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基于聚乙烯吡咯烷酮 K-30 的交联快速溶胀纳米凝胶:改善药物溶解度的完美方法。

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.

机构信息

College of Pharmacy, University of Sargodha, Sargodha City Punjab, Pakistan.

Quaid-e-Azam College of Pharmacy, Sahiwal, Punjab, Pakistan.

出版信息

Biomed Res Int. 2022 Aug 26;2022:5883239. doi: 10.1155/2022/5883239. eCollection 2022.

Abstract

Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug's solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with 178.99 ± 15.32 nm, and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.

摘要

溶解度差是众多制药行业面临的全球性问题,因为大量处于研发阶段和已上市的药物溶解度较差,导致溶解度低,最终需要增加剂量。本研究旨在开发一种基于聚乙烯吡咯烷酮(PVP-K30)的纳米凝胶给药系统,以提高难溶性药物奥氮平(OLP)的溶解度,因为增溶是纳米系统最值得注意的应用。通过交联聚合和随后的缩合技术合成纳米凝胶,这是一种对药物溶解度具有高响应性的聚合物网络。所开发的纳米凝胶通过包封效率、溶胶-凝胶、溶胀度、载药量(%DLC)、孔隙率、稳定性、溶解度、体外溶解研究、FTIR、XRD 和 SEM 分析进行了表征。此外,还对兔子进行了细胞毒性研究,以检查系统的生物相容性。纳米凝胶的粒径为 178.99 ± 15.32nm,体外溶解研究表明,与市售奥氮平制剂相比,药物释放性能得到了显著提高。溶解度研究表明,在 pH 6.8 的磷酸盐缓冲液中,OLP 的溶解度提高了 36.7 倍。体内细胞毒性研究表明,所制备的基于 PVP-K30 的制剂具有生物相容性。基于所获得的结果,所开发的 PVP-K30-共-聚(AMPS)纳米凝胶给药系统有望成为提高难溶性药物溶解度的安全、有效和具有成本效益的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/bb1def64cddd/BMRI2022-5883239.001.jpg

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