El-Refaie Wessam M, Elnaggar Yosra S R, El-Massik Magda A, Abdallah Ossama Y
Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Egypt.
Int J Pharm. 2015;486(1-2):88-98. doi: 10.1016/j.ijpharm.2015.03.052. Epub 2015 Mar 27.
Despite its effectiveness, curcumin (Curc) dermal delivery is handicapped by hydrophobicity, high metabolism and poor skin permeation. In this work, the potential of novel self-assembled nanogels, namely gel-core hyaluosome (GC-HS) to enhance Curc delivery to wound sites, enhance healing rate and decrease scar formation was evaluated. Curc-GC-HS were prepared using film hydration technique and evaluated regarding size, zeta potential (ZP), entrapment efficiency (% EE), and in vitro release. Structure elucidation was performed using light, polarizing and transmission electron microscopy (TEM). In-vivo burn-wound healing potential, skin deposition ability and histological study were evaluated using female Sprague Dawley rats. Curc-GC-HS were compared to conventional transfersomal gel (Curc-T-Pl gel), and other conventional gels. Curc-GC-HS showed nanosize (202.7 ± 0.66 nm), negative ZP (-33 ± 2.6 mV) and % EE (96.44 ± 1.29%). TEM revealed discrete vesicles with characteristic bilayer structure. Polarizing microscopy proposed liquid crystalline consistency. Burn-wound healing study showed that Curc-GC-HS was the only system exhibiting marked improvement at day 7 of treatment. At 11th day, Curc-GC-HS treated wounds showed almost normal skin with no scar confirmed by histological analysis. Curc-GC-HS showed five folds higher skin deposition compared to conventional Curc-T-Pl gel. To conclude, novel gel-core hyaluosomes elaborated are promising nanogels able to increase Curc skin penetration and dermal localization while protecting it against degradation. Future perspective encompasses assessing potential of novel nanocarrier for skin cancer therapy.
尽管姜黄素(Curc)具有有效性,但其经皮给药受到疏水性、高代谢率和皮肤渗透性差的限制。在本研究中,评估了新型自组装纳米凝胶,即凝胶核透明质体(GC-HS)增强姜黄素向伤口部位递送、提高愈合率和减少瘢痕形成的潜力。采用薄膜水化技术制备了Curc-GC-HS,并对其粒径、zeta电位(ZP)、包封率(%EE)和体外释放进行了评估。使用光学显微镜、偏光显微镜和透射电子显微镜(TEM)进行结构解析。使用雌性Sprague Dawley大鼠评估体内烧伤创面愈合潜力、皮肤沉积能力和组织学研究。将Curc-GC-HS与传统传递体凝胶(Curc-T-Pl凝胶)和其他传统凝胶进行比较。Curc-GC-HS呈现纳米尺寸(202.7±0.66nm)、负ZP(-33±2.6mV)和%EE(96.44±1.29%)。TEM显示具有特征性双层结构的离散囊泡。偏光显微镜显示为液晶状态。烧伤创面愈合研究表明,Curc-GC-HS是唯一在治疗第7天表现出显著改善的体系。在第11天,经Curc-GC-HS处理的伤口显示几乎正常的皮肤,组织学分析证实无瘢痕形成。与传统的Curc-T-Pl凝胶相比,Curc-GC-HS的皮肤沉积量高出五倍。总之,所制备的新型凝胶核透明质体是有前景的纳米凝胶,能够增加姜黄素的皮肤渗透和真皮定位,同时保护其不被降解。未来的展望包括评估新型纳米载体用于皮肤癌治疗的潜力。