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柚皮苷载药前体脂质体凝胶的制备及促伤口愈合研究。

Design and development of naringin-loaded proposomal gel for wound healing.

机构信息

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India.

Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India.

出版信息

J Cosmet Dermatol. 2022 Oct;21(10):5187-5202. doi: 10.1111/jocd.15029. Epub 2022 May 16.

DOI:10.1111/jocd.15029
PMID:35486446
Abstract

BACKGROUND

The injuries or wounds caused by various means will impact human lives severely. An increase in the demand for wounds or burns was observed. For better wound healing and to combat the free radical effect on the healing process, wounds must be treated with multifunctional or multipurpose dressing or gel or any other type of biomaterial.

OBJECTIVES

The study aimed to develop, optimize, and evaluate the naringin-loaded proposomal gel (PPG) for quick wound healing.

METHODS

The central composite design was employed for the optimization of proposomes. Naringin-loaded proposomes were evaluated for percentage entrapment efficiency (EE), the particle size of proposomes (PsP), and the zeta potential of proposomes (ZpP). The change in drug release profile was studied by dissolution. Furthermore, naringin and naringin-loaded proposomes, antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH) reagent and ascorbic acid as a reference standard. Different gel bases were prepared, and based on various parameters, the G2 (0.6% Carbopol 974) gel base was selected for naringin proposomes loading. The naringin-loaded PPG was evaluated for various in vitro and in vivo wound-healing properties.

RESULTS

The optimized naringin-loaded proposomes showed extended drug release (90.78 ± 2.19%) for 72 h. The naringin-loaded PPG improved the permeability of naringin, which showed 28.91 ± 2.81% of drug release after 96 h, and the drug solution showed 9.05 ± 0.92%. IC50 values of antioxidant activity of naringin and naringin proposomes were found to be 337.31 μg/ml and 201.86 μg/ml, respectively. The naringin-loaded PPG showed better wound closure on the 15th day (3.32%) compared with proposomal solution (4.75%) or naringin topical gel (4.2%).

CONCLUSION

Based on the obtained results, we conclude naringin-loaded PPG can be an alternative strategic approach to deliver the naringin for quick wound healing.

摘要

背景

各种原因造成的损伤或创伤会严重影响人类的生命。观察到对伤口或烧伤的需求增加。为了更好地促进伤口愈合,并对抗愈合过程中的自由基影响,必须使用多功能或多用途敷料或凝胶或任何其他类型的生物材料对伤口进行治疗。

目的

本研究旨在开发、优化并评价载柚皮苷前体脂质体凝胶(PPG)以促进伤口快速愈合。

方法

采用中心复合设计对前体脂质体进行优化。评价载柚皮苷前体脂质体的包封率(EE)、前体脂质体的粒径(PsP)和前体脂质体的zeta 电位(ZpP)。通过溶出度研究药物释放曲线的变化。此外,通过 2,2-二苯基-1-苦基肼水合物(DPPH)试剂和抗坏血酸作为参比标准,测定柚皮苷和载柚皮苷前体脂质体的抗氧化活性。制备了不同的凝胶基质,并根据各种参数,选择 0.6%卡波姆 974(Carbopol 974)凝胶基质用于载柚皮苷前体脂质体的加载。对载柚皮苷 PPG 进行了各种体外和体内伤口愈合性能评价。

结果

优化的载柚皮苷前体脂质体显示出延长的药物释放(90.78±2.19%),持续 72 h。载柚皮苷 PPG 提高了柚皮苷的通透性,96 h 后显示 28.91±2.81%的药物释放,而药物溶液显示 9.05±0.92%。柚皮苷和载柚皮苷前体脂质体的抗氧化活性 IC50 值分别为 337.31μg/ml 和 201.86μg/ml。载柚皮苷 PPG 在第 15 天(3.32%)的伤口闭合率优于前体脂质体溶液(4.75%)或柚皮苷局部凝胶(4.2%)。

结论

根据所得结果,我们得出结论,载柚皮苷 PPG 可以作为一种替代策略,用于快速促进伤口愈合的柚皮苷传递。

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