普萘洛尔纳米凝胶:用于潜在局部血管瘤治疗的制备、体外和体内特性分析

Taif Abdullah, Khalid Al-Kinani
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引用次数: 0

摘要

口服盐酸普萘洛尔(PHCl)缺乏安全有效的局部替代药物,这阻碍了婴儿血管瘤(IH)的最佳治疗,尤其是在副作用严重或治疗失败的复杂病例中。本研究旨在开发一种用于局部注射盐酸普萘洛尔的纳米乳液凝胶(NEG)。由丁香油、吐温 20 和聚乙二醇 400 精心配制的纳米乳液(NE)因其卓越的稳定性、回弹性和良好的载药量而成为最佳候选物质(NE3)。NE3 具有 14.57 nm 的显著球形尺寸、0.282 的低多分散指数(PDI)和 -19.89 mV 的稳定 zeta 电位。随后配制的 PHCl-NEG 具有理想的流变性和铺展性,适合局部应用。体内皮肤保留和渗透研究表明,PHCl 能有效地沉积在真皮层内,而全身暴露极少。这种前景广阔的方法为口服 PHCl 提供了潜在的替代方案,有可能减轻严重的副作用,改善复杂 IH 病例的治疗效果。
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Propranolol nanoemulgel: Preparation, in-vitro and ex-vivo characterization for a potential local hemangioma therapy
A lack of safe and effective topical alternatives to oral propranolol HCl (PHCl) hampers optimal management of infantile hemangioma (IH), particularly in complex cases with severe side effects or treatment failures. This study aimed to develop a nanoemulsion gel (NEG) for topical PHCl delivery. A meticulously formulated nanoemulsion (NE) encapsulated with clove oil, Tween 20, and polyethylene glycol 400 emerged as the standout candidate (NE3) due to its exceptional stability, resilience, and favorable drug loading. NE3 exhibited a remarkable globule size of 14.57 nm, a low polydispersity index (PDI) of 0.282, and a stabilizing zeta potential of −19.89 mV. The subsequent formulation of PHCl-NEG displayed desired rheological and spreadability properties for topical application. Ex-vivo skin retention and permeation studies revealed effective PHCl deposition within the dermal layer with minimal systemic exposure. This promising approach offers a potential alternative to oral PHCl, potentially mitigating severe side effects and improving outcomes in complex IH cases.
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