Purpose

An attempt was made to formulate carvedilol-loaded cubosome (cubogel) to accelerate the wound healing activity. The combined effect of a natural healing agent, Moringa oleifera Lam. leaf extract and cubosomes was also studied.

Methods

Cubosomes were prepared by emulsification method. A 3² factorial design was applied to optimize independent variables: glycerol monooleate and Lutrol F127 and response variables mainly, particle size, entrapment efficiency, and drug release. Optimized formulation was incorporated in the gel base to get cubogel and was characterized for pH, drug content, and viscosity.

Results

Cubosomal formulations were of small particle size (249.2 ± 2.2 nm), exhibited high entrapment efficiency (37.1 ± 1.01%) and effectively delayed drug release (85.02 ± 0.91% within 24 h), hence was selected as optimized formulation. Cubic-shaped cubosomes were confirmed by transmission electron microcopy, having zeta potential − 29.05 mV. Cubosomes were incorporated into Carbopol 934 base (1%) to get cubogel. Texture analyzer demonstrated less spreadability due to viscous nature of cubogel. Diffusion study revealed slow diffusion of drug through the cubosomes. In vivo study was performed in rats using excision wound model; it showed rapid initiation of wound healing on day 3, closing above 94% on day 7 and scar formation on day 10, for both cubogel and cubogel with Moringa oleifera leaf extract.

Conclusion

Carvedilol-loaded cubogel in combination with Moringa oleifera leaf extract can be considered as an excellent formulation to accelerate the wound healing potential.

中文翻译：

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负载卡维地洛的立方体凝胶可加速伤口愈合

目的

尝试配制负载卡维地洛的立方体（cubogel）以加速伤口愈合活性。天然愈合剂辣木的综合作用。还研究了叶提取物和立方体。

方法

采用乳化法制备立方体。应用3× ²因子设计来优化自变量：单油酸甘油酯和 Lutrol F127 以及主要响应变量：粒径、包封效率和药物释放。将优化的配方纳入凝胶基质中以获得立方凝胶，并对其 pH、药物含量和粘度进行表征。

结果

立方体制剂粒径小（249.2±2.2 nm），具有较高的包封率（37.1±1.01%）和有效延迟药物释放（24 h内85.02±0.91%），因此被选为优化制剂。通过透射电子显微镜证实立方体形状，具有 zeta 电位 - 29.05 mV。将 Cubosomes 掺入 Carbopol 934 基质 (1%) 中得到 cubogel。由于立方体凝胶的粘性，质地分析仪显示出较差的铺展性。扩散研究揭示了药物通过立方体的缓慢扩散。使用切除伤口模型在大鼠中进行体内研究；对于 cubogel 和含有辣木叶提取物的 cubogel，其结果表明，伤口在第 3 天开始快速愈合，第 7 天闭合超过 94%，第 10 天形成疤痕。

结论

载有卡维地洛的立方凝胶与辣木叶提取物相结合可被认为是加速伤口愈合潜力的绝佳配方。