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用于提高硫唑嘌呤口服生物利用度的胆酸接枝硫醇化壳聚糖包封纳米脂质体：体外和体内评价

Cholic Acid-Grafted Thiolated Chitosan-Enveloped Nanoliposomes for Enhanced Oral Bioavailability of Azathioprine: In Vitro and In Vivo Evaluation.

作者信息

Arshad Muqeeza, Sarwar Hafiz Shoaib, Sarfraz Muhammad, Jalil Aamir, Bin Jardan Yousef A, Farooq Umer, Sohail Muhammad Farhan

机构信息

Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore Campus, 54660 Lahore, Pakistan.

Faculty of Pharmaceutical Sciences, University of Central Punjab, 54000 Lahore, Pakistan.

出版信息

ACS Omega. 2024 Jul 16;9(30):32807-32816. doi: 10.1021/acsomega.4c03369. eCollection 2024 Jul 30.

DOI:10.1021/acsomega.4c03369
PMID:39100346
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11292647/
Abstract

The purpose of the present study was to develop a cholic acid-grafted thiolated chitosan (CA-CS-TGA) polymeric biomaterial for attaining improved permeation via attaching thiol groups and cholic acid moieties. For this purpose, a CA-CS-TGA graft was prepared, and modification was confirmed via FTIR analysis. The prepared CA-CS-TGA graft was used to coat the azathioprine-loaded nanoliposomes (ENLs), with subsequent characterization in terms of zeta size, zeta potential, and SEM analysis. Pharmaceutical evaluation was carried out in terms of drug release studies, and ex vivo permeation and in vivo oral bioavailability were studied. The particle size and zeta potential of CA-CS-TGA coated nanoliposomal formulation CA-CS-TGA-NLs were found to be 245 ± 15.6 and +22.4 ± 0.58, respectively, compared to that of nonenveloped nanoliposomal formulation 165.7 ± 12.3 and -21.8 ± 0.14, respectively, indicating successful coating. CA-CS-TGA-NLs indicated 64% of drug release in 24 h at pH 7.4. Ex vivo permeation enhancement and relative oral bioavailability studies indicated a 2.84-fold enhanced permeation and 6-fold enhanced oral bioavailability of CA-CS-TGA-NLs compared to Azathioprine suspension. Based on the results, it can be concluded that grafting the CA-CS-TGA polymer onto nanoliposomes seems to be a promising strategy to enhance the oral bioavailability of Azathioprine.

摘要

本研究的目的是开发一种胆酸接枝的硫醇化壳聚糖（CA-CS-TGA）聚合物生物材料，通过连接硫醇基团和胆酸部分来实现改善渗透。为此，制备了CA-CS-TGA接枝物，并通过傅里叶变换红外光谱（FTIR）分析确认了改性。将制备的CA-CS-TGA接枝物用于包被载有硫唑嘌呤的纳米脂质体（ENLs），随后进行zeta粒径、zeta电位和扫描电子显微镜（SEM）分析表征。从药物释放研究方面进行了药学评价，并研究了体外渗透和体内口服生物利用度。发现与未包被的纳米脂质体制剂（分别为165.7±12.3和-21.8±0.14）相比，CA-CS-TGA包被的纳米脂质体制剂CA-CS-TGA-NLs的粒径和zeta电位分别为245±15.6和+22.4±0.58，表明包被成功。CA-CS-TGA-NLs在pH 7.4条件下24小时内药物释放率为64%。体外渗透增强和相对口服生物利用度研究表明，与硫唑嘌呤混悬液相比，CA-CS-TGA-NLs的渗透增强了2.84倍，口服生物利用度提高了6倍。基于这些结果，可以得出结论，将CA-CS-TGA聚合物接枝到纳米脂质体上似乎是提高硫唑嘌呤口服生物利用度的一种有前景的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/1c819b221d72/ao4c03369_0009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/003584dc1c58/ao4c03369_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/99b327828ed0/ao4c03369_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/81aece871110/ao4c03369_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/2805f9b9eda5/ao4c03369_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/57e84d0c62f9/ao4c03369_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9939/11292647/1c819b221d72/ao4c03369_0009.jpg

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