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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研制及研究

Basil seed mucilage as a bioadhesive polymer: Development of naproxen sodium microspheres and suppositories with and studies.

作者信息

Tripathi Devika, Rathour Krislay, Pandey Prashant, Tiwari Ritesh Kumar, Rai Awani Kumar

机构信息

PSIT-Pranveer Singh Institute of Technology (Pharmacy), Kanpur-209305, U.P., India.

Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University Lucknow- 226025, U.P., India.

出版信息

ADMET DMPK. 2024 Oct 3;12(6):881-901. doi: 10.5599/admet.2372. eCollection 2024.

DOI:10.5599/admet.2372
PMID:39713257
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11661803/
Abstract

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 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 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.

摘要

背景与目的

本研究探索了罗勒籽黏液作为萘普生钠的生物黏附载体,证明其在直肠给药时增强溶解性的能力。经傅里叶变换红外光谱(FTIR)和X射线衍射分析证实,源自罗勒籽的黏液具有生物黏附特性和热稳定性。

实验方法

采用复乳溶剂蒸发技术制备微球,通过改变聚合物比例来优化药物递送。

关键结果

粒径分析显示范围为456±0.51至712±0.21μm,由于黏度增加,在较高黏液浓度下形成更大的微球。包封率范围为45.01±0.25%至79.4±0.93%,随着罗勒/海藻酸盐比例升高而提高。最优批次OBM5在实验中表现出优异的黏膜黏附质量,这归因于聚合物含量增加,便于与直肠黏膜相互作用。OBM5的扫描电子显微镜(SEM)分析表明其为有利于自由流动的球形整体结构。药物释放有效,OBM5在7小时后达到88.7±1.3%,表明具有控释特性。

结论

将其掺入聚乙二醇(PEG)4000栓剂中,栓剂在缓冲溶液中25分钟内完全崩解。罗勒籽黏液对直肠黏膜的生物黏附力显著增强,达到6.44±0.58 g,与黏液浓度相关。这些发现强调了罗勒籽黏液作为直肠给药系统生物黏附性生物聚合物的有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/208d75261aa8/ADMET-12-2372-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/f83b31fa7817/ADMET-12-2372-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/c3943c176cf4/ADMET-12-2372-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/2b13a74c936a/ADMET-12-2372-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/6f569e6b97d4/ADMET-12-2372-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/42cd0e625627/ADMET-12-2372-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/895f48dca1f0/ADMET-12-2372-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/cb9133a4f994/ADMET-12-2372-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/208d75261aa8/ADMET-12-2372-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/f83b31fa7817/ADMET-12-2372-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/c3943c176cf4/ADMET-12-2372-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/2b13a74c936a/ADMET-12-2372-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/6f569e6b97d4/ADMET-12-2372-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/42cd0e625627/ADMET-12-2372-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/895f48dca1f0/ADMET-12-2372-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/cb9133a4f994/ADMET-12-2372-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f8/11661803/208d75261aa8/ADMET-12-2372-g008.jpg

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