吡罗昔康糖化壳聚糖稳定透皮贴剂的制备与表征

IF 1.7 4区 化学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Sajid Raza, Muhammad Akhlaq, Aisha Siddiqua, Rukhshnda Habib, Khalid J. Alzahrani, Khalaf F. Alsharif, Abul Kalam Azad
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引用次数: 0

摘要

目的:设计经皮给药系统,通过皮肤将药物输送到血液中。方法:采用乙二醇壳聚糖为透皮剂,制备吡罗昔康缓释贴剂,以解决胃溃疡和频繁给药的问题。采用不同比例的壳聚糖和乙二醇壳聚糖制备基质型吡罗昔康贴剂,以达到药物控释和促透的目的。结果和讨论:制备的贴片具有一致的药物含量、重量均匀性、折叠耐久性、拉伸强度和吸湿/损失值。该研究的一个关键新颖之处在于使用乙二醇壳聚糖作为渗透促进剂,显著提高了吡罗昔康在体内的生物利用度。乙二醇壳聚糖改变了角质层的蛋白质结构,影响了颗粒层的紧密连接,导致角质层含水量增加和细胞间脂质的改变。还评估了贴片的稳定性和皮肤敏感性。兔皮Franz扩散池体外释放实验表明,该药物的释放动力学符合非菲克零阶模型。稳定性研究表明,随着时间的推移,贴片特性没有显著变化。乙二醇壳聚糖含量最高的配方FPRXG6具有最大的皮肤通透性和最高的血药浓度(Cmax = 15.87 ± 2.35 ng/mL)。结论:该制剂提高并延长了生物利用度,使血浆药物水平维持在治疗范围内。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Fabrication and Characterization of Piroxicam-Loaded Glycolated Chitosan-Stabilized Transdermal Patch

Fabrication and Characterization of Piroxicam-Loaded Glycolated Chitosan-Stabilized Transdermal Patch

Objective: The transdermal drug delivery system is designed to transport drugs into the bloodstream through the skin. Methods: A controlled-release transdermal patch of piroxicam was developed using glycol chitosan as a permeation enhancer to address issues related to gastric ulcers and frequent dosing. Matrix-type piroxicam patches were prepared using chitosan and glycol chitosan in various ratios to achieve controlled drug release and enhanced skin penetration. Results and Discussion: The prepared patches demonstrated consistent drug content, weight uniformity, folding endurance, tensile strength, and moisture uptake/loss values. A key novelty of the study is the use of glycol chitosan as a permeation enhancer, which significantly improved the bioavailability of piroxicam in vivo. Glycol chitosan was found to alter the protein structure of the stratum corneum and affect tight junctions in the granular layer, leading to increased water content and modification of intercellular lipids in the stratum corneum. The patches were also evaluated for stability and skin sensitivity. In vitro release studies using a Franz diffusion cell with rabbit skin revealed that the drug release kinetics followed a non-Fickian and zero-order model. Stability studies indicated no significant changes in patch characteristics over time. The formulation FPRXG6, which contained the highest concentration of glycol chitosan, exhibited maximum skin permeability and the highest plasma drug concentration (Cmax = 15.87 ± 2.35 ng/mL). Conclusions: These findings suggest that the formulation enhances and prolongs bioavailability, maintaining plasma drug levels within the therapeutic range.

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来源期刊
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry 生物-生化与分子生物学
CiteScore
1.80
自引率
10.00%
发文量
118
审稿时长
3 months
期刊介绍: Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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