罗勒籽黏液作为一种生物黏附聚合物:萘普生钠微球和栓剂的体外和离体研究。

IF 3.4 Q2 CHEMISTRY, MEDICINAL ADMET and DMPK Pub Date : 2024-10-03 eCollection Date: 2024-01-01 DOI:10.5599/admet.2372
Devika Tripathi, Krislay Rathour, Prashant Pandey, Ritesh Kumar Tiwari, Awani Kumar Rai
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引用次数: 0

摘要

背景与目的:本研究探讨罗勒种子粘液作为萘普生钠的生物黏附载体,证明其在直肠给药时能够提高溶解度。通过红外光谱和x射线衍射分析,证实了从罗勒种子中提取的黏液具有生物黏附性能和热稳定性。实验方法:采用双乳液溶剂蒸发技术制备微球,改变聚合物比以优化给药效果。关键结果:粒径范围为456±0.51 ~ 712±0.21 μm,黏液浓度越高,黏度越大,形成的微球越大。包封率在45.01±0.25% ~ 79.4±0.93%之间,随罗勒/海藻酸盐比例的增加而提高。优质批次OBM5在离体试验中表现出优异的黏附性,这归因于聚合物含量的增加,促进了与直肠粘膜的相互作用。SEM分析表明,OBM5为球形整体结构,有利于自由流动。药物释放效率高,7 h后OBM5达到88.7±1.3%,缓释效果良好。结论:聚乙二醇(PEG) 4000栓剂在缓冲液中溶解25分钟即可完全溶解。罗勒籽黏液对直肠粘膜的生物粘附力显著增强,达到6.44±0.58 g,与黏液浓度相关。这些发现强调罗勒种子粘液作为直肠给药系统的生物粘合剂生物聚合物的功效。
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Basil seed mucilage as a bioadhesive polymer: Development of naproxen sodium microspheres and suppositories with in-vitro and ex-vivo studies.

Background and purpose: The study explores basil seed mucilage as a bioadhesive carrier for naproxen sodium, demonstrating its ability to enhance solubility when administered rectally. The mucilage, derived from Ocimum basilicum seeds, showed bioadhesive properties and thermal stability, as confirmed by FTIR spectroscopy and X-ray diffraction analysis.

Experimental approach: Microspheres were prepared using a double emulsion solvent evaporation technique, varying polymer ratios to optimize drug delivery.

Key results: Particle size analysis revealed a range of 456±0.51 to 712±0.21 μm, with larger microspheres formed at higher mucilage concentrations due to increased viscosity. Encapsulation efficiency ranged from 45.01±0.25 % to 79.4±0.93 %, improving with higher basil/alginate ratios. The superior batch, OBM5, showed excellent mucoadhesive qualities in ex-vivo assays, attributed to the increased polymer content, facilitating interaction with rectal mucosa. SEM analysis of OBM5 indicated a spherical, monolithic structure conducive to free flow. Drug release was efficient, with OBM5 achieving 88.7±1.3 % after 7 hours, indicating a controlled release profile.

Conclusion: Incorporated into polyethylene glycol (PEG) 4000 suppositories, supposetories were completely disintegrated in buffer solution within 25 minutes. The bioadhesive force of basil seed mucilage on rectal mucosa was significantly enhanced, reaching 6.44±0.58 g, correlating with mucilage concentration. These findings underscore the efficacy of basil seed mucilage as a bioadhesive biopolymer for rectal drug delivery systems.

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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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