Optimization and Transfollicular Delivery of Finasteride Loaded PLGA Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth Stimulation

Q2 Pharmacology, Toxicology and Pharmaceutics

Current Bioactive Compounds Pub Date : 2024-01-19 DOI:10.2174/0115734072269998240101043601

Mounika Kuchukuntla, Venkatesan Palanivel, Ananthula Madhubabu

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引用次数: 0

Abstract

One of the frequent side effects of cancer treatment is chemotherapyinduced alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor, has shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side effects constrained its broad use in alopecia from oral treatment and a low absorption rate at the target site— PLGA-loaded nanoparticles (NPs) for topical delivery of FNS—to overcome these issues. The nano-precipitation process was used to make FNS-NPs. The independent variables (stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on the point prediction method obtainable by the Box Behnken design software, the best FNS-NPs composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal FNS-NPs composition was further transformed into a gel formulation. The prepared topical gel formulation (FNS-NPs gel) included gel characterization, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), invitro and in vivo studies. Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI, 71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content, viscosity, pH, and spreadability. According to the release and permeation investigation findings, FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before. In a dose- and time-dependent manner, the produced nanoparticles considerably (p≤0.05) increased FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery mechanism of the FNS-NPs gel might stimulate hair growth. These findings imply that the innovative formulation that has been developed has several beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata

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非那雄胺负载型聚乳酸（PLGA）纳米颗粒（载Carbopol凝胶）用于刺激毛发生长治疗的优化和经叶脉给药

化疗引起的脱发（CIA）是癌症治疗的常见副作用之一。脱发带来的心理不适可能会导致患者停止接受化疗，从而降低治疗效果。非那雄胺（FNS）是一种 JAK 抑制剂，在治疗秃头方面显示出巨大的治疗前景。然而，全身性的副作用限制了它在脱发治疗中的广泛应用，而口服治疗和用于局部给药的低吸收率靶点--PLGA负载纳米颗粒（NPs）则可以克服这些问题。自变量（稳定剂和聚合物）为 PLGA（X1）、P407（X2）和超声时间（X3）。根据 Box Behnken 设计软件得出的点预测方法，选出了最佳 FNS-NPs 成分。用包封效率、粒度、ZETA电位和多分散指数来表征纳米颗粒。使用 Carbopol 作为聚合物，将理想的 FNS-NP 组合物进一步转化为凝胶配方。制备的外用凝胶配方（FNS-NPs 凝胶）包括凝胶表征、动态光散射（DLS）、扫描电子显微镜（SEM）、粉末 X 射线衍射（PXRD）、差示扫描量热仪（DSC）、傅立叶变换红外光谱（FTIR）、体内外研究。优化后的 FNS-NPs (F13) 粒径为 175.26±3.85 nm，PDI 为 0.241±0.11，EE 为 71.04±1.35%，表面电荷为-33.27±0.39。傅立叶变换红外光谱研究表明，药物与辅料之间没有相互作用。在 X 射线衍射图中可以看到 FNS 包裹在聚合物基质中。所开发的 FNS-NPs 凝胶配方显示出理想的药物含量、粘度、pH 值和铺展性。释放和渗透研究结果表明，FNS释放缓慢（68.73±0.94%），但渗透膜比以前明显增加。与FNS溶液相比，在剂量和时间依赖性方面，所制备的纳米颗粒大大增加了FNS的给药量（p≤0.05）。FNS-NPs凝胶疗法能显著增加毛囊的数量和大小，这与剂量有关。1% FNSNPs凝胶和2%米诺西地溶液的效果相当。72 小时后，FNS-NPs 凝胶未显示皮肤刺激迹象。这些研究结果表明，所开发的创新配方具有多种有益特性，适合用于治疗脱发症的 FNS 皮肤给药。

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来源期刊

Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.90

自引率

0.00%

发文量

112

期刊介绍： The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.