Nanostructured Lipid Carriers-Based Topical Gel of Betulinic Acid: In Vitro, In Vivo Evaluation and Dermatokinetic Analysis

IF 1.7 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Xin Wang, Yangnan Chen, Yan Liu, Danqing Wu, Yanqiu Long, Shuangying Gui, Zhiyun Zheng, Ning He
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Abstract

The aim of this study was to improve the penetration of betulinic acid (BA) into skin efficiently by incorporating it into a nanostructured lipid carrier (NLC)-based gel. BA-NLC was prepared by the melt-emulsification and low-temperature solidification method. The optimized formulation was incorporated into the hydrogel and evaluated for pH, in vitro release, occlusion factor, and dermatokinetics. Furthermore, the transdermal penetration mechanism of the NLC gel was investigated by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), skin histological staining, and fluorescence microscopic methods. The optimized NLC showed a particle size of 153.40 nm and a high EE of 86.21%. In vitro drug release behavior of the BA-NLC gel showed higher cumulative release at 24 h (67.17 ± 2.39%) compared to the free drug (57.53 ± 2.17%). In vivo dermatokinetic studies disclosed that the BA-NLC gel presented elevated Cmax and AUC0–24 in the epidermis and dermis in contrast to the conventional gel. FT-IR and DSC research indicated that the NLC formulations changed the configuration of skin keratin and augmented lipid fluidity, thus facilitating the percutaneous permeability of actives. Fluorescence microscopy also indicated improved skin penetration of the BA-NLC gel. Hence, the optimized NLC gel could potentially be a promising drug nanocarrier to boost skin drug penetration and retention.

Abstract Image

基于纳米结构脂质载体的白桦酸局部凝胶:体外、体内评价和皮肤动力学分析。
本研究的目的是通过将白桦酸(BA)掺入纳米结构脂质载体(NLC)凝胶中,提高白桦酸(BA)对皮肤的渗透效率。采用熔融乳化-低温凝固法制备BA-NLC。将优化后的配方加入水凝胶中,并对pH、体外释放、遮挡因子和皮肤动力学进行评价。采用傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)、皮肤组织染色和荧光显微镜等方法研究了NLC凝胶的透皮渗透机理。优化后的NLC粒径为153.40 nm, EE高达86.21%。BA-NLC凝胶的体外释药行为显示,24 h累积释药量(67.17±2.39%)高于游离释药量(57.53±2.17%)。体内皮肤动力学研究表明,与常规凝胶相比,BA-NLC凝胶在表皮和真皮中的Cmax和AUC0-24含量升高。FT-IR和DSC研究表明,NLC配方改变了皮肤角蛋白的结构,增加了脂质流动性,从而促进了活性物质的透皮性。荧光显微镜也显示BA-NLC凝胶的皮肤渗透性提高。因此,优化后的NLC凝胶可能是一种有潜力的药物纳米载体,可以促进皮肤药物的渗透和滞留。
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来源期刊
CiteScore
3.60
自引率
0.00%
发文量
35
审稿时长
6-12 weeks
期刊介绍: Biopharmaceutics & Drug Dispositionpublishes original review articles, short communications, and reports in biopharmaceutics, drug disposition, pharmacokinetics and pharmacodynamics, especially those that have a direct relation to the drug discovery/development and the therapeutic use of drugs. These includes: - animal and human pharmacological studies that focus on therapeutic response. pharmacodynamics, and toxicity related to plasma and tissue concentrations of drugs and their metabolites, - in vitro and in vivo drug absorption, distribution, metabolism, transport, and excretion studies that facilitate investigations related to the use of drugs in man - studies on membrane transport and enzymes, including their regulation and the impact of pharmacogenomics on drug absorption and disposition, - simulation and modeling in drug discovery and development - theoretical treatises - includes themed issues and reviews and exclude manuscripts on - bioavailability studies reporting only on simple PK parameters such as Cmax, tmax and t1/2 without mechanistic interpretation - analytical methods
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