Enhanced therapy for diabetic neuropathy utilizing venlafaxine hydrochloride-loaded transferosome-based transdermal gel

Kajol Patil , Pramod S. Salve , Ujban Md Hussain Hussain , Amol Tatode , Mohammad Qutub
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Abstract

Diabetic neuropathy (DN), a prevalent and debilitating complication of diabetes mellitus, significantly impairs the quality of life. Venlafaxine hydrochloride (VXH), a serotonin-norepinephrine reuptake inhibitor, offers potential for DN management but suffers from poor oral bioavailability and systemic side effects. This study aimed to develop and evaluate a VXH-loaded transferosome-based transdermal gel to address these limitations. Transferosomes, ultra-deformable vesicles, were optimized using response surface methodology to achieve an entrapment efficiency of 92.64 % and vesicle size of 165.8 nm. Comprehensive characterization confirmed high stability, enhanced drug release (87.66 % in 24 h), and superior permeation profiles. Pharmacokinetic studies demonstrated prolonged drug retention and improved bioavailability compared to conventional formulations. Pharmacodynamic evaluations in diabetic neuropathy models revealed significant alleviation of neuropathic pain, supported by histopathological evidence of nerve integrity restoration. These findings underscore the potential of VXH-loaded transferosome gels as a non-invasive, patient-friendly alternative for DN management, offering enhanced therapeutic outcomes with reduced systemic exposure. Clinical translation of this innovative delivery system could revolutionize DN therapy.

Abstract Image

利用盐酸文拉法辛负载转移体透皮凝胶增强糖尿病神经病变的治疗
糖尿病性神经病变(DN)是一种常见的糖尿病并发症,严重影响生活质量。盐酸文拉法辛(vvxh)是一种血清素-去甲肾上腺素再摄取抑制剂,具有治疗DN的潜力,但口服生物利用度差且有全身副作用。本研究旨在开发和评估一种负载vxh的基于转移体的透皮凝胶来解决这些局限性。利用响应面法对超变形囊泡Transferosomes进行了优化,其包封效率为92.64%,囊泡大小为165.8 nm。综合表征证实了高稳定性,增强药物释放(24 h内87.66%)和优越的渗透谱。药代动力学研究表明,与传统配方相比,延长了药物保留时间,提高了生物利用度。糖尿病神经病变模型的药效学评估显示神经性疼痛明显减轻,神经完整性恢复的组织病理学证据支持。这些发现强调了装载vvxh的转移体凝胶作为一种非侵入性、对患者友好的DN治疗替代方案的潜力,在减少全身暴露的情况下提供了增强的治疗结果。这种创新的给药系统的临床翻译可能会彻底改变DN治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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