Pilot Formulation Study of Ph-sensitive Gels

European Pharmaceutical Journal Pub Date : 2023-08-24 DOI:10.2478/afpuc-2023-0005

T. Wolaschka, S. Rohaľová, I. Zelinska, Ľ. Balážová, M. Bačkorová, S. Kurhajec

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引用次数: 0

Abstract

Abstract Drugs remain for a short time on mucus membranes, such as oral, ocular, or nasal mucus, which are washed with physiological fluids. One of the possibilities to overcome this obstacle is the application of solutions that, due to the physiological environment or stimulus, turn into more viscous gels. These gels often also have mucoadhesive properties and the drug is released from them for a longer period. Carbomer 940 (C940), polycarbophil (PCP), and chitosan (CH) are gel-forming excipients, and the consistency of their solutions changes due to the concentration of protons (pH); therefore, they are referred to as pH-sensitive gelling agents. The aim of this study was to prepare pH-sensitive solutions that form gels in the pH of the oral cavity. We prepared water solutions with various concentrations of gel-forming excipients and evaluated the appearance, pH of the solution, injectability of the solution, and pH of gelation. By determining the pH of gelation, suitable concentrations (w/w) of the used polymers were found, namely, 0.1% C940, 0.225% PCP, and 2.5% CH with medium molecular weight (CHM). The 0.1% C940 and 0.225% PCP solutions were injectable through the syringe with the smallest 0.5 mm needle diameter. The 2.5% CHM solution was not injectable even through the syringe with the largest 0.8 mm needle diameter. Solgels prepared at the determined concentrations were evaluated by a dissolution test in a pH 6.8 phosphate buffer using methylene blue (MB) as a model substance. After 60 min of dissolution, 77.04% ± 5.94%, 48.85% ± 5.74%, and 77.35% ± 4.98% of MB were released from samples with C940, PCP, and CHM, respectively. The dissolution of the C940 and CHM samples took place according to the Korsmeyer–Peppas kinetic model (R2 0.999 ± 0.001, 0.978 ± 0.003) and of the PCP samples took place according to the first-order model (R2 0.994 ± 0.001). The 0.225% PCP pH-sensitive gel showed the most advantageous properties in terms of injectability, pH gelation, and prolonged release of MB.

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ph敏感凝胶的中试配方研究

摘要药物在粘膜上停留的时间很短，如用生理液冲洗的口腔粘液、眼粘液或鼻腔粘液。克服这一障碍的可能性之一是应用溶液，由于生理环境或刺激，这些溶液会变成更粘稠的凝胶。这些凝胶通常还具有粘膜粘附特性，并且药物从凝胶中释放的时间更长。卡波姆940（C940）、聚卡波姆（PCP）和壳聚糖（CH）是凝胶形成赋形剂，其溶液的稠度因质子浓度（pH）而变化；因此，它们被称为pH敏感胶凝剂。本研究的目的是制备在口腔pH值下形成凝胶的pH敏感溶液。我们制备了具有不同浓度凝胶形成赋形剂的水溶液，并评估了溶液的外观、pH、溶液的可注射性和凝胶化的pH。通过测定凝胶化的pH，发现所用聚合物的合适浓度（w/w），即0.1%的C940、0.225%的PCP和2.5%的中等分子量（CHM）的CH。0.1%的C940和0.225%的PCP溶液可通过具有最小0.5mm针头直径的注射器注射。2.5%的CHM溶液即使通过具有最大0.8mm针头直径的注射器也不能注射。使用亚甲基蓝（MB）作为模型物质，通过在pH 6.8的磷酸盐缓冲液中的溶解测试来评估以所确定的浓度制备的溶胶凝胶。溶解60分钟后，含有C940、PCP和CHM的样品中分别释放出77.04%±5.94%、48.85%±5.74%和77.35%±4.98%的MB。C940和CHM样品的溶解根据Korsmeyer–Peppas动力学模型进行（R2 0.999±0.001，0.978±0.003），PCP样品的溶解按照一阶模型进行（R20.994±0.001）。0.225%PCP pH敏感凝胶在注射性、pH胶凝性和MB缓释方面表现出最有利的特性。

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来源期刊

European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

0.60

自引率

0.00%

发文量

期刊介绍： European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.