Lipid Nanocarriers of Naringin Dispersed Gel for Topical Application: Development, In Vitro, Ex Vivo, and In Vivo Kinetics Evaluations

IF 3.2 4区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Biopolymers Pub Date : 2025-07-08 DOI:10.1002/bip.70039

Meghanath Shete, Krantee Chavan, Swati Raysing, Ansari Imtiyaz Ejaz

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Abstract

Nanostructured lipid carriers (NLCs) have emerged as promising systems for topical drug delivery due to their enhanced stability and high entrapment efficiency for lipophilic compounds. This study aimed to improve the topical skin permeation of poorly water-soluble Naringin (Nrg) for the treatment of diabetes mellitus (DM) using an NLC-based gel. Nrg-loaded NLCs were prepared via a microemulsion technique followed by homogenization and optimized using a Box–Behnken design. The optimized Nrg-loaded NLCs exhibited a particle size of 212.1 ± 1.8 nm, zeta potential of −23.6 ± 2.8 mV, and entrapment efficiency of 77.47% ± 4.3%. Further, XRD, DSC, and TEM analyses confirmed the crystalline state and nanoscale structure. In vitro release studies revealed a biphasic sustained release profile. The optimized Nrg-NLCs were incorporated into a Carbopol 940 (Cp) gel, which showed 2.36-fold higher skin permeation compared with plain Nrg-Cp gel. In vivo pharmacokinetic studies demonstrated a 1.56-fold increase in bioavailability versus oral Nrg suspension. No skin irritation was observed in animal models. These findings suggest that Nrg-NLC-Cp gel offers a non-invasive and effective alternative for topical delivery of Nrg with improved permeation and systemic availability that can potentially enhance therapeutic outcomes and patient compliance in DM management.

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局部应用的柚皮苷分散凝胶的脂质纳米载体：开发，体外，离体和体内动力学评估

纳米结构脂质载体（nlc）由于其增强的稳定性和对亲脂性化合物的高包裹效率而成为局部药物递送的有前途的系统。本研究旨在改善低水溶性柚皮苷（Nrg）治疗糖尿病（DM）的局部皮肤渗透。负载nrg的NLCs通过微乳液技术制备，然后进行均质，并采用Box-Behnken设计优化。优化后的nrg负载NLCs粒径为212.1±1.8 nm， zeta电位为- 23.6±2.8 mV，包封效率为77.47%±4.3%。XRD、DSC和TEM分析进一步证实了材料的晶体状态和纳米级结构。体外释放研究显示双相缓释谱。将优化后的Nrg-NLCs掺入Carbopol 940 （Cp）凝胶中，其皮肤透性比普通Nrg-Cp凝胶高2.36倍。体内药代动力学研究表明，与口服Nrg混悬液相比，生物利用度增加1.56倍。动物模型未见皮肤刺激。这些研究结果表明，Nrg- nlc - cp凝胶提供了一种非侵入性和有效的替代方案，可以改善Nrg的渗透性和全身可用性，从而潜在地提高糖尿病治疗的治疗效果和患者依从性。

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来源期刊

Biopolymers 生物-生化与分子生物学

CiteScore

5.30

自引率

0.00%

发文量

审稿时长

3 months

期刊介绍： Founded in 1963, Biopolymers publishes strictly peer-reviewed papers examining naturally occurring and synthetic biological macromolecules. By including experimental and theoretical studies on the fundamental behaviour as well as applications of biopolymers, the journal serves the interdisciplinary biochemical, biophysical, biomaterials and biomedical research communities.