Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
School of Life and Medical Sciences, University of Hertfordshire Hosted By Global Academic Foundation, New Administrative Capital, Cairo, Egypt.
Daru. 2024 Dec;32(2):705-714. doi: 10.1007/s40199-024-00541-y. Epub 2024 Oct 8.
Over the past decades, a substantial portion of the population worldwide has been infected with varicella zoster and most cases developed shingles. Unfortunately, shingles is usually accompanied by postherpetic neuralgia, which may persist for months to years after the resolution of the viral infection.
Gabapentin is an orally gamma-aminobutyric acid analogue approved by the Food and Drug Administration to manage shingles postherpetic neuralgia. However, gabapentin shows nonlinear pharmacokinetics, with variable absorption and bioavailability along with its short half-life and long side effects that may include dizziness and somnolence, which calls for an appropriate topical dosage form. Bigels are unique semisolid dosage forms with boosted penetrability and satisfactory hydrophilic texture.
The current work pointed to formulating gabapentin-loaded bigels for the treatment of postherpetic neuralgia, where the analysis and optimization of design were performed via Design-Expert®.
The selected bigel (F5), incorporating 400 mg Span 60, 1000 mg Tween 80, and 1000 mg Transcutol, displayed spherical nanosized particles with acceptable viscosity and spreadability. Subsequent topical application of the selected bigel on the skin of Wistar rats, F5, demonstrated a boosted accumulation of gabapentin in the skin similar to PLO gel but superior to the drug solution. Furthermore, a histopathological study demonstrated the biosafety of the selected bigel when applied topically. Accordingly, gabapentin-loaded bigel would be considered a potentially topical dosage form for the delivery of gabapentin for the management of postherpetic neuralgia.
在过去的几十年中，世界上很大一部分人口感染了水痘带状疱疹病毒，大多数病例发展为带状疱疹。不幸的是，带状疱疹通常伴有带状疱疹后神经痛，这种疼痛可能在病毒感染消退后持续数月至数年。
加巴喷丁是一种口服γ-氨基丁酸类似物，已被美国食品和药物管理局批准用于治疗带状疱疹后神经痛。然而，加巴喷丁表现出非线性药代动力学特征，其吸收和生物利用度存在变异性，半衰期短，副作用长，可能包括头晕和嗜睡，这需要一种合适的局部剂型。巴布剂是一种独特的半固体制剂，具有增强的渗透性和令人满意的亲水性质地。
目前的工作旨在开发用于治疗带状疱疹后神经痛的加巴喷丁负载巴布剂，通过 Design-Expert® 对设计进行分析和优化。
所选的巴布剂（F5），包含 400mg Span 60、1000mg Tween 80 和 1000mg Transcutol，显示出具有可接受的粘度和铺展性的球形纳米颗粒。随后将选定的巴布剂（F5）局部应用于 Wistar 大鼠的皮肤，结果表明加巴喷丁在皮肤中的蓄积量增加，类似于 PLO 凝胶，但优于药物溶液。此外，组织病理学研究表明，局部应用选定的巴布剂具有生物安全性。因此，加巴喷丁负载的巴布剂可以被认为是一种潜在的局部剂型，用于递送加巴喷丁治疗带状疱疹后神经痛。
