜具有更好的皮肤渗透和沉积潜力。α,α-二苯基-β-苦基肼(DPPH)自由基清除活性测定显示,THC-TF 乳霜的抗氧化潜力(77%)与纯 THC 的抗氧化潜力(81%)相当,这表明 THC 的抗氧化活性不受其封装成转移体的影响。细胞活力研究表明,与纯 THC 溶液相比,THC-TF 乳霜(***p < 0.001)明显降低了对正常细胞(L-929)的细胞毒性。
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Formulation, Optimization, and Antioxidant Evaluation of Tetrahydrocurcumin-Loaded Ultradeformable Nanovesicular Cream

Purpose

Tetrahydrocurcumin (THC) has excellent anti-inflammatory and antioxidant properties, but its poor aqueous solubility limits its use in pharmaceutical and cosmetic formulations. The present study aimed to develop, optimize, and characterize a nanovesicular cream-loaded tetrahydrocurcumin transfersomes (THC-TFs) to improve its topical delivery and enhance its antioxidant activity.

Methodology

THC-TFs were prepared using the thin-film hydration technique and characterized for vesicle size, zeta potential, entrapment efficiency, and skin penetration. The optimized transfersomal formulation was incorporated into a cream base and characterized for various parameters.

Results

The optimized THC-TF (OPT-THC-TF) suspension showed a vesicle size of 212 ± 4.78 nm, a zeta potential of –40.3 mV, and percentage entrapment efficiency of 83.74 ± 0.21. Fluorescence microscopy revealed that transfersomes penetrated the deeper layers of skin. Ex vivo skin permeation demonstrated that OPT-THC-TF cream has better skin permeation and deposition potential compared to the THC conventional cream. The α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activity assay revealed that the antioxidant potential of THC-TF cream (77%) was comparable to that of pure THC (81%), demonstrating that THC antioxidant activity is unaffected by its encapsulation into transfersomes. The cell viability study revealed that THC-TF cream (***p < 0.001) significantly decreased the cytotoxicity toward normal cells (L-929) compared to pure THC solution.

Conclusion

Based on these findings, it was concluded that the OPT-THC-TF cream could be a promising strategy for the topical delivery of encapsulated drugs for the effective treatment of various dermatological disorders.

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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