{"title":"尿囊素局部制剂研究:体外药物释放研究和流变特性。","authors":"Alisa Elezović, Amar Elezović, Miroslav Hadnađev, Adna Džemat, Emina Hrnčić, Belma Imamović, Ervina Bečić, Veljko Krstonošić","doi":"10.1080/10837450.2024.2414938","DOIUrl":null,"url":null,"abstract":"<p><p>The extent and rate of release of active substances from topical products must be sufficient to ensure their effectiveness, which depends on selecting the most appropriate formulation. This study examined allantoin emulsions and gel formulations. In water-in-oil (W/O) and oil-in-water (O/W) emulsions, the main emulsifier was varied, while the same gelling agent was used in all formulations to test the effects of oil phase presence and emulsifier type on allantoin release, as well as the formulations' rheological and textural characteristics. O/W emulsions exhibited similar release rates and the overall amount released over six hours (11-14.8%), while the highest amount of allantoin (20.9%) was released from the gel formulation. Conversely, the amount of allantoin released from the W/O emulsion (0.77%) was insufficient. Experimental data generally fit best with the Higuchi model kinetics. The formulations demonstrated shear-thinning thixotropic behavior. The greatest deviation from the Newtonian type of flow, with the smallest value of constant n (0.106-0.13) and the largest thixotropic loop area (6602.67-8140 Pas<sup>-1</sup>) were shown by O/W emulsions. The W/O emulsion exhibited the highest constant n (0.70) and smaller hysteresis area (991.23 Pas<sup>-1</sup>). Firmness and consistency values increased in the order: gel < W/O emulsion < O/W emulsions. The O/W emulsions showed similarity in microstructure and textural characteristics, likely explaining their similar release behavior.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1033-1041"},"PeriodicalIF":2.6000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Studies on allantoin topical formulations: in vitro drug release studies and rheological characteristics.\",\"authors\":\"Alisa Elezović, Amar Elezović, Miroslav Hadnađev, Adna Džemat, Emina Hrnčić, Belma Imamović, Ervina Bečić, Veljko Krstonošić\",\"doi\":\"10.1080/10837450.2024.2414938\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The extent and rate of release of active substances from topical products must be sufficient to ensure their effectiveness, which depends on selecting the most appropriate formulation. This study examined allantoin emulsions and gel formulations. In water-in-oil (W/O) and oil-in-water (O/W) emulsions, the main emulsifier was varied, while the same gelling agent was used in all formulations to test the effects of oil phase presence and emulsifier type on allantoin release, as well as the formulations' rheological and textural characteristics. O/W emulsions exhibited similar release rates and the overall amount released over six hours (11-14.8%), while the highest amount of allantoin (20.9%) was released from the gel formulation. Conversely, the amount of allantoin released from the W/O emulsion (0.77%) was insufficient. Experimental data generally fit best with the Higuchi model kinetics. The formulations demonstrated shear-thinning thixotropic behavior. The greatest deviation from the Newtonian type of flow, with the smallest value of constant n (0.106-0.13) and the largest thixotropic loop area (6602.67-8140 Pas<sup>-1</sup>) were shown by O/W emulsions. The W/O emulsion exhibited the highest constant n (0.70) and smaller hysteresis area (991.23 Pas<sup>-1</sup>). Firmness and consistency values increased in the order: gel < W/O emulsion < O/W emulsions. 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引用次数: 0
摘要
外用产品释放活性物质的程度和速度必须足以确保其有效性,这取决于选择最合适的配方。本研究考察了尿囊素乳液和凝胶配方。在油包水(W/O)乳剂和水包油(O/W)乳剂中,主要乳化剂各不相同,而在所有配方中都使用了相同的胶凝剂,以测试油相存在和乳化剂类型对尿囊素释放的影响,以及配方的流变和质地特性。油相/水相乳剂的释放率和六小时内释放的总量(11-14.8%)相似,而凝胶配方释放的尿囊素量最高(20.9%)。相反,W/O 型乳液释放的尿囊素量不足(0.77%)。实验数据一般最符合樋口动力学模型。配方表现出剪切稀化触变性。O/W 型乳液与牛顿型流动的偏差最大,常数 n 值最小(0.106-0.13),触变环面积最大(6602.67-8140 Pas-1)。W/O 型乳液的常数 n 值最高(0.70),滞后面积较小(991.23 Pas-1)。硬度和稠度值的增加顺序为:凝胶
Studies on allantoin topical formulations: in vitro drug release studies and rheological characteristics.
The extent and rate of release of active substances from topical products must be sufficient to ensure their effectiveness, which depends on selecting the most appropriate formulation. This study examined allantoin emulsions and gel formulations. In water-in-oil (W/O) and oil-in-water (O/W) emulsions, the main emulsifier was varied, while the same gelling agent was used in all formulations to test the effects of oil phase presence and emulsifier type on allantoin release, as well as the formulations' rheological and textural characteristics. O/W emulsions exhibited similar release rates and the overall amount released over six hours (11-14.8%), while the highest amount of allantoin (20.9%) was released from the gel formulation. Conversely, the amount of allantoin released from the W/O emulsion (0.77%) was insufficient. Experimental data generally fit best with the Higuchi model kinetics. The formulations demonstrated shear-thinning thixotropic behavior. The greatest deviation from the Newtonian type of flow, with the smallest value of constant n (0.106-0.13) and the largest thixotropic loop area (6602.67-8140 Pas-1) were shown by O/W emulsions. The W/O emulsion exhibited the highest constant n (0.70) and smaller hysteresis area (991.23 Pas-1). Firmness and consistency values increased in the order: gel < W/O emulsion < O/W emulsions. The O/W emulsions showed similarity in microstructure and textural characteristics, likely explaining their similar release behavior.
期刊介绍:
Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology.
Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as:
-Preformulation and pharmaceutical formulation studies
-Pharmaceutical materials selection and characterization
-Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation
-QbD in the form a risk assessment and DoE driven approaches
-Design of dosage forms and drug delivery systems
-Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies
-Drug delivery systems research and quality improvement
-Pharmaceutical regulatory affairs
This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.