Bhattacharyya Sayani, Lakshmanan Kalai Tamilselvi, Muthukumar Andhuvan
Krupanidhi College of Pharmacy, Department Of Pharmaceutics, Bengaluru, India.
Al Ameen College of Pharmacy, Department of Pharmacology, Bengaluru, India.
Turk J Pharm Sci. 2024 Sep 2;21(4):303-312. doi: 10.4274/tjps.galenos.2023.46735.
Famciclovir, the drug of choice for cold sores and recurrent genital herpes, has poor oral bioavailability and is associated with numerous side effects. The study aimed to explore the possibility of transdermal application of famciclovir through a transferosome-loaded gelling system to localize the drug at the site of application with improved penetrability, therapeutic effects, and comfort.
Transferosomes of famciclovir were prepared using tween 80, phospholipid, and cholesterol. To optimize drug entrapment and the vesicular size of the transferosomes, a central composite design was employed. The optimized formulation was evaluated for physicochemical characteristics, surface morphology, and degree of deformability. The optimized product was included in the Carbopol 940 gelling system. The gel was evaluated for ex vivo permeation, skin irritation, drug deposition at various skin layers, and histopathological analysis.
The design optimization yielded an optimized product (FAMOPT) of nanosized (339 nm) stable vesicles of the transferosome of famciclovir. The surface morphology analysis revealed the formation of nanovesicles without aggregation. Compatibility between the drug and excipients was established. The elasticity of the vesicles demonstrated resistance to leakage. The permeation of the drug was enhanced by 2.8 times. The gel was found to be non-irritating and non-sensitizing to the animal skin. The drug deposition at various skin layers was remarkably improved, indicating effective drug penetration. The histopathological examination further demonstrated the penetration of nano-vesiculate drugs through deeper layers of the skin.
Hence, nano-vesicular famciclovir delivery is a promising alternative to conventional famciclovir delivery with enhanced local and systemic action for herpes treatment.
泛昔洛韦是治疗唇疱疹和复发性生殖器疱疹的首选药物，但其口服生物利用度差，且伴有多种副作用。本研究旨在探索通过载有传递体的凝胶系统经皮应用泛昔洛韦的可能性，以使药物在应用部位定位，同时提高其渗透性、治疗效果和舒适度。
使用吐温80、磷脂和胆固醇制备泛昔洛韦传递体。为优化药物包封率和传递体的囊泡大小，采用了中心复合设计。对优化后的制剂进行了物理化学特性、表面形态和变形程度评估。将优化后的产品加入卡波姆940凝胶系统中。对该凝胶进行了体外渗透、皮肤刺激性、药物在不同皮肤层的沉积以及组织病理学分析。
设计优化得到了一种优化产品（FAMOPT），即纳米尺寸（339 nm）的泛昔洛韦传递体稳定囊泡。表面形态分析显示形成了无聚集的纳米囊泡。确定了药物与辅料之间的相容性。囊泡的弹性表明其具有抗渗漏性。药物渗透性提高了2.8倍。发现该凝胶对动物皮肤无刺激性和致敏性。药物在不同皮肤层的沉积显著改善，表明药物有效渗透。组织病理学检查进一步证明了纳米囊泡药物可穿透皮肤深层。
因此，纳米囊泡递送泛昔洛韦是一种有前景的替代传统泛昔洛韦递送的方法，在疱疹治疗中具有增强的局部和全身作用。
