An Experimental Design Approach for Development of Crocin-Loaded Microparticles Embedded in Gelatin/Oxidized Alginate-Based Hydrogel

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2023-07-29 DOI:10.1007/s12247-023-09755-0
Faezeh Merati, Fatemeh Mehryab, Seyed Alireza Mortazavi, Azadeh Haeri
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Abstract

Purpose

The objective of this study was to prepare gelatin/oxidized alginate (OAlg) hydrogel incorporating chitosan (CS)/alginate (Alg) microparticles (MPs) for topical delivery of crocin and maintaining MPs at the target site.

Methods

Crocin-loaded MPs were prepared using the ionic gelation method, and the effects of CS, Alg, and tripolyphosphate (TPP) concentrations on particle size and entrapment efficiency% (EE) were evaluated by applying a factorial design. OAlg was synthesized, and the optimum MP formulation was loaded into gelatin/OAlg hydrogel. The developed formulation was characterized in terms of morphology, chemical structure, crystallinity, thermal behavior, viscosity, swelling behavior, mucoadhesion, and in vitro release profile.

Results

The designed particles had a size ranging from 7.2 to 47.8 µm with the EE results varying between 12.5 and 58.4%. The mathematical models with suitable determination coefficients (R2) were established which confirmed a satisfactory correlation between the independent variables and the results. The optimized formulation showed a particle size of ~ 28 µm and a zeta potential of ~ 24 mV with about 58% crocin entrapment. The successful oxidation process was confirmed by the appearance of aldehyde peak in FTIR spectroscopy, and the oxidation degree (OD) of prepared OAlg was found to be about 62%. The prepared complex could release crocin in a sustained manner through 48 h and showed superior mucoadhesive strength, compared to gelatin/Alg-based hydrogel.

Conclusion

The fabricated gelatin/OAlg hydrogel containing CS/Alg MPs exhibited the promising potential to be utilized in mucosal delivery applications.

Graphical Abstract

Abstract Image

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明胶/氧化海藻酸盐水凝胶包埋Crocin负载微粒的实验设计方法
目的 本研究旨在制备明胶/氧化藻酸盐(OAlg)水凝胶,其中包含壳聚糖(CS)/海藻酸盐(Alg)微颗粒(MPs),用于局部递送巴豆毒素,并将MPs保持在目标部位。方法 采用离子凝胶法制备了巴豆毒素载体MPs,并通过因子设计评估了CS、Alg和三聚磷酸钠(TPP)浓度对粒径和夹带效率(EE)的影响。合成了 OAlg,并将最佳 MP 配方载入明胶/OAlg 水凝胶中。所开发的配方在形态、化学结构、结晶度、热行为、粘度、溶胀行为、粘附性和体外释放曲线等方面都有特征。结果所设计的颗粒大小在 7.2 到 47.8 µm 之间,EE 结果在 12.5 到 58.4% 之间。建立的数学模型具有合适的确定系数(R2),证实了自变量与结果之间令人满意的相关性。优化配方的粒径约为 28 微米,zeta 电位约为 24 毫伏,藏有约 58% 的巴豆素。傅立叶变换红外光谱中出现的醛峰证实了氧化过程的成功,制备的 OAlg 的氧化度(OD)约为 62%。所制备的复合物可在 48 小时内持续释放巴豆素,与明胶/Alg 水凝胶相比,其粘附强度更高。
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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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