Prakash Dev, Chaudhary Anjali, Chaudhary Amit
School of Pharmacy, Abhilashi University, Mandi, Himachal Pradesh, India.
School of Pharmacy, Chitkara University, Baddi, Himachal Pradesh.
Curr Drug Deliv. 2024 Oct 2. doi: 10.2174/0115672018329544240922151617.
Psoriasis is a chronic inflammatory skin disorder that poses significant challenges regarding effective and targeted drug delivery. Bioactive substances like betulin have shown tremendous utility in treating these conditions; however, they pose limited utility owing to their physicochemical characteristics. Here, we aimed to develop a novel topical dosage form for treating psoriasis, utilising betulin-loaded solid lipid nanoparticles (NLCs) incorporated into a hydrogel matrix.
The optimization of the formulation was meticulously conducted using a design of experiments methodology, and its diverse physicochemical attributes were thoroughly examined. Evaluating betulin's in vitro release pattern from the NLC-hydrogel demonstrated consistent and regulated drug release properties. Additionally, the formulation demonstrated improved skin penetration abilities as determined by in vitro skin permeation experiments employing Franz diffusion cells- furthermore, the therapeutic effectiveness of the betulin-NLC-hydrogel was assessed by an in vivo experiment carried out using an imiquimod-induced psoriasis-like skin inflammation model in BALB/c female mice.
The NLCs exhibited a pH of 5.67±0.86, particle size of 148.16±12.66 nm, and zeta potential of -22.84±2.37 mV, ensuring stability and suitability for topical use. The gel, with a pH of 6.05±0.43 and viscosity of 17550±120 cPs, showed enhanced skin hydration and lipid restoration. Drug release studies indicated a slower release from NLCs and gel, improving skin retention. Stability tests revealed that the formulations were stable at room temperature but not at elevated temperatures. The in vitro safety profile of the formulation revealed no significant adverse effects on HaCaT cell lines. The NLC gel demonstrated significant anti-psoriatic activity, reducing inflammation and cytokine levels.
The betulin-NLC-hydrogel formulation exhibited promising characteristics for the topical treatment of psoriasis, showcasing optimised drug delivery, sustained release, and notable therapeutic efficacy. The findings from this study provide a foundation for the potential clinical translation of this innovative topical dosage form for improved psoriasis management.
银屑病是一种慢性炎症性皮肤病，在有效和靶向给药方面面临重大挑战。桦木醇等生物活性物质在治疗这些病症方面已显示出巨大效用；然而，由于其物理化学特性，其效用有限。在此，我们旨在开发一种用于治疗银屑病的新型局部剂型，利用负载桦木醇的固体脂质纳米粒（NLCs）并入水凝胶基质中。
使用实验设计方法精心进行制剂的优化，并对其各种物理化学属性进行全面检查。评估桦木醇从NLC-水凝胶中的体外释放模式，显示出一致且可控的药物释放特性。此外，通过使用Franz扩散池的体外皮肤渗透实验确定，该制剂显示出改善的皮肤渗透能力；此外，通过在BALB/c雌性小鼠中使用咪喹莫特诱导的银屑病样皮肤炎症模型进行的体内实验评估了桦木醇-NLC-水凝胶的治疗效果。
NLCs的pH值为5.67±0.86，粒径为148.16±12.66 nm，zeta电位为-22.84±2.37 mV，确保了稳定性和局部使用的适用性。该凝胶的pH值为6.05±0.43，粘度为17550±120 cPs，显示出增强的皮肤水合作用和脂质恢复。药物释放研究表明，从NLCs和凝胶中释放较慢，改善了皮肤滞留。稳定性测试表明，制剂在室温下稳定，但在高温下不稳定。该制剂的体外安全性表明对HaCaT细胞系无明显不良影响。NLC凝胶显示出显著的抗银屑病活性，降低了炎症和细胞因子水平。
桦木醇-NLC-水凝胶制剂在银屑病局部治疗方面表现出有前景的特性，展示了优化的药物递送、持续释放和显著的治疗效果。本研究结果为这种创新的局部剂型用于改善银屑病管理的潜在临床转化提供了基础。
