研究动态
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复方药房出售用于治疗婴儿血管瘤的脂质体普萘洛尔。

Liposomal propranolol for treatment of infantile hemangioma at compounding pharmacies.

发表日期:2024 Feb 09
作者: Antigone Nifli, Aggeliki Liakopoulou, Elena Mourelatou, Konstantinos Avgoustakis, Sophia Hatziantoniou
来源: JOURNAL OF LIPOSOME RESEARCH

摘要:

婴儿血管瘤(IH)是常见的良性软组织肿瘤,经常影响婴儿。虽然盐酸普萘洛尔 (Pro HCl) 已成为 IH 的一种有前途的治疗方法,但由于需要稳定有效的载体,其局部应用仍然具有挑战性。本研究探讨了预配制脂质体作为局部递送 Pro HCl 的载体以治疗复合药房 IH 的潜力。使用活性药物成分或市售普萘洛尔片剂和各种稀释介质(包括注射用水 (WFI)、葡萄糖 5% 和 NaCl 0.9%)制备负载 Pro HCl 的脂质体。脂质体制剂的理化性质(Pro HCl 含量、包封效率、负载能力和胶体稳定性)在 4°C 下储存 90 天进行评估。还评估了脂质体中 Pro HCl 的体外释放动力学和透皮渗透。脂质体性质受稀释介质的影响。无论稀释介质如何,封装 API 的脂质体 (Lipo-Pro) 中的 Pro HCl 含量保持稳定。 Lipo-Pro 显示出随着时间的推移持续的药物释放,表明其维持治疗水平的潜力。与水溶液相比,Pro HCl 表现出 Lipo-Pro 增强的透皮渗透性,表明其用于局部 IH 治疗的潜力。预配制的脂质体为 Pro HCl 提供了稳定有效的载体,可能适用于复合药房的临时制剂。它们增强的透皮渗透性为局部 IH 治疗提供了一种有前景的替代方案。这项研究为开发用于管理 IH 的创新且有效的药物输送策略提供了宝贵的见解,未来的研究重点是体内应用和治疗潜力。
Infantile hemangiomas (IH) are common benign soft tissue tumors, frequently affecting infants. While Propranolol Hydrochloride (Pro HCl) has emerged as a promising treatment for IH, its topical application remains challenging due to the need for stable and efficacious carriers. This study investigates the potential of preformulated liposomes as carriers for topical delivery of Pro HCl for the treatment of IH in compounding pharmacies. Liposomes loaded with Pro HCl were prepared using active pharmaceutical ingredient or commercially available propranolol tablets and various dilution media, including Water for Injection (WFI), Dextrose 5%, and NaCl 0.9%. The physicochemical properties of the liposomal formulations (Pro HCl content, encapsulation efficiency, loading capacity, and colloidal stability) were assessed over a 90-day storage at 4 °C. In vitro release kinetics and transdermal permeation of Pro HCl from liposomes were also evaluated. Liposome properties were influenced by the dilution medium. Pro HCl content remained stable in liposomes encapsulating API (Lipo-Pro), regardless of the dilution medium. Lipo-Pro showed sustained drug release over time, suggesting its potential for maintaining therapeutic levels. Pro HCl exhibited enhanced transdermal permeability from Lipo-Pro compared to aqueous solution, indicating its potential for topical IH treatment. Preformulated liposomes offer a stable and effective carrier for Pro HCl, potentially suitable for extemporaneous preparations in compounding pharmacies. Their enhanced transdermal permeability presents a promising alternative for topical IH treatment. This study provides valuable insights into the development of innovative and effective drug delivery strategies for managing IH, with future research focusing on in vivo applications and therapeutic potential.