Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon.

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-06 DOI:10.1080/10837450.2024.2321250
Fatemeh Soltani, Hossein Kamali, Abbas Akhgari, Hadi Afrasiabi Garekani, Ali Nokhodchi, Fatemeh Sadeghi
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Abstract

The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the descending colon. Pellets containing budesonide (1.5%w/w), PVP K30 (5%w/w), lactose monohydrate (25%w/w) and Avicel pH 102 (68.5%w/w) were prepared using extrusion spheronization technique. Coating formulations were designed using response surface methodology with pH and time-dependent Eudragits. Dissolution tests were conducted at different pH levels (1.2, 6.5, 6.8, and 7.2). Optimal coating formulation, considering coating level and the Eudragit (S + L) ratio to the total coating weight, was determined. Budesonide pellets were coated with the optimized composition and subjected to continuous dissolution testing simulating the gastrointestinal tract. The coating, with 48% S, 12% L, and 40% RS at a 10% coating level, demonstrated superior budesonide delivery to the descending colon. Coated pellets had a spherical shape with a uniform 30 µm thickness coating, exhibiting pH and time-dependent release. Notably, zero-order release kinetics was observed for the last 9 h in colonic conditions. The study suggests that an optimized single-layer coating, incorporating pH and time-dependent polymers, holds promise for consistently delivering budesonide to the descending colon.

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用于将布地奈德颗粒靶向送入降结肠的单层包衣的配制和优化。
目前的布地奈德制剂不足以治疗左侧结肠炎,患者可能会对长期使用灌肠器犹豫不决。本研究的重点是开发一种针对降结肠的布地奈德颗粒单层包衣。采用挤压球化技术制备了含有布地奈德(1.5%w/w)、PVP K30(5%w/w)、一水乳糖(25%w/w)和 Avicel pH 102(68.5%w/w)的颗粒。采用响应面方法设计了包衣配方,并使用了与 pH 值和时间相关的 Eudragits。在不同的 pH 值(1.2、6.5、6.8 和 7.2)下进行了溶解试验。考虑到包衣量和 Eudragit(S + L)占包衣总重量的比例,确定了最佳包衣配方。布地奈德颗粒包衣了优化后的成分,并进行了模拟胃肠道的连续溶出试验。在 10%的包衣水平下,包衣中 S 含量为 48%,L 含量为 12%,RS 含量为 40%。包衣颗粒呈球形,包衣厚度均匀为 30 微米,其释放量与 pH 值和时间有关。值得注意的是,在结肠条件下的最后 9 小时内,观察到了零阶释放动力学。研究表明,优化的单层包衣结合了与 pH 值和时间相关的聚合物,有望将布地奈德持续释放到降结肠。
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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
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.
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