Application of cosolvency and cocrystallization approach to enhance acyclovir solubility

IF 4.3 2区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

BMC Chemistry Pub Date : 2025-07-30 DOI:10.1186/s13065-025-01591-2

Elham Azad Khiabani, Abolghasem Jouyban, Anahita Fathi Azarbayjani

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Abstract

Acyclovir (ACY) is a commonly used antiviral drug with limited aqueous solubility and poor permeability. It is administered via oral and intravenous routes. The aim of this work is to employ cocrystallization and cosolvency method to improve the solubility of orally administered dosage forms, including tablet and oral solution. Cocrystallization is carried out through the solvent evaporation method using different types of coformers including formic acid (FA), tartaric acid (TA), and ascorbic acid (AA). The physical states of the obtained samples were characterized by differential scanning calorimeter (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). The solubility of the developed samples were evaluated and compared with those of the parent drug. DSC and XRD findings indicate that ACY-AA and ACY-TA may be classified as cocrystals. Physicochemical characterization of ACY-FA did not demonstrate any change with respect to the parent drug. ACY-AA had the highest increase in drug solubility and created almost 3 folds enhancement. In another approach, cosolvency was employed to study the solubilization enhancement of 6 different binary solvent mixtures at 298.15 K. PEG 400 + water at 0.5:0.5 demonstrated a twofold enhancement in drug solubility. Both cocrystallization and cosolvency method seem effective in enhancing drug solubility and have the potential to be employed for the development of oral drug delivery systems including tablets and oral suspensions. The findings of this work suggest that ACY solubility can be enhanced by proper choice of the coformer and cosolvent. The result of this finding is beneficial for the development of acyclovir dosage forms.

Graphical abstract

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应用共溶和共结晶方法提高阿昔洛韦溶解度。

无环鸟苷（ACY）是一种常用的抗病毒药物，其水溶性有限，渗透性差。它通过口服和静脉注射给药。本研究的目的是采用共结晶和共溶的方法来提高口服剂型的溶解度，包括片剂和口服液。采用甲酸（FA）、酒石酸（TA）和抗坏血酸（AA）等不同类型的共形物通过溶剂蒸发法进行共结晶。采用差示扫描量热仪（DSC）、x射线衍射仪（XRD）和傅里叶变换红外光谱（FT-IR）对所得样品的物理状态进行了表征。评价了制备样品的溶解度，并与母体药物的溶解度进行了比较。DSC和XRD结果表明，ACY-AA和ACY-TA可归类为共晶。ACY-FA的理化性质没有显示出与母体药物有关的任何变化。ACY-AA的药物溶解度提高幅度最大，几乎达到3倍。在298.15 K下，用共溶度法研究了6种不同二元溶剂混合物的增溶增强作用。PEG 400 +水在0.5:0.5时，药物溶解度提高了两倍。共结晶和共溶方法似乎都有效地提高了药物的溶解度，并有潜力用于开发口服药物给药系统，包括片剂和口服混悬液。本研究结果表明，通过选择合适的共溶剂和助溶剂，可以提高ACY的溶解度。这一发现的结果对阿昔洛韦剂型的开发是有益的。

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来源期刊

BMC Chemistry Chemistry-General Chemistry

CiteScore

5.30

自引率

2.20%

发文量

审稿时长

27 weeks

期刊介绍： BMC Chemistry, formerly known as Chemistry Central Journal, is now part of the BMC series journals family. Chemistry Central Journal has served the chemistry community as a trusted open access resource for more than 10 years – and we are delighted to announce the next step on its journey. In January 2019 the journal has been renamed BMC Chemistry and now strengthens the BMC series footprint in the physical sciences by publishing quality articles and by pushing the boundaries of open chemistry.