Formulation characterization of lecithin organogel as topical drug delivery system for psoriasis: In-vitro permeation and preclinical evaluation

IF 3.5 4区 医学 Q2 CHEMISTRY, MEDICINAL Drug Development Research Pub Date : 2024-04-29 DOI:10.1002/ddr.22191
Prajakta Bule, Prashant Kadkanje, Ravikiran Kshirsagar, Eswara Rao Puppala, Vegi Ganga Modi Naidu, Naveen Chella
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Abstract

Psoriasis is a chronic inflammatory and proliferative skin disease that causes pathological skin changes and has a substantial impact on the quality of patient life. Apremilast was approved by the US Food and Drug Administration as an oral medication for psoriasis and is beneficial in mild to moderate conditions for chronic usage. However, 5%–7% of withdrawals were reported due to severe side effects. To address the issue, a localized drug delivery strategy via the topical route may be a viable approach. However, poor physicochemical properties make it vulnerable to passing through the skin, requiring a specialized drug delivery system to demonstrate its full potential via a topical route like lecithin organogel. The formulation was optimized by screening the suitable lecithin type and non-polar solvents based on the gel formation ability of lecithin and the solubility of apremilast in the solvent. The pseudo-ternary diagram was used to optimize the water content required to form the gel. The optimized gel was found to be shear thinning characterized for rheological parameters, in-vitro diffusion studies, and in-vitro skin distribution studies. Preclinical studies in Imiquimod-induced mice showed a better reduction in severity index, cytokine levels, and epidermal hyperplasia from the lecithin organogel group compared to the apremilast oral administration and marketed standard topical gel group. Based on these results, lecithin organogel can be considered a promising approach to deliver molecules like apremilast by topical route in psoriatic-like conditions.

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卵磷脂有机凝胶作为银屑病局部给药系统的配方特征:体外渗透和临床前评估
银屑病是一种慢性炎症性和增生性皮肤病,会引起皮肤病理变化,对患者的生活质量有很大影响。美国食品和药物管理局批准阿普司特为治疗银屑病的口服药物,长期服用对轻度至中度银屑病患者有益。然而,据报道,5%-7%的患者因严重副作用而停药。为了解决这一问题,通过局部途径进行局部给药可能是一种可行的方法。然而,卵磷脂的理化性质较差,容易透过皮肤,因此需要一种专门的给药系统,才能像卵磷脂有机凝胶一样通过局部途径充分展示其潜力。根据卵磷脂的凝胶形成能力和阿普瑞司特在溶剂中的溶解度,通过筛选合适的卵磷脂类型和非极性溶剂,对配方进行了优化。利用假三元图优化形成凝胶所需的水含量。通过流变学参数、体外扩散研究和体外皮肤分布研究发现,优化后的凝胶具有剪切稀化特性。对咪喹莫特诱导的小鼠进行的临床前研究表明,与阿普司特口服给药组和市场上销售的标准外用凝胶组相比,卵磷脂有机凝胶组能更好地降低严重指数、细胞因子水平和表皮增生。基于这些结果,卵磷脂有机凝胶被认为是一种很有前景的方法,可以通过局部途径将阿普瑞司特等分子递送到类似银屑病的病症中。
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来源期刊
CiteScore
6.40
自引率
2.60%
发文量
104
审稿时长
6-12 weeks
期刊介绍: Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.
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