Towards Enhanced Solubility of Cannabidiol: Preparation and Evaluation of Cannabidiol Solid Dispersions Using Vacuum Compression Molding

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2025-03-11 DOI:10.1208/s12249-025-03078-8

Achref Cherif, Janhavi Deshmukh, Kavish Sanil, Iman Taha, Daniel Treffer, Eman A. Ashour

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引用次数: 0

Abstract

The present study aims to develop and characterize cannabidiol (CBD) solid dispersions using Vacuum Compression Molding (VCM) to enhance the drug solubility and release profile. Solid dispersions of CBD and polymers were processed using VCM at 130 °C for 4 min after a prior physical mixing. Five percent w/w of CBD was used with 5% w/w of poloxamer 188 and 90% w/w of polymeric carrier (Polyethylene Oxide, PEO-N80 or Hydroxypropyl cellulose, HPCEF). Discs were collected and milled to obtain formulations (F1V, F2V). The degradation temperature of CBD was determined using Thermogravimetric Analysis (TGA). The formulations were further characterized using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-Transform Infrared Spectroscopy (FTIR). In vitro dissolution testing of pure CBD and formulations was evaluated using USP apparatus II. TGA showed that CBD degradation occurs after 200 °C. FTIR spectra of formulations indicate potential interactions between the drug and polymers. DSC thermograms of F1V showed a thermal peak at 65 °C that could correspond to PEO-N80. F2V did not show any of the thermal event peaks, which suggests the conversion of the drug to the amorphous state. Images from the SEM showed irregular surfaces for both formulations. The release profile showed an increase in the CBD dissolution rate by 4.75 folds for F1V and 3.63 folds for F2V in four hours. In this study, solid dispersions of CBD formulations were successfully achieved. The VCM technology has proven to be successful in formulating solid dispersions of CBD for early-stage drug development.

Graphical Abstract

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提高大麻二酚的溶解度：真空压缩成型大麻二酚固体分散体的制备和评价

本研究旨在利用真空压缩成型（VCM）技术开发和表征大麻二酚（CBD）固体分散体，以提高药物的溶解度和释放特性。在事先的物理混合后，使用VCM在130°C下处理CBD和聚合物的固体分散体4分钟。5% w/w的CBD与5% w/w的poloxam188和90% w/w的聚合物载体（聚乙烯氧化物，PEO-N80或羟丙基纤维素，HPCEF）一起使用。收集圆盘并研磨得到配方（F1V, F2V）。采用热重分析法（TGA）测定了CBD的降解温度。采用差示扫描量热法（DSC）、扫描电镜（SEM）和傅里叶变换红外光谱（FTIR）对配方进行了进一步表征。使用USP仪器II评估纯CBD和制剂的体外溶出度。TGA结果表明，CBD在200℃后发生降解。配方的FTIR光谱显示药物和聚合物之间潜在的相互作用。F1V的DSC热图显示，在65°C处有一个与PEO-N80对应的热峰。F2V没有显示出任何热事件峰，这表明药物已转化为非晶态。扫描电镜图像显示两种配方的表面不规则。释放谱显示，在4小时内，F1V和F2V的CBD溶出率分别提高了4.75倍和3.63倍。在本研究中，成功地实现了CBD制剂的固体分散。VCM技术已被证明是成功的，在制定固体分散的CBD早期药物开发。图形抽象

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.