Preparation and characterisation of esculetin-loaded nanostructured lipid carriers gels for topical treatment of UV-induced psoriasis.

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Pharmaceutical Development and Technology Pub Date : 2024-10-01 DOI:10.1080/10837450.2024.2407854

Rawia M Khalil, Mohamed F Abdelhameed, Sally Abou Taleb, Mohamed A El-Saied, Eman Samy Shalaby

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Abstract

Significance: As an inflammatory and autoimmune skin condition, psoriasis affects 2-3% of people worldwide. Psoriasis requires prolonged treatments with immunosuppressive medications which have severe adverse effects. Esculetin (Esc) is a natural medication that has been utilised to treat psoriasis.

Objective: The goal of this work is to improve Esc's solubility by developing novel Esc nanostructured lipid carriers (NLCs) for treating psoriasis and increasing the residence time on the skin which infers better skin absorption.

Methods: The particle size, zeta potential and entrapment efficiency (EE) of Esc NLCs were assessed. Incorporating NLCs into gum Arabic gel preparation enhances their industrial applicability, absorption and residence time on the skin. Esc NLC gels were evaluated by in vitro release and in vivo effectiveness on a rat model of UV-induced psoriasis.

Results: Esc NLCs showed high EE reaching more than 95% and reasonable particle size ranging between (53.86 ± 0.38 to 236.3 ± 0.11 nm) and were spherical. The release study of Esc NLCs gel demonstrated a fast release of Esc denoting enhanced bioavailability. Compared to free Esc, Esc NLCs gel (F2) could considerably lower the level of CD34 and TNF-α in the skin. The results were validated through histopathological analysis.

Conclusion: As Esc NLCs gel (F2) has strong anti-inflammatory properties, our results showed that it presented a significant potential for healing psoriasis.

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用于局部治疗紫外线诱发的银屑病的埃克替林负载纳米结构脂质载体凝胶的制备和表征。

意义重大：作为一种炎症性和自身免疫性皮肤病，银屑病影响着全球 2%-3% 的人。银屑病需要长期使用免疫抑制药物治疗，但这些药物会产生严重的不良反应。埃斯奎林（Esc）是一种天然药物，已被用于治疗银屑病：这项工作的目的是通过开发新型埃斯可纳米结构脂质载体（NLCs）来提高埃斯可的溶解度，用于治疗银屑病，并增加其在皮肤上的停留时间，从而更好地促进皮肤吸收：方法：评估了＼纳米脂质载体的粒度、ZETA电位和夹带效率（EE）。将 NLCs 加入阿拉伯胶凝胶制剂中可提高其工业适用性、吸收性和在皮肤上的停留时间。在紫外线诱发的银屑病大鼠模型上，通过体外释放和体内有效性对 Esc NLCs 凝胶进行了评估：结果：＼NLCs的EE值高达95%以上，粒径在（53.86 ± 0.38至236.3 ± 0.11nm）之间，呈球形。＼NLCs凝胶的释放研究表明，＼的释放速度快，生物利用度提高。与游离＼相比，＼NLCs凝胶（F2）能显著降低皮肤中CD34和TNF-α的水平。组织病理学分析验证了这一结果：由于＼NLCs凝胶（F2）具有很强的抗炎特性，我们的研究结果表明它在治疗银屑病方面具有很大的潜力。

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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来源期刊

Pharmaceutical Development and Technology 医学-药学

CiteScore

5.90

自引率

2.90%

发文量

审稿时长

1 months

期刊介绍： Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.